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Mawlana Bhashani Science and Technology University
Santosh, Tangail-1902
Department of Pharmacy
Assignment No: 01
Assignment
on
Pharmaceutical Dosage Forms
Course Code: PHAR 2205
Course Tittle: Pharmaceutical Technology I
Submitted By Submitted To
Md. Shakil Sarker
Student ID: PHA-20008
2nd
Year, 2nd
Semester
Session: 2019-2020
Department of Pharmacy
Mawlana Bhashani Science and Technology
University
Santosh, Tangail-1902
Dr. Md. Mizanur Rahman Moghal
Professor
Department of Pharmacy
Mawlana Bhashani Science and Technology
University
Santosh, Tangail-1902
Date of Submission: November 14, 2022
Pharmaceutical Dosage Forms
Introduction to Pharmaceutical Dosage Form
Drugs are rarely delivered as pure chemical entities but are approximately usually
provided as prepared formulations i.e. dosage form. After converting them into an
appropriate dose formulation, they are delivered in several dosage forms.To create
an alternative dosage form, non-medicinal chemicals (also known as pharmaceutical
ingredients or excipients) are added. By adding pharmaceutical ingredients that
solubilize or suspend or thicken or dilute or emulsify or stabilize or preserve them,
drug dosage forms can be made more effective and appealing.
Definition of Dosage Form
Dosage forms are the mechanism by which drug molecules / APIs are administered
to areas of action inside the body to generate maximum intended benefits and the
lowest unwanted effects. OR The Dosage form is the combination of Active
Pharmaceutical Ingredients (API) and Excipients in the formulation.
Need Of Dosage Forms
Mainly depend on Patient Safety and Drug Safety/ Benefits.
1. Deliver precise dosages in a safe and easy manner. Example – Tablets, capsules,
syrups
2. Cover bitter taste or odor of drug substances. Example – Capsules, coated
tablets, flavored syrups
3. Insoluble or unstable in the selected vehicle, provide a liquid formulation of the
insoluble or unstable medication. Example –Suspension
4. Controlled-release methods prolong the duration of medication effect. Example –
Controlled release tablets, capsules, suspensions
5. After oral delivery, a drug substance is protected from stomach acid. Example –
Enteric-coated tablets
6. Provide optional drug action from topical administration sites. Example –
Ointment, cream, ear and nasal preparations
7. Drugs can be injected into the body's tissues. Example – Implants
8. Inhalation treatment is the most effective way to get optimum medication activity.
Example – Inhalants
9. Liquid dosage forms of chemicals soluble in the vehicle of your choice. Example –
Solution
10. Provide for the introduction of medication into the body’s orifice. Example –
Rectal and vaginal suppositories
11. Protection of a drug substance from atmospheric oxygen or moisture. Example –
Coated capsules, sealed ampules.
Definition of Drug (Active Pharmaceutical Ingredients)
Drogue is an old French term that means "dry herb" and is sometimes used
interchangeably with the word "drug". Chemical compounds intended for use in the
diagnosis, prevention, treatment, and management of disease(s) in humans and
other animals are referred to as "pharmaceutical products" or "pharmaceuticals".
Chemical/organic synthesis, molecular modification, and biotechnology have all been
used to produce medicines in recent years. OR The Active Pharmaceutical
Ingredient (API) is the component of a medication that creates its action.
Definition of Excipients
They do not increase or affect the therapeutic action of the active components. They
are also known as inactive components or excipients and have no pharmacological
action in general. Examples of inactive components are dyes, preservatives,
sweetening agents, binding materials, coloring agents and flavoring agents, etc
Desirable properties of dosage form:
Should:
• Convenient to handle, use and store
• Stable during storage and use
• Withstand mechanical shock during transport
• Flexibility in different drug strength
• Provide expected therapeutic effect
• Extent, drug release, onset, intensity, duration of action predictable
• Economical and elegant
Classification of Dosage Forms
SOLID DOSAGE FORM:
1. UNIT DOSAGE FORM:
● TABLETS
○ Lozenges
○ Chewable Tablets
○ Modified Release Tablets
○ Effervescent Tablets etc
● CAPSULE
○ Hard gelatin Capsule
○ Soft Gelatin Capsule
2. BULK
● INTERNAL
○ Fine Powder
○ Granules and Effervescent Granules
● EXTERNAL
○ Dentifrices (Tooth Powder)
○ Ear Powder
Liquid Dosage from
1. Biphasic
● Liquid in Liquid
○ Emulsions
● Solid in liquid
○ Suspensions
2. Monophasic
● Internal
○ Syrups
○ Elixirs
○ Linctus
○ Drops
● External
○ Liniments
○ Lotions
○ Gargles
○ Throat Paints
○ Mouth Washes
○ Sprays
○ Eye Lotions
○ Eye Drops
○ Nasal Drops
● Parenteral
3. Semisolid Dosage from
● Internal
● External
● Ointments
● Creams
● Pastes
● Jellies
Solid dosage forms
Powders
Powders are the solid dosage form of medicament, which are meant for internal or
external use. They are available in crystalline and amorphous form. In crystalline
powders the constituent atoms and molecules are packed in a regularly ordered,
repeating three-dimensional pattern. Amorphous powders are non-crystalline
materials which possess no long-range order. Any material ranging in particle size
from 0.1 to 10000 µ may be described as powder. However powders used in
pharmacy generally have a size between 0.1 to 10 µ.
The powders are generally used in the following forms:
1. Bulk powder for internal use, Eg: Fine powders or granules
2. Bulk powder for external use, Eg: snuffs, dusting powders and tooth powders.
3. Simple and compound powders for internal use.
4. Powders in the form of compressed tablets and tablet triturates.
5. Powders enclosed in cachets and capsules.
6. Insufflations: Micronized powders meant for being blown in the nasal tract, ears,
tooth
sokets, vagina etc.
7. Parenteral powders: Powders for dissolution into vehicles before injection.
Dusting Powder
Dusting powders are meant for application to the intact or broken skin.
They are meant for external applications.
Desired Property:
1. Ease of flow
2. Spreadability
3. The powder should adhere to the skin and possess good covering.
4. The dusting powder should protect the skin from drying and irritation.
5. Dusting powder should not have any irritant effect.
Types:
Dusting powders are of two types
1. MEDICAL
2. SURGICAL
• Medical dusting powders are used mainly for superficial skin conditions whereas
surgical dusting powders are used in body cavities and also on major wounds as a
result of burns.
• Surgical dusting powders must be sterile (free from bacteria or other living
microorganisms) before their use.
Formulation:
It is generally prepared by mixing two or more ingredients one of which must be
either starch, kaolin or talc. Talc and kaolin are most commonly used because these
are chemically inert.
Use:
Dusting powders are mainly used for antiseptic (preventing the growth of
disease-causing microorganisms.), astringent (a mild protein precipitant suitable for
topical application to shrink tissues), adsorbent (Substance that binds to the drug
surface), antiperspirant (a substance that is applied to the skin, especially under the
arms, to prevent or reduce perspiration.) and antipruritic (used to relieve
itching.)Action.
Insufflations
• Insufflations are meant for powders being blown in various body cavities, like nose,
throat, ears etc.
• They are generally applied with the help of insufflators. It sprays the powder into a
stream of finely divided particles all over the site of application.
Desired Quality
1. It should be finely divided powder.
2. They should be absolutely free from irritation and sensitizing quality.
Disadvantages:
1. It is difficult to obtain a measured quantity of the drug as a uniform dose
2. Particles adhere to each other and to the wall of the insufflators due to the
electrostatic force.
Use:
Used for local effects, as in the treatment of ear, nose and throat infections with
antibiotics (a
medicine such as penicillin or its derivatives that inhibits the growth of or destroys
microorganisms.).
Snuffs
These are finely divided solid dosage forms of medicament which are inhaled into
nostrils for its antiseptic, bronchodilator and decongestion action.
Dentifrices
Dentifrices or tooth powders are hygienic products of everyday use. They may also
be medicated in order to exercise some definite action on individual person. These
are applied with the help of tooth brush for cleaning the surface of the teeth.
Formulation:
They contain abrasive agents such as calcium sulphate, magnesium carbonate,
sodium carbonate and sodium chloride. It may also contain some detergent and
suitable flavor. Detergent action is given by incorporating surfactants. Flavour and
taste qualities are very significant in the formulation of dentifrices.
Granules
The primary powder particles are made to adhere to form larger, multiparticle entities
called granules and the process is known as granulation. The bitter, nauseous and
unpleasant powders cannot be given in tablet form or in a capsule because a large
number of them are required to be taken as a single dose. They also cannot be
given as liquid form because of stability problem. Such medicaments are given in the
form of granules. The drug is mixed with sugar, flavouring agent and a granulating
agent to prepare a coherent mass, which is passed through a sieve to convert it into
granules and then dried. These dried granules are supplied in single dose sachets
which are dissolved in water before taking. Eg: Granules of antibiotics, such as
erythromycin, and penicillin salts.
Effervescent granules
The effervescent granules are the specially prepared solid dosage form of
medicaments, meant for internal use. They contain a medicament mixed with citric
acid, tartaric acid and sodium bicarbonate. Sometimes saccharin or sucrose may be
added as a sweetening agent. Before administration, the desired quantity is
dissolved in water, the acid and bicarbonate reacts together and produce
effervescence. The carbonated water produced from the release of carbondioxide
serves to mask the bitter taste of drugs. Moreover carbon dioxide stimulates the flow
of gastric juice and helps in the absorption of medicaments.
3NaHCO3 + C6H8O7.H2O = C6H5Na3O7 + 3CO2 + 3H2O
Sodium Bicarbonate + Citric Acid = Sodium Citrate
Tablet
A tablet is a hard, compressed medication in round, oval or square shape. Solid
dosage form containing unit dose of one or more medicament. Prepared by mould
method or compression method.
The excipients include:
-Binders, glidants (flow aids) and lubricants to ensure efficient tabletting.
-Disintegrants to ensure that the tablet breaks up in the digestive tract.
-Sweeteners or flavours to mask the taste of bad-tasting active ingredients.
-Pigments to make uncoated tablets visually attractive.
A coating may be applied to:
1- hide the taste of the tablet's components.
2- make the tablet smoother and easier to swallow .
3- make it more resistant to the environment.
4- extending its shelf life.
Types of tablets:
Compressed Tablets
● Dispersible tablets
● Chewable tablets
● Film coated tablets
● Enteric coated tablets
● Effervescent tablets
● Immediate release tablets
● Sustained release tablets
Molded tablets
● Hypodermic tablets
● Dispensing tablets
Special Tablets
● Sub-lingual tablets
● Buccal tablets
● Vaginal tablets
● Rectal tablets
BUCCAL AND SUBLINGUAL TABLET
Sublingual and buccal medications are administered by placing them in the mouth,
either under the tongue (sublingual) or between the gum and the cheek (buccal). The
medications dissolve rapidly and are absorbed through the mucous membranes of
the mouth, where they enter into the bloodstream. Avoid the acid and enzymatic
environment of the stomach and the drug metabolizing enzymes of the liver.
Examples of drugs administered by this route: e.g. vasodilators, steroidal hormones.
EFFERVESCENT TABLET
Effervescent tablets are uncoated tablets that generally contain acid substances
(citric and tartaric acids) and carbonates or bicarbonates and which react rapidly in
the presence of water by releasing carbon dioxide.They are intended to be dissolved
or dispersed in water before use providing:
A- Very rapid tablet dispersion and dissolution. B- pleasant tasting carbonated drink.
CHEWABLE TABLET
They are tablets that chewed prior to swallowing.They are designed for
administration to children e.g. vitamin products.
HYPODERMIC TABLETS
Molded tablets made from completely and readily water-soluble ingredients; formerly
intended for use in making preparations for hypodermic injection. They may be
administered orally or sublingually when rapid drug substance availability is required.
MODIFIED-RELEASE TABLETS
Two categories of modified-release tablet formulations are recognized by USP.
Delayed-release tablets: Tablets are sometimes formulated with acid-resistant or
enteric (also called “gastro-resistant”) coatings to protect acid-labile drug substances
from the gastric environment or to prevent adverse events such as irritation.
Extended-release tablets: Extended-release tablets are formulated in such a
manner as to make the drug substance available over an extended period of time
following ingestion. Requirements for dissolution are typically specified in the
individual monographs.
ORALLY DISINTEGRATING TABLETS
Orally disintegrating tablets are intended to disintegrate rapidly within the mouth to
provide a dispersion before the patient swallows the resulting slurry where the drug
substance is intended for gastrointestinal delivery and/or absorption. Some of these
dosage forms have been formulated to facilitate rapid disintegration and are
manufactured by conventional means or by using lyophilization or molding
processes. Further details may be found in the CDER Guidance for Industry: Orally
Disintegrating Tablets.
SUBLINGUAL TABLETS
Sublingual tablets are intended to be inserted beneath the tongue, where the drug
substance is absorbed directly through the oral mucosa. As with buccal tablets, few
drug substances are extensively absorbed in this way, and much of the drug
substance is swallowed and is available for gastrointestinal absorption.
TABLETS FOR ORAL SOLUTION
Before administration, tablets for oral solution are intended to be solubilized in a
liquid diluent. In some cases, tablets for oral solution also may be chewed or
swallowed.
TABLETS FOR ORAL SUSPENSION
Tablets for oral suspension are intended to be dispersed in a liquid before
administration as a suspension. The dosage form is tablets for oral suspension when
either the drug substance or the excipients do not dissolve when dispersed in a
liquid. In some cases, tablets for oral suspension also may be chewed or swallowed.
TABLET TRITURATES
Small, usually cylindrical, molded or compacted tablets. Tablet triturates traditionally
were used as dispensing tablets in order to provide a convenient, measured quantity
of a potent drug substance for compounding purposes, but they are rarely used
today.
Bolus Tablet
Large, usually elongated, tablets intended for administration to large animals.
Conventional tableting processes can be used to manufacture bolus tablets, but due
to their size higher compression forces may be necessary.
Dispersible Tablets
Tablets that disintegrates within few seconds in liquid making homogenous mixture
before administration to patient. e.g: Zinc DT 10
Capsules
Capsules are solid dosage forms in which the drug substance and/or excipients are
enclosed within a soluble container or shell or coated on the capsule shell. The
shells may be composed of two pieces (a body and a cap), or they may be
composed of a single piece. Two-piece capsules are commonly referred to as
hard-shell capsules, and one-piece capsules are often referred to as soft-shell
capsules. This two-piece and one-piece capsule distinction, although imprecise,
reflects differing levels of plasticizers in the two compositions and the fact that
one-piece capsules typically are more pliable than two-piece capsules.The shells of
capsules are usually made from gelatin. However, they also may be made from
cellulose polymers (e.g.,hypromellose)or other suitable material. Most capsules are
designed for oral administration. When no deliberate effort has been made to modify
the drug substance release rate, capsules are referred to as immediate-release.
TWO-PIECE OR HARD-SHELL CAPSULES
Two-piece capsules consist of two telescoping cap and body pieces in a range of
standard sizes.
ONE-PIECE OR SOFT-SHELL CAPSULES
One-piece capsules typically are used to deliver a drug substance as a solution or
suspension. Liquid formulations placed into one-piece capsules may offer
advantages by comparison with dry-filled capsules and tablets in achieving content
uniformity of potent drug substance(s) or acceptable dissolution of drug substance(s)
with poor aqueous solubility. Because the contact between the shell wall and its
liquid contents is more intimate than in dry-filled capsules, undesired interactions
may be more likely to occur (including gelatin cross-linking and pellicle formation).
MODIFIED-RELEASE CAPSULES
The release of drug substance(s) from capsules can be modified in several ways.
Two categories of modified-release capsule formulations are recognized by USP.
Delayed-release capsules: Capsules are sometimes formulated to include
enteric-coated granules to protect acid-labile drug substances from the gastric
environment or to prevent adverse events such as irritation. Enteric-coated
multiparticulate capsule dosage forms may reduce variability in bioavailability
associated with gastric emptying times for larger particles (i.e., tablets) and may
minimize the likelihood of a therapeutic failure when coating defects occur during
manufacturing. Alternatively, a coating may be applied to the capsule shell to
achieve delayed release of the contents.
Extended-release capsules: Extended-release capsules are formulated in such a
manner as to make the contained drug substance available over an extended period
of time following ingestion. Requirements for dissolution are typically specified in the
individual monograph. Methods for modifying drug substance release from capsules
include coating the filled capsule shells or the contents, in the case of dry-filled
capsules.
PILLS
Pills are small rounded solid dosage forms containing medicament and are intended
to be administered orally. Pills are spherical in shape and sometimes coated with
varnish, silver leaf, and gold leaf to improve the finish, mask the unpleasant tastes
and increase stability. In olden days pills were preferred because of their spherical
shape which can be easily swallowed. But now a days it is not used because of the
following reasons:
1. Disintegration time of the pills is uncertain.
2. It is difficult to prepare pills of a uniform size.
3. It is difficult to prepare pills of uniform weight.
Cachets
Cachets are the solid unit dosage forms of medicaments in which drug is enclosed in
tasteless sheet made by pouring mixture of rice flour and water between two hot,
polished, revolving cylinders. Water is evaporated and sheet of water formed is
known is cachet.
TYPES
Wet sheet cachet: Sealed by moistening the edges with water.
Dry sheet cachet
Administration: A cachet should be immersed in water for few seconds and then
placed on the toungue and swallowed with draught of water.
ADVANTAGE
* They are quite useful for administering the drugs with unpleasant taste
* A large dose can be enclosed in cachet than in a tablet or capsule.
Examples:
* Sodium amino salicylate cachet. * Isoniazid cachet.
Lozenges
Lozenges are solid oral dosage forms that are designed to dissolve or disintegrate
slowly in the mouth. They contain one or more drug substances that are slowly
liberated from the typically flavored and sweetened base. They are frequently
intended to provide local action in the oral cavity or the throat but also include those
intended for systemic absorption after dissolution. The typical therapeutic categories
of drug substances delivered in lozenges are antiseptics, analgesics, decongestants,
antitussives, and antibiotics. Molded lozenges are called cough drops or pastilles but
these terms are not used in official article titles. Lozenges prepared by compression
or by stamping or cutting from a uniform bed of paste are sometimes known as
troches (a term not used in official article titles). Compressed or stamped lozenges
are often produced in a circular shape. Lozenges can be made using sugars such as
sucrose and dextrose, or can provide the benefits of a sugar-free formulation that is
usually based on sorbitol or mannitol. Polyethylene glycols and hypromellose are
sometimes included to slow the rate of dissolution.
Suppositories
Suppository is another way to deliver drugs.It’s a small, round or cone shaped object
that put in body orifice, often into bottom. Once its inside, its melt and dissolves and
releases the medicine and exert local or systemic effects.
Type of suppository
There are three type of suppository
Rectal Suppository – into the rectum.
Vaginal Suppository – into the vagina.
Urethral Suppository – into male urethra.
ADVANTAGES OF SUPPOSITORIES
Over Oral Drug Administration:
• Avoid first pass metabolism
• Introduce drugs into the body
• Does not cause nausea and vomiting due to gastric irritation in case of oral therapy
• Used before surgery since oral therapy is restricted
• Beneficial for patients suffering from severe vomiting
• Can be administered to unconscious patients
• Can be used as targeted drug delivery system
• Localized action with reduced systemic distribution
• Get to site of action with lower dose reducing systemic toxicity
• Highly beneficial in haemorrhoids or vaginal infections
• Prolonged drug action achieved
Over parenteral drug administration:
• Self-medication
• No systemic side effects
• No pain or site of action related issues
Over Vaginal Tablets:
• Suppositories dissolves faster
• Total bioavailability achieved
• No residue remains like tablet
• No need of applicator
• Non staining
• Non itching
DISADVANTAGES OF SUPPOSITORIES:
• Mucosal irritation
• Patient compliance
• Erratic and undesired absorption
• Placement too high into rectum may lead to first pass metabolism
• Installation may trigger defecation reaction
• GI state affects absorption, Diarrhoea & disease states affect absorption
Poultices
Solid dosage form converted to paste like preparation used externally in the skin to
reduce inflammation. A Poultice is a soft, moist mass that is spread on a cloth and
than applied on the skin to treat various ailments. Ailments such as insect bites ,
arthritis , boils, infections and more ...... It is also called CATAPLASM.
FORMATION OF POULTICES
A homemade poultice is made by mashing herbs, plant material, or another
substance with warm or natural oils to make a paste. The paste is applied directly on
skin and covered with a piece of clean cloth.
TYPES OF POUTICES
• Some major types of poultices are:
• Onion poultice
• Potato poultice
• Mustard poultice
• Plantain poultice
• Comfrey poultice
• Tumeric poultice
USES
• POULTICES are used to cure arthritis.
• POULTICES are used to cure inflamation.
• To relief itching.
• To relief muscle pain muscle spasm
• For desalination
• In horses to treat joints pain.
Liquid dosage forms
The liquid dosage forms, whether for internal, parenteral or external use may be
either monophasic or biphasic products. Monophasic products are represented by
true or colloidal solutions and solubilised preparations. They are appeared to be
similar in physical appearance and consists of only one phase. They may have water
as the solvent or may be occasionally based on some other liquids. The biphasic
products are exemplified by emulsions or suspensions and consists of two phases.
In emulsions generally both the phases are liquids, while in suspensions the
continuous phase is liquid and the dispersed phase is finely divided solids. Liquid
preparations are easy to swallow and thus more useful for pediatrics and geriatrics.
On the other hand drug in soluble state is chemically less stable than its insoluble
state.
Monophasic dosage forms are available as:
1. Liquid for internal use, Eg: Syrups, Elixirs, Linctus, drops and draughts.
2. Liquids for external use, which are of two types:
A. Liquid to be applied to the skin, eg: liniments and lotions.
B. Liquids for body cavities. Eg: Gargles, throat paints, mouth washes, eye drops,
eye lotions, ear drops, nasal drops, spray and inhalations.
Liquid for internal use:
The largest proportion of the liquid formulations are liquid for internal use. Drug
should have sufficient solubility in commonly used solvent, like water.
Liquid Formulations for External Use:
Monophasic liquids for external use may be categorised into following classes
a. Liquids for application to the intact skin, such as liniments, lotions etc
b. Liquids for the use in one or the other body cavities such as gargles, throat paints,
eye drops, eye lotions, ear drops, ear douches, nasal drops, enemas etc.
c. Liquids meant to be inhaled into or sprayed in nasal or respiratory tracts.
Biphasic Liquid Dosage form:
Liquids which consist of two phases are known biphasic liquids. Eg: Emulsions and
suspensions.
Collodions
Liquid preparations for external use having nitro cellulose used to protect the skin.
Collodion is a solution of nitrocellulose in ether or acetone, sometimes with the
addition of alcohols. Its generic name is pyroxylin solution. It is highly flammable. As
the solvent evaporates, it dries to a celluloid-like film. Compound Wart Remover
consists of acetic acid and salicylic acid in an acetone collodion base used in
Treatment of warts by keratolysis.
Droughts
Liquid preparations for oral containing medicaments available in single ose or
multiple dose. A draught is an older term used to describe a liquid preparation
formulated as a single dose, in a volume which is larger than generally utilised
intraditional mixturebformulations. Each draught was usually supplied in a 50mL unit
dose container. Example: Ipecacuanha emetic draughts-BPC(treatment of poison).
The normal is 10 or 15ml and therefore multiple dose volume is prescribed. Malefern
draught emulsion. Paraldehyde draughts- oxidized to acetic acid and cause death
Precautions: Do not use, if the solution is discolored.
Elixirs
Liquid preparation for oral containing medicaments with suitable excipients. Elixirs
are clear sweetened and flavoured hydroalcoholic solutions for oral use. Non
medicated elixiers such as aromatic elixir are mainly used as flavoured vehicle.
Medicated elixiers have their own therapeutic value. Alcohol content in elixiers varies
from 3 to 40%. Due to high alcohol content, elixirs are not the
choice of dosage forms for pediatrics. The main ingredients of elixirs are ethyl
alcohol, water, glycerin, propylene glycol, flavouring agent, colouring agent and
some preservative. The medicated elixirs usually contain a potent drug such as,
antibiotics, antihistamines or sedatives. Eg: Piperazine Citrate Elixirs I.P (Piperazine
Citrate)
Emulsions
Biphasic liquid dosage form for oral containing medicaments in which fine oil
globules dispersed in continuous phase. Emulsions are thermodynamically unstable
heterogeneous biphasic system consisting of two immiscible liquids, one of which is
dispersed as minute globules into the others. This type of formulations are stabilized
by using emulsifying agent. Internal phase droplets are generally ranged in diameter
of 0.1 µm to 100 µm. Emulsions are mostly classified as oil in water (o/w) emulsions
and water in oil (w/o) emulsions.
Emulsions are used for
1. Oral administration, Eg: Liquid Paraffin Emulsion IP
2. Intravenous administration, Eg: Emulsion of vitamin A,D and K and
3. For external use, Eg: Emulsions for topical administration.
Oral emulsion
Oral emulsions are stabilized oil-in-water dispersions, either or both phases of which
may contain dissolved solids either oil is dispersed in finely divided form in water or
vice versa
Suspensions
Biphasic liquid dosage form for oral containing medicaments in which fine solid
particles suspended in continuous phase.Suspensions are heterogeneous biphasic,
thermodynamically unstable liquid dosage form of medicaments in which insoluble
solid particles (as internal, discontinuous or dispersed phase) is uniformly distributed
in liquid phase (External, continuous or dispersion phase). In suspensions finely
divided particles ranging from 0.5 to 5 microns are dispersed in a liquid vehicle.
Suspensions are used for oral, parenteral and external applications. Suspensions
which are meant for external applications should have small particle size to avoid
gritty feeling to the skin and to cover a larger area of the skin. Smaller particles also
helps in the penetration of drug through the skin.
Oral suspension
Liquid preparations for oral use containing one or more active ingredients suspended
in a suitable vehicle. may show a sediment which is readily dispersed on shaking to
give a uniform suspension which remains sufficiently stable to enable the correct
dose to be delivered
Enemas
Liquid preparation for rectal containing medicaments. An enema is the procedure of
introducing liquids into the rectum and colon via the anus.
Types of enema:
1- Evacuant enema: used as a bowel stimulant to treat constipation. E.g. soft
soap enema & Mgso4 enema
-The volume of evacuant enemas may reach up to 2 liters.
- They should be warmed to body temperature before administration.
2- Retention enema:
- Their volume does not exceed 100 ml.
- No warming needed.
- May exert:
A- Local effect: e.g. a barium enema is used as a contrast substance in the
radiological imaging of the bowel.
B- Systemic effect: e.g. the administration of substances into the bloodstream. This
may be done in situations where it is impossible to deliver a medication
by mouth, such as antiemetics. e.g. nutrient enema which contains carbohydrates,
vitamins &minerals.
Gargles
Concentrated aqueous solutions for external use used to treat throat infections.
Gargles are clear aqueous solutions used in the posterior region of mouth by
agitating the solution with exhaled air to produce local effect in throat and these are
not to be swallowed in large amount. They are usually available in concentrated form
with direction for dilution with warm water before use. They are brought into intimate
contact with the mucous membrane of the throat and are allowed to remain in
contact with it for a few seconds before they are thrown out of the mouth. They are
used to relieve soreness in mild throat infection. Phenol or thymol is generally
present in small concentration for its antibacterial activity. Potassium chlorate is also
included in gargles for its weak astringent effect to tone up a relaxed throat. It also
stimulates secretion of saliva which relieves dryness, eg: Phenol gargles, Potassium
chloride and phenol gargles.
Gels
Aqueous colloidal suspensions containing medicaments used as antacids. Gels and
jellies are transparent to opaque semisolid preparations meant for external
application to the skin or mucous membrane. Considered to be more rigid than
jellies. Jellies contain more fluid and less cross-linking agent. They are non-greasy
and prepared from Natural gums, eg: Tragacanth, Pectin, Sodium Alginate etc.
Synthetic derivatives of natural substances, eg: Methyl cellulose, Sodium
carboxymethyl cellulose.
Linctuses
Viscous, liquid oral preparations used to relief cough. Linctuses are viscous liquid
and oral preparations that are generally prescribed for the relief of cough. Mostly it
contains ingredient with sedative action and some contains expectorants. Simple
syrup is generally used as a vehicle for most of the linctuses. This give soothing to
the sore mucous membrane of the throat. To obtain and prolong local action,
linctuses should be taken undiluted and sipped and swallowed slowly. Eg: Codeine
Linctus B.P.C (API: Codeine Phosphate)
Lotions
Liquid preparations for external application usually applied without friction. Lotions
are suspensions, emulsions, combination of emulsion-suspension or aqueous or
non-aqueous solutions designed to be applied to the unbroken skin without friction.
Lotions are an emulsified liquid dosage form intended for external application to the
skin. Historically, some topical suspensions such as calamine lotion have been
called lotions but that nomenclature is not currently preferred. Lotions share many
characteristics with creams. The distinguishing factor is that they are more fluid than
semisolid and thus pourable. Duento their fluid character, lotions are more easily
applied to large skin surfaces than semisolid preparations. Lotions may contain
antimicrobial agents as preservatives. They are used for their epidermic effect, such
as local cooling, soothing, protective, drying or moisturizing properties depending
upon the ingredients used. They are directly applied to the skin with the help of
some adsorbent material, such as, cotton wool. Eg: Calamine Lotion I.P
Liniments
Liquid preparations for external application usually applied with friction. The liniments
are liquid or semi-liquid preparations meant for application to the skin. The liniments
are usually applied to the skin with friction and rubbing of the skin. They are solutions
or emulsions in an aqueous or oily vehicles. They are used as counter irritant,
rubefacient and soothing. Alcohols are also used in the preparation of liniments.
Alcohol in the liniments helps in the penetration of medicaments into the skin and
also increases its counter irritant and rubefacient action. In oily liniments arachis oil
is used commonly, which spread more easily on the skin. A liniment should not be
applied to the broken skin because it may causes excessive irritation. Eg: Liniment of
Camphor.
Mixtures
Liquid oral preparations containing one or more
medicaments. A mixture is a liquidpreparation meant for oral administration in which
medicament or medicaments are dissolved, suspended or dispersed in a suitable
vehicle.
CLASSIFICATION OF MIXTURES
1. Simple mixture containing soluble substances
2. Mixture containing diffusible solids
3. Mixture containing indiffusible solids
4. Mixture containing Precipitate forming liquids
5. Mixture containing Slightly soluble liquid
SIMPLE MIXTURE CONTAINING SOLUBLE SUBSTANCES
It contains only soluble ingredients.It is represented by true solution.It is a clear
homogenous mixture. E.g. Carminative mixture, Expectorant mixture etc.
MIXTURE CONTAINING DIFFUSIBLE SOLIDS
Diffusible solids are insoluble in water. Uniformly dispersed in the vehicle on shaking.
No need of suspending agent. Ex. Bismuth carbonate, Bismuth
subnitrate,Magnesium carbonate.
MIXTURE CONTAINING INDIFFUSIBLE SOLIDS
Indiffusible solids are insoluble in vehicle. Not evenly distribute throughout the
vehicle on shaking or not distribute in vehicle for sufficiently long time. So
suspending agents are added in formulation.. Ex. Acetyl salicylic acid, Phenacetin,
chalk powder.
MIXTURE CONTAINING PRECIPITATE FORMING LIQUIDS
These liquids are not only insoluble in water but they form indiffusible precipitates
particularly when salts are present.They contain resinous matter and when it is
mixed with water it leads to precipitation of resin and may stick to the sides of the
bottle which will be difficult to rediffuse by shaking. To prevent this, a protective
colloid is dispersed in the vehicle before tincture is added.
MIXTURE CONTAINING SLIGHTLY SOLUBLE LIQUIDS
The insoluble portion of slightly soluble liquids is not readily diffusible.So a
suspending agent such as tragacanth powder or tragacanth mucilage are needed to
dispense such mixtures. Ex. Paraldehyde liquid
Mouth washes
Concentrated aqueous solutions for external use used to treat mouth infections and
oral hyginic. These are aqueous solutions with a pleasant taste and odour used to
make clean and deodorise the buccal cavity. Generally they contain antibacterial
agents, alcohol, glycerin, sweetening agents, flavouring agents and colouring
agents. Eg: Sodium Chloride Mouth Wash, Compound B.P.C.
Nasal drops
Liquid preparations containing medicaments that are instilled in to the nose with a
dropper used to treat nose infections and blockage of nose. Drugs in solution may be
instilled into the nose from a dropper or from a plastic squeeze bottle. The drug may
have a local effect, e.g. antihistamine, decongestant. Alternatively the drug may be
absorbed through the nasal mucosa to exert a systemic effect.The use of oily nasal
drops should be avoided because of possible damage to the cilia of the nasal
mucosa.
Paints
Liquid preparations for external application to the skin or mucous membrane with
soft brush. Paints are liquids for application to the skin or mucous membranes.Skin
paints contain volatile solvent that evaporates quickly to leave a dry resinous film of
medicament. Throat paints are more viscous due to a high content of glycerol,
designed to prolong contact of the medicament with the affected site.
Throat Paints
Throat paints are viscous preparations of medicaments for local action in the
pharynx. Glycerin is commonly used as a base because, being viscous, it adheres to
mucous membrane for a long period and it possesses sweet taste. They are applied
to the throat with a brush. Throat paints are used in treatment of inflammations of
various areas of the mouth and throat.
Solutions
Clear liquid preparation containing with or without medicaments used to internal or
external preparations. A solution is a preparation that contains one or more dissolved
chemical substances in a suitable solvent or mixture of mutually miscible solvents.
Because molecules of a drug substance in solution are uniformly dispersed, the use
of solutions as dosagebforms generally provides assurance of uniform dosage upon
administration and good accuracy when the solution is diluted or otherwise mixed.
Substances in solutions are more susceptible to chemical instability than they are in
the solid state and, dose-for-dose, arengenerally heavier and more bulky than solid
dosage forms. These factors increase the cost of packaging and shipping relative to
that of solid dosage forms. Some solutions are prepared and ready for use, and
others are prepared as powders or other solids intended for reconstitution with an
appropriate vehicle just before use . Solution dosage forms can be administered by
injection, inhalation, and the mucosal, topical, and gastrointestinal routes. A solution
administered by injection is officially titled “injection”. Some solutions are designed to
form a mass in situ. These solutions comprise polymer, drug substance, and solvent
for the polymer. The polymer solvent can be water or an organic solvent. After
administration of the solution to a patient by subcutaneous or intramuscular
administration, it forms a gel or a solid polymeric matrix that traps the drug
substance andbextends the drug substance release for days or months. Solutions
intended for oral administration usually contain flavorings and colorants to make the
medication more attractive and palatable for the patient or consumer. When needed,
they also may contain stabilizers to maintain chemical and physical stability and
preservatives to prevent microbial growth. Solutions are sometimes placed on
devices such as swabs, cloths, or sponges, that aid application. A solution that
needs to be diluted prior to administration previously has been called aconcentrate.
The term “concentrate” is no longer preferred.
Oral solution
Oral solutions are clear Liquid preparations for oral use containing one or more
active ingredients dissolved in a suitable vehicle.
Syrups
Sweet, viscous, concentrated liquid preparations containing with or without sugar
and medicaments. Syrups are sweet and viscous aqueous preparations. Simple
syrup is a saturated solution of sucrose in purified water. The concentration of
sucrose used is 66.7 % w/w (as per Indian Pharmacopoeia, IP). They are either
flavoring syrups (syrups containing aromatic or flavored substances) and medicated
syrups (Syrup containing medicinal substances). Syrups are used for formulating
antibiotics, antitussives, antihistaminic, sedatives, vitamins etc. Most syrups are
aqueous solutions of sucrose or dextrose. Artificial syrups are also in the
market, where artificial sweetening agents (Eg: saccharine and sodium cyclamate)
are used.
The artificial syrups are having two points in their favour
1. They are free from carbohydrates and suitable for diabetics.
2. They have lesser stability problems as compared to sugar based syrups.
Syrups are commonly used for the following reasons:
1. They are palatable
2. Syrups have high osmotic pressure which prevents growth of bacteria, fungi and
prevent decomposition of many vegetable substances. Due to this syrups have the
self-preservative activity.
3. Syrups retards oxidation because it is partly hydrolysed into reducing sugars, such
as lavulose and dextrose.
Semisolid dosage forms
Semisolid dosage forms are dermatological products of semisolid consistency and
applied to skin for therapeutic or protective action or cosmetic function. Semisolid
dosage forms usually are intended for localized drug delivery. In the past few years,
however, these forms also have been explored for the systemic delivery of various
drugs. Semisolids constitute a significant proportion of pharmaceutical dosage forms.
They can be applied topically to the skin, cornea, rectal tissue, nasal mucosa,
vagina, buccal tissue,urethral membrane, and external ear lining. Eg: Ointments,
creams, jellies and pastes etc.
Advantages of semi-solid dosage form:
• It is used externally
• The probability of side effects can be reduced
• First, pass gut and hepatic metabolism is avoided.
• Local action and Site-specific action of the drug on the affected area.
• Convenient for unconscious patients or patients to have difficulty in oral
administration.
• Suitable dosage form for bitter drugs.
• More stable than a liquid dosage form.
Disadvantages of semi-solid dosage form:
• The accuracy can’t be measured, for the semisolid dosage form.
• May cause staining.
• They are bulky to handle.
• Application with a finger may cause contamination.
• Physico-chemical is less stable than a solid dosage form.
• May cause irritation or allergy to some patients
Ideal properties of semisolid dosage forms:
• Smooth texture
• Elegant in appearance
• Non-dehydrating
• Non-gritty
• Non-greasy and non-staining
• Non-hygroscopic
Ingredients needed for semisolid dosage form:
• Bases
• Preservative
• Humectants
• Antioxidants
• Emulsifier
• Gelling agent
• Permeation enhancer
• Buffers
Bases used in semisolid dosage form:
It is one of the most important ingredients used in the formulation of the semisolid
dosage form. Ointment bases do not merely act as the carriers of the medicaments,
but they also control the extent of absorption of medicaments incorporated in them.
Ideal characterization of bases used in semisolid dosage form:
They should be:
• Inert, non-irritating, and non-sensitizing.
• Compatible with skin pH and the drug.
• Good solvent and/or emulsifying agent.
• Emollient, protective, non-greasy and easily removable.
• Release medicament readily at the site of application.
• Pharmaceutically elegant and possess good stability
Classification of Bases:
According to USP ointment bases are classified into four general groups:
• Hydrocarbon bases (oleaginous bases) (Petrolatum, Paraffin, Lanolin, etc.)
• Absorption bases (cold cream, anhydrous lanolin, etc.)
• Water-removable bases ( oil in water)
• Water-soluble bases (polyethylene glycol)
Antioxidants used in semisolid dosage form:
Oxygen has the capability to become a part of potentially damaging molecules called
“free radicals.” Free radicals can attack the healthy cells of the body. It can break
their structure and that’s why the function is also affected. Example: Butylated
hydroxyanisole, Butylated hydroxytoluene
Ingredients that increase permeation:
Skin can act as a barrier. There are various penetration enhancers that can help the
drug to penetrate through the skin.
The emulsifier used in semisolid dosage form: Emulsifiers are used to improve
the stability of an emulsion by increasing its kinetic stability. It reduces surface
tension and prevents coalescence. It helps to increase the viscosity at low
concentration.
Emulsifying agents used in semisolid dosage form:
Sodium lauryl sulfate: Oil/Water emulsion – Sodium stearate and calcium stearate.
Glyceryl monostearate: This is a weak Water/Oil emulsifying agent and it is used as
a stabilizer and emollient in the Oil/Water emulsion.
Humectant used in semisolid dosage form:
The humectant is a hygroscopic substance used to increase the solubility of the
active ingredient to increase skin penetration. It’s also used to improve the hydration
of the skin.
Buffers used in semisolid dosage form:
Buffers are added for various purposes. Such as
• Compatibility with skin.
• Drug solubility.
• Drug stability.
• Influence the ionization of drugs.
Preservatives used in semisolid dosage form:
Preservatives are used to inhibit the growth of contamination of microorganisms.
Example: Para-hydroxybenzoate (parabens), phenols, benzoic acid, sorbic acid, etc.
Ointments
Semisolid dosage forms for external use containing with or without medicaments
with suitable ointment base. Ointments are semisolid preparations with or without
medicaments intended for application to the skin. Medicaments used in the
formulation is dissolved, suspended or emulsified in an ointment base. Ointment
bases recognized for use as vehicles fall into four general classes: hydrocarbon
bases, absorption bases, water-removable bases, and water-soluble bases.
HYDROCARBON BASE
• The ointments are mainly used as protective or emollient for the skin.
• Ointments may be used as-
1. Antibiotic ointments. Drug used: Neomycin.
2. Antifungal ointment. Drug used: Benzoic acid, salicylic acid, nystatin.
3. Anti-inflammatory ointment. Drug used: hydrocortisone, etc
ENVIRONMENT Temperature: 20-300 C, Humidity: 30-60 %,
DOCUMENTS:
1. Standard Operating Procedure (SOP)
2. Batch Manufacturing Record (BMR)
3. Batch Packaging Record (BPR)
4. In House specification
Creams
Semisolid dosage forms for external use containing with or without medicaments
with suitable fatty base. These are viscous semisolid emulsions which are meant for
external use. They usually contain a water soluble base due to which they can be
easily removed from the skin.They are of softer consistency and have light weight in
comparison to true ointments when applied to the skin. Cream leave no visible
evidence of their presence on the skin.
They are of mostly two types
a. Aqueous cream, Eg: Cetrimide Cream B.P
b. Oily cream, Eg: Proflavine cream BPC
Creams are semi-solid emulsions, that is mixtures of oil and water. - They are
divided into two types:
A- oil-in-water (O/W) creams: which are composed of small droplets of oil
dispersed in a continuous aqueous phase. Oil-in-water creams are more comfortable
and cosmetically acceptable as they are less greasy and more easily washed off
using water.
B- water-in-oil (W/O) creams: which are composed of small droplets of water
dispersed in a continuous oily phase. Water-in-oil creams are more difficult to handle
but many drugs which are incorporated into creams are hydrophobic and will be
released more readily from a water-in-oil cream than an oil-in-water cream.
Water-in-oil creams are also more moisturising as they provide an oily barrier which
reduces water loss from the stratum corneum, the outermost layer of the skin.
Paste
Semisolid dosage forms for external use containing high proportion of finely
powdered medicaments with suitable fatty base. Pastes are basically ointments into
which a high percentage of insoluble solid has been added.The extraordinary
amount of particulate matter stiffens the system. Pastes are less penetrating and
less macerating and less heating than ointment. Pastes make particularly good
protective barrier when placed on the skin, the solid they contain can absorb and
thereby neutralize certain noxious chemicals before they ever reach the skin. Like
ointments, paste forms an unbroken relatively water – impermeable film unlike
ointments the film is opaque and therefore can be used as an effective sun block
accordingly.
There are two types of paste:
a) Fatty pastes (e.g: leaser's paste) .
b) Non greasy pastes (e g: - bassorin paste).
Fatty pastes that have a high proportion of hydrophilic solids appear less greasy and
are more absorptive than ointments.They are used to absorb serous secretions and
are often preferred for acute lesions that have a tendency toward crusting,
vesiculation, or oozing. Dental pastes are applied to the teeth. Other orally
administered pastes may be indicated for adhesion to the mucous membrane for a
local effect. Although rare, pastes can be administered orally, for example to
evaluate pharyngeal function. In veterinary medicine, pastes are typically
administered orally and are intended for systemic delivery of drug substances. The
paste is squeezed into the mouth of the animal, generally at the back of the tongue,
or is spread inside the mouth.
Gels
Transparent semisolid dosage forms for external use containing hydrophilic or
hydrophobic base with gelling agents
Poultices
Semisolid dosage forms for external use containing medicaments applied to the skin
to hold the dressing and protective.
Gaseous dosage forms
Aerosols
Suspension of fine solid or liquid particles with gas used to apply drug to respiratory
tract having atomizer with in device. Aerosols are dosage forms packaged under
pressure and contain therapeutic agent(s) and propellant(s) that are released upon
actuation of an appropriate valve system. Upon actuation of the valve system, the
drug substance is released as a plume of fine particles or droplets. Only 1 dose is
released from the preparation upon actuation of a metered valve. In the case of
topical products and depending on the nature of the drug substance and the
conditions being treated, actuation of the valve may result in a metered release of a
controlled amount of the formulation or the continuous release of the formulation as
long as the valve is depressed. The aerosol dosage form refers only to those
products packaged under pressure that release a fine mist of particles or droplets
when actuated . Other products that produce dispersions of fine droplets or particles
will be covered in subsequent sections (e.g., Sprays and Powders).
TYPES OF AEROSOL DOSAGE FORMS
Aerosol dosage forms can be delivered via various routes. The container, actuator,
and metering valve, as well as the formulation, are designed to target the site of
administration. Inhalation aerosols, commonly known as metered-dose inhalers
(MDIs), are intended to produce fine particles or droplets for inhalation through the
mouth and deposition in the pulmonary tree. The design of the delivery system is
intended to release measured mass and appropriate quality of the active substance
with each actuation.
Nasal aerosols, commonly known as nasal MDIs, produce fine particles or droplets
for delivery through the nasal vestibule and deposition in the nasal cavity. Each
actuation of the valve releases a measured mass of the drug substance with
appropriate quality characteristics.
Lingual aerosols are intended to produce fine particles or droplets for deposition on
the surface of the tongue. The design of the delivery system releases 1 dose with
each actuation.
Topical aerosols produce fine particles or droplets for application to the skin.
Inhalations
Internal liquid preparations containing medicaments dissolved in suitable solvent or if
insoluble suspended in the propellent.
Inhaler
They are solutions, suspensions or emulsion of drugs in a mixture of inert propellants
held under pressure in an aerosol dispenser. Release of a dose of the medicament
in the form of droplets of 50 um diameter or less from the container through a
springloaded valve incorporating a metering device. The patient then inhales the
released drug through a mouthpiece. In some types. the valve is actuated by finger
pressure, in other types the valve is actuated by the patient breathing in through the
mouthpiece. It is commonly used to treat asthma and other respiratory problems.
Nebulizer or (atomizer)
A nebulizer is a device used to administer medication to people in forms of a liquid
mist to the airways. It is commonly used in treating asthma, and other respiratory
diseases. - It pumps air or oxygen through a liquid medicine to turn it into a vapor,
which is then inhaled by the patient.
As a general rule, doctors generally prefer to prescribe inhalers for their
patients, because:
1-These are cheaper
2- more portable
3- carry less risk of side effects. Nebulizers, for that reason, are usually reserved
only for serious cases of respiratory disease, or severe attacks.
Sprays
Gaseous preparations of drugs containing alcohol applied to mucous membrane of
nose or throat with atomizer or nebulizer. Spray preparations may deliver either
accurately metered or nonmetered amounts of formulation. A spray drug product is a
dosage form that contains a drug substance in the liquid state as a solution or
suspension and is intended for administration as a mist. Sprays are distinguished
from aerosols in that spray containers are not pressurized. Most of the sprays are
generated by manually squeezing a flexible container or actuation of a pump that
generates the mist by discharging the contents through a nozzle. Depending on the
design of the formulation and the valve system, the droplets generated may be
intended for immediate inhalation through the mouth and deposition in the pulmonary
tree, or for inhalation into the nose and deposition in the nasal cavity. The
mechanism for droplet generation and the intended use of the preparation
distinguish various types of spray drug products. A spray drug product may be
composed of a pump, container, actuator, valve, nozzle, or mouthpiece in addition to
the formulation containing the drug(s), solvent(s), and any excipient(s). The design of
each component plays a role for the appropriate performance of the drug product
and in determining the critical characteristics of the droplet size distribution. Droplet
and particle size distributions, delivered dose uniformity, plume geometry, and
droplet velocity are critical parameters that influence the efficiency of drug delivery.
When the preparation is supplied as a multidose container, the addition of a suitable
antimicrobial preservative may be necessary. Spray formulations intended for local
or systemic effect typically have an aqueous base and may contain excipients to
control pH and viscosity. In addition, depending on the route of administration, the
formulation may be isotonic.
Others Dosage Forms
Magmas
Two-phase system with large particle size or floccules of small distance particles.
These water insoluble particles. Thick and viscous. Commonly known as milk
magnesia .Magma is semi-solid dosage form. Route administration of magma: oral
Plasters
A plaster is a semisolid substance for external application that is supplied on a
support material. Plasters are applied for prolonged periods to provide protection,
support, or occlusion (maceration). This term is not preferred and should not be used
for new drug product titles. Plasters consist of an adhesive layer that may contain
active substances. This layer is spread uniformly on an appropriate support that is
usually made of a rubber base or synthetic resin. Unmedicated plasters are designed
to provide protection or mechanical support to the site of application. Plasters are
available in a range of sizes or cut to size to effectively provide prolonged contact to
the site of application. They adhere firmly to the skin but can be peeled off the skin
without causing injury.
Douches
Douches are aqueous solutions intended to clean, deodorise, soothe or medicate
body cavities. Eye douches, often termed as eyewashes, are used to remove foreign
particles and discharges from the eyes. Douches are generally dispensed in the form
of a powder or tablet with a specific directions for dissolving it in a specific quantity of
warm water. Vaginal douches must be sterile.
They are used for:
a. Cleansing agents: Isotonic sodium chloride solution
b. Antiseptics. Eg: Mercuric chloride (0.001%)
c. Astringent, Eg: Alum (1%
Tooth Paste
Toothpaste is a paste or gel dentifrice used with a toothbrush to clean and maintain
the aesthetics and health of teeth. Toothpaste is used to promote oral hygiene: it is
an abrasive that aids in removing dental plaque and food from the teeth, assists in
suppressing halitosis, and delivers active ingredients (most commonly fluoride) to
help prevent tooth decay (dental caries) and gum disease (gingivitis). Owing to
differences in composition and fluoride content, not all toothpastes are equally
effective in maintaining oral health. The decline of tooth decay during the 20th
century has been attributed to the introduction and regular use of fluoride-containing
toothpastes worldwide.Large amounts of swallowed toothpaste can be toxic.
Common colors for toothpaste include white (sometimes with colored stripes or
green tint) and blue.
Hand creams
They are a high – viscosity product specifically designed to be used on the hands, to
soften and moisturise dry and cracked hands. The high viscosity of the hand cream
means that they have a higher percentage of oil as compared to water. As a result,
hand creams don’t have the runny texture of lotions and are thicker. These are
recommended for people with dry skin as it helps in giving them extra coverage.
Hand creams are used most commonly in winter.
Hand Washings
liquid soap for washing one's hands. Handwash is formulated with a synthetic
surfactants, or foaming bases, like SLS (sodium lauryl sulfate), SDS (sodium dodecyl
sulfate), ALS (ammonium lauryl sulfate) or SLES (sodium lauryl ether sulfate). These
surfactants are derived from petroleum or made synthetically. Either way, they are
heavily processed. Synthetic surfactants are detergents that can be used as a base
for handwash, body wash, dishwashing detergent, laundry detergent and car
cleaning detergent.
Hair cream
Commonly termed as styling cream, adds natural shine to rough hair. It smoothens
the tamed hair and holds them well so that they don't fall. In simple words, it removes
frizz and fly-aways without making them heavy.a cosmetic preparation used to
improve the condition of, and/or to style the hair.
Hair dyes
A natural or synthetic substance used to change the colour of a person's hair. Hair
coloring, or hair dyeing, is the practice of changing the hair color. The main reasons
for this are cosmetic: to cover gray or white hair, to change to a color regarded as
more fashionable or desirable, or to restore the original hair color after it has been
discolored by hairdressing processes or sun bleaching. Hair coloring can be done
professionally by a hairdresser or independently at home. Today, hair coloring is very
popular, with 75% of women[1] and 18% of men living in Copenhagen having
reported using hair dye.
Hair lotion
It is a hair styling product that is generally applied to the hair and left on. Its purpose
is typically to moisturize the hair, although hair lotion can also be used to treat dry
scalp, eczema, dermatitis, and other skin conditions affecting the scalp. Medicated
hair lotions may also play a part in many hair-retention and hair-regeneration
programs marketed for those suffering from hair loss. While a wide range of hair
lotions and oils are available for sale, it is also fairly easy to make these products at
home. They often contain simple, readily-available ingredients such as eggs, sugar,
and vegetable oil.
Soaps and Shampoos
Soaps and shampoos are solid or liquid preparations intended for topical application
to the skin or scalp followed by subsequent rinsing with water. Soaps and shampoos
are emulsions, suspensions, or surface-active compositions that readily form
emulsions, micelles, or foams upon the addition of water followed by rubbing.
Incorporation of drug substances in soaps and shampoos combines the
cleansing/degreasing abilities of the vehicle and facilitates the topical application of
the drug substance to affected areas, even large areas, of the body. The
surface-active properties of the vehicle facilitate contact of the drug substance with
the skin or scalp. Medicated soap and shampoo formulations frequently contain
suitable antimicrobial agents to protect against bacteria, yeast, and mold
contamination.
Throat Paints
Throat paints are viscous preparations of medicaments for local action in the
pharynx. Glycerin is commonly used as a base because, being viscous, it adheres to
mucous membrane for a long period and it possesses sweet taste. They are applied
to the throat with a brush. Throat paints are used in treatment of inflammations of
various areas of the mouth and throat.
Eye drops
Eye drops are saline-containing drops used as a vehicle to administer medication in
the eye. Depending on the condition being treated, they may contain steroids,
antihistamines or topical anesthetics. Eye drops sometimes do not have medications
in them and are only lubricating and tear-replacing solutions. These are sterile
solutions or suspensions of drugs that are instilled into the eye with a dropper.The
eye drops are usually made in aqueous vehicle. It should be sterile, isotonic with
lachrymal secretions and free from foreign particles to avoid irritation to the eye. A
suitable preservative like phenyl mercuric nitrate (0.002%), Benzalkonium chloride
(0.01%) may be used to prevent bacterial or fungal growth. Eye drops usually
contain substances having antiseptic, anti-inflammatory, anesthetic and miotic
properties.
Ophthalmic ointment & gel
These are sterile semi-solid. Preparations intended for application. To the
conjunctiva or eyelid margin.
Ear Drops
Ear drops are solutions, suspensions or emulsions of drugs in water, glycerin or
propylene glycol intended for instillation into the ear. These are used for removal of
excessive cerumen, to treat infection, inflammation or pain and for cleaning and
drying of ear. Ear drops are solutions, suspensions or emulsions of drugs that are
instilled into the ear with a dropper. It is used to treat or prevent ear infections,
especially infections of the outer ear and ear canal.
Nasal Drops
These are aqueous solutions of drops that are instilled into the nose with a dropper.
Nasal drops should be isotonic with 0.9% sodium chloride having neutral pH and
viscosity similar to nasal secretions by using0.5% methyl cellulose. Drugs in solution
may be instilled into the nose from a dropper or from a plastic squeeze bottle. The
drug may have a local effect, e.g. antihistamine, decongestant. Alternatively the drug
may be absorbed through the nasal mucosa to exert a systemic effect.The use of
oily nasal drops should be avoided because of possible damage to the cilia of the
nasal mucosa.
EYE LOTIONS
Eye lotion are the sterile aqueous solutions used for washing of the eyes.The eye
lotions are supplied in concentrated form and are required to be diluted with warm
water immediately before use. They are usually applied with a clean eye-bath or
sterilized fabric dressing and a large volume of solutions is allowed to flow quickly
over the eye. o Eye lotions should be isotonic and free from foreign particles to avoid
irritation to the eye.They are required to be prepared fresh and should not be stored
for more than two days as the lotion may get contaminated.
Films
Films are thin sheets that are placed in the oral cavity. They contain one or more
layers. A layer may or may not contain the drug substance. Typically, these thin
sheets are formed by casting or extrusion that results in a dispersion of the
components through the film. Films are classified by the site of application. “Oral
films” can be formulated to deliver medication to the mouth such as oral hygiene
products or to deliver medication to the gastrointestinal tract for absorption. “Buccal
films” and “sublingual films” are formulated to facilitate absorption through the
proximal mucosal membranes avoiding first pass metabolism or degradation in the
gastrointestinal tract and providing a quick onset of action. Films can be formulated
with edible polymers such as pullulan or with water-soluble polymers such as
modified cellulose, edible gums, and copolymers. The dissolution rate of the film is
controlled to facilitate incorporation of the medication into saliva or for absorption by
the proximal mucosa. These films must be substantial enough to maintain their
integrity during manufacture and packaging, and permit handling by the patient.
Because of the rapid dissolution, taste and mouth feel are important considerations.
Foams
Foams are dispersions of gas in a liquid or solid continuous phase wherein the liquid
or solid contains the drug substance and suitable excipients. Typical excipients
intended for foam dosage forms include surfactants to ensure distribution of the gas/
propellant in the formulation, aqueous or nonaqueous vehicles, and propellants (for
pressurized systems). Foams are produced by mechanical means or via interaction
of propellant gas and the formulation under pressure. Foams dispensed from
nonpressurized containers use mechanical force to mix the formulation and air
resulting in foam generation. Foams dispensed from pressurized containers use the
propellant(s) present in the gas phase to increase pressure inside the container.
When the nozzle of the actuator is opened, the liquid phase is pushed out through
specific actuators resulting in foam generation. Foams are primarily intended for
application to the skin or mucous membranes. Foams can also be delivered by the
injection route. Foams can be formulated to quickly break down into liquid or to
remain as a foam to ensure prolonged contact. Medicated foams intended to treat
severely injured skin, open wounds, or administered by injection must be sterile.
Gases
Medical gases are products that are administered directly as a gas. A medical gas
has a direct pharmacological action or acts as a diluent for another medical gas.
Gases used as excipients for administration of aerosol products, as adjuvants in
packaging, or produced by other dosage forms, are not included in this definition.
COMPONENTS
Medical gases may be single components or defined mixtures of components.
Mixtures also can be extemporaneously prepared at the point of use.
ADMINISTRATION
Medical gases may be administered to the patient using several methods: nasal
cannulas, face masks, atmospheric tents, and endotracheal tubes for the pulmonary
route; hyperbaric chambers for the pulmonary and topical routes of administration;
jetted tubes that are directed at dental tissue to promote drying in preparation for
fillings and crowns; tubes for expanding the intestines to facilitate medical imaging
during colonoscopy; tubes for expanding the pelvis via transuterine inflation in
preparation for fallopian tubal ligation; and tubes for expanding angioplasty devices.
Gums
Medicated gum is a pliable dosage form that is designed to be chewed rather than
swallowed. Medicated gums release the drug substance(s) into the saliva. Medicated
gums can deliver therapeutic agents for local action in the mouth or for systemic
absorption via the buccal or gastrointestinal routes (e.g., nicotine or aspirin). Most
gums are manufactured using the conventional melting process derived from the
confectionary industry or alternatively may be directly compressed from gum powder.
Medicated gums are formulated from insoluble synthetic gum bases such as
polyisoprene, polyisobutylene, isobutyleneisoprene copolymer, styrene butadiene
rubber, polyvinyl acetate, polyethylene, ester gums, or polyterpenes. Plasticizers and
softeners such as propylene glycol, glycerin, oleic acid, or processed vegetable oils
are added to keep the gum base pliable and to aid in the incorporation of the drug
substance(s), sweeteners, and flavoring agents. Sugars as well as artificial
sweeteners and flavorings are incorporated to improve taste, and dyes may be used
to enhance appearance. Some medicated gums are coated with magnesium
stearate to reduce tackiness and improve handling during packaging. A preservative
may be added.
Implants
Implants are long-acting dosage forms that provide continuous release of the drug
substance often for periods of months to years. They are administered by the
parenteral route and are sterile. Some implants approved as animal drugs to be
administered subcutaneously to the ears are not required to be sterile. Typically for
systemic delivery, they may be placed subcutaneously, or for local delivery they can
be placed in a specific region in the body (e.g., in the sinus, in an artery, in the eye,
in the brain). Implants are usually administered by means of a suitable injector or by
surgical procedure.Polymer implants can be formed as a single-shaped mass such
as a cylinder. The polymer matrix must be biocompatible, but it can be either
bioabsorbable or nonbioabsorbable. Shaped polymer implants are administered by
means of a suitable special injector. Release kinetics are typically not zero-order, but
zero-order kinetics are possible. Drug substance release can be controlled by the
diffusion of the drug substance from the bulk polymer matrix or by the properties of a
rate-limiting polymeric membrane coating. Polymer implants are used to deliver
potent small molecules like steroids (e.g., estradiol for cattle) and large molecules
like peptides [e.g., luteinizing hormone-releasing hormone (LHRH)]. Example
durations of drug substance release are 2 and 3 months for bioabsorbable implants
and up to 3 years for nonbioabsorbable implants. An advantage of bioabsorbable
implants is that they do not require removal after the release of all drug substance
content. Nonbioabsorbable polymer implants can be removed before or after a drug
substance release is complete or may be left in situ. An implant can have a tab with
a hole in it to facilitate suturing it in place (e.g., for an intravitreal implant for local
ocular delivery). Such implants may provide therapeutic release for periods as long
as 2.5 years. Drug substance-eluting stents combine the mechanical effect of the
stent to maintain arterial patency with the prolonged pharmacologic effect of the
incorporated drug substance (to reduce restenosis, inhibit clot formation, or combat
infection). As an example, a metal stent can be coated with a nonbioabsorbable or
bioabsorbable polymer-containing drug substance. The resultant coating is a
polymeric matrix that controls the extended release of the drug substance.
Injections
An injection is an infusion method of putting liquid into the body, usually with a hollow
needle and a syringe which is pierced through the skin to a sufficient depth for the
material to be forced into the body.There are several methods of injection, including:
Intravenous injection
It is a liquid administered directly into the bloodstream via a vein. It is advantageous
when a rapid onset of action is needed.
Intramuscular injection
It is the injection of a substance directly into a muscle.- Many vaccines are
administered intramuscularly. Depending on the chemical properties of the drug, the
medication may either be absorbed fairly quickly or more gradually. Intramuscular
injections are often given in the deltoid, vastus lateralis, ventrogluteal and
dorsogluteal muscles. - Injection fibrosis is a complication that may occur if the
injections are delivered with great frequency or with improper technique.
Subcutaneous injection
Subcutaneous injections are given by injecting a fluid into the subcutis,the layer of
skin directly below the dermis and epidermis. Subcutaneous injections are highly
effective in administering vaccines and such medications as insulin.
Inserts
Inserts are solid dosage forms that are inserted into a naturally occurring
(nonsurgical) body cavity other than the mouth or rectum . The drug substance in
inserts is delivered for local or systemic action. Vaginal inserts are usually globular or
oviform and weigh about 5 g each. Inserts intended to dissolve in vaginal secretions
are usually made from water-soluble or water-miscible vehicles such as polyethylene
glycol or glycerinated gelatin.
Irrigations
These are solutions of medicaments used to treat infections of the bladder, vaginal
and less often the nose. Thin soft rubber tubes used for irrigation solutions
administration are Catheter. (Bladder) A vulcanite or plastic pipe (Vagina), Special
Glass Irrigator (nose). e.g: sterile water for irrigation.
Liquids
As a dosage form, a liquid consists of a pure chemical in its liquid state. Examples
include mineral oil, isoflurane, and ether. This dosage form term is not applied to
solutions.
Pellets
The use of the term “pellet” for implantable dosage forms is no longer preferred . In
veterinary medicine, medicated articles and feeds may be pelletized but are not
considered dosage forms. Pellets are small solid dosage forms that can be designed
as single or multiple entities. They can have a spherical or nearly spherical shape,
although such a shape is not required. Spherical pellets are sometimes referred to
as beads. Pellets used in veterinary medicine may instead be cylindrical in shape.
Pellets can provide several advantages, including physical separation for chemically
or physically incompatible materials and for control of the release of drug substance.
Pellets may be designed with the drug substance dispersed in a matrix or the pellets
may be coated with an appropriate polymer. Pellets may be administered by the oral
(gastrointestinal) route.
Depending on the design, pellets for oral administration can:
1. Protect stomach tissues from irritation
2. Sometimes minimize variability associated with gastric retention of larger dosage
forms
3. Solely extend the release of the drug substance
4. Solely delay the release
5. Both extend and delay the release of the drug substance
Some pellets can be sprinkled on food. In the case of delayed-release formulations,
the coating polymer is chosen to resist dissolution at the lower pH of the gastric
environment but to dissolve in the higher pH of the intestinal environment. Pellets
may be administered by injection. One or several pellets can be injected or surgically
administered to provide continuous therapy for periods of months or years. In
veterinary medicine, pellets may be used to improve palatability of the drug product
and pellets for oral administration may be delivered on top of an individual animal’s
food or feed.
Rinses
A flavored or medicated solution swirled in the mouth, used to treat halitosis, oral
infections, apthous ulcers, stomatitis, or dental biofilm (plaque).
Strips
A strip is a dosage form or device in the shape of a long, narrow, thin, absorbent,
solid material such as filter paper. Typically it is sterile and it may be impregnated
with a compound or be gauged to allow measurements for diagnostic purposes, such
as in measuring tear production. The term “strip” should not be used when another
term such as “film” is more appropriate.
Systems
Systems are preparations of drug substance(s) in carrier devices, often containing
adhesive backing, that are applied topically or inserted into body cavities. The drug
substance is designed to be released in a controlled manner over a specified period
of time or the drug substance is released based on its concentration in the
formulation. Unless otherwise stated in the labeling, the carrier device is removed
after use. The term “system” should not be used when another dosage form term is
more appropriate (e.g., inserts and implants). The notation of strength is either
defined in terms of the amount of the drug substance released from the system over
a specific period of time or as the drug concentration within the formulation (e.g., the
percentage of the drug). Various routes of administration are possible, so the route
must always be indicated in the compendial name when a specific location for
application is essential for proper use (e.g., “intrauterine”, “ocular”, or “periodontal”
as the route of administration). For example, systems applied to the eye are called
ocular systems. The route is named “transdermal” when, for example, systemic
absorption of the drug substance may take place through the dermis without
specifying the region of the body to which the system is applied.
The term “patch” has sometimes been used but is not preferred for use in drug
product monograph nomenclature when referring to a system.
Intrauterine systems are intended for placement in the uterus. Release of the drug
substance can be up to 5 years.
Ocular systems are intended for placement in the lower conjunctival fornix from
which the drug diffuses through a membrane at a constant rate.
Periodontal systems are intended for placement in the pocket between the tooth
and the gum. In some cases, periodontalsystems may be formed in situ in the
periodontal pocket and release the drug substance(s) for several weeks.
TDSs are placed onto intact skin to deliver the drug to the systemic circulation. They
are designed for prolonged release (upto 7 days). Specific quality tests for TDS are
found in (3).
Injectable emulsions Emulsions intended for parenteral administration can be
formulated using the same principles as creams and lotions. The formulation should
be designed for ease of administration. The particle size of the dispersed phase can
vary by route of administration. For example, emulsions intended for intravenous
administration should comply with Globule Size Distribution in Lipid Injectable
Emulsions . The procedure to assure sterility should be validated by media fills.
Preservatives are generally not used in injectable emulsions.
Tapes
A tape is a dosage form suitable for delivering drug substances to the skin. It
consists of a drug substance(s) impregnated into a durable yet flexible woven fabric
or extruded synthetic material that is coated with an adhesive agent. Typically the
impregnated drug substance is present in the dry state. The adhesive layer is
designed to hold the tape securely in place without the aid of additional bandaging.
Unlike TDSs, tapes are not designed to control the release rate of the drug
substance. The term “tape” is not preferred and should not be used for new official
article titles .The drug substance content of tapes is expressed as amount per
surface area with respect to the tape surface exposed to the skin. The use of an
occlusive dressing with the tape enhances the rate and extent of delivery of the drug
substance to deeper layers of the skin and may result in greater systemic absorption
of the drug substance.
PASTILLES
They are solid medicated preparations designed to dissolve slowly in the mouth.
They are softer than lozenges and their bases are either glycerol and gelatin, or
acacia and sugar.
DENTAL CONES
A tablet form intended to be placed in the empty socket following a tooth extraction,
for preventing the local multiplication of pathogenic bacteria associated with tooth
extractions. The cones may contain an antibiotic or antiseptic.
Pessary
Pessaries are solid medicated preparations designed for insertion into the vagina
where they melt or dissolve. There are three types: A- Moulded pessaries: they are
cone shaped and prepared in a similar way to moulded suppositories. B-
Compressed pessaries: made in a variety of shapes and are prepared by
compression in a similar manner to oral tablets. C- Vaginal capsules: are similar to
soft gelatin oral Capsules differing only in size and shape.
Inhalation Powders
Inhalation Powders, commonly known as dry powder inhalers (DPIs), consist of a
mixture of API(s) and typically the carrier; and all formulation components exist in a
finely divided solid state packaged in a suitable container-closure system. The dose
is released from the packaging by a mechanism and is mobilized into a fine
dispersion upon oral inhalation by the patient.
Nasal suppositories
Called nasal bougies or buginaria meant for introduction in to nasal cavity.
Ear cones
Aurinaria and meant for introduction into ear. It is rarely used.
NASAL POWDERS
This dosage form may be developed if solution and suspension dosage forms cannot
be developed e.g. due to lack of drug stability The advantages to the nasal powder
dosage forms are the absence of preservative and superior stability of the
formulation. However, the suitability of the powder formulation is dependent on the
solubility particle size, aerodynamic properties and nasal irritancy of the active drug
and/or excipients. Local application of drug is another advantage of this system but
nasal mucosa irritancy and metered dose delivery are some of the challenges for
formulation Generally, the absorption enhancers act via one of the following
mechanisms: Inhibit enzyme activity: Reduce mucus viscosity or elasticity: Decrease
muco-ciliary clearance; Open tight junctions: Solubilize or stabilize the drug.
Absorption enhancers are generally classified as physical and chemical enhancers.
Chemical enhancers act by destroying.
Transdermal patch
A transdermal patch or skin patch is a medicated adhesive patch that is placed on
the skin to deliver a specific dose of medication through the skin and into the
bloodstream. An advantage of a transdermal drug delivery route over other types
such as oral, topical, etc is that it provides a controlled release of the medicament
into the patient. The first commercially available patch was scopolamine for motion
sickness.
Ear Powder
Ear Powder is an antibacterial and antifungal multi use powder, which works great
not only for moist or yeast-infected ears but also on hotspots. It can be used on any
moist, yeast-infected or scratched part of a dog’s body as a treatment or for faster
healing. On top of that, it’s a great tool for pulling-out ear hair.This remedy is used to
cleanse the ear of excess hair that could contain bacteria, and make cleaning easier.
Ear Powder keeps ears clean and odor-free while reducing waxy build up leaving the
ear canal open and clear.
Colloids
Colloids are the preparations of biphasic system in which one phase is dispersed as
minute particles throughout the other phase. These are preparations for external
use. These are applied with the help of a brush or rod. After application volatile
solvent evaporates leaving flexible, protective film covering the site. e.g: aerosols,
paints, etc
INTERMEDIATE PRODUCTS USED IN COMPOUNDING
Extracts
These are concentrated preparations containing the active principals of vegetable or
animal drugs which have been extracted with suitable solvents and concentrated to
form liquid, soft or dry extract.
Glycerins
These are solutions of medicaments in glycerol with or withoutthe addition of water.
Infusions
These are dilute solutions containing the readily soluble constituents of crude drugs
and prepared by diluting 1 part of concentrated infusion with 10 parts of water.
Concentrated infusions are prepared by cold extraction of crude drugs with 25%
ethanol.
Oxymels
These are preparations in which the vehicle is a mixture of acetic acid and honey.
Spirits
They are alcoholic or aqueous alcoholic solutions of volatile substances used as
flavouring agents.
Tinctures
These are alcoholic preparations containing the active principals of vegetable drugs.
They are relatively weak compared to extracts.
Aromatic waters
These are aqueous solutions, usually saturated of volatile oils or other volatile
substances. Used as flavoring agents.
References
1. Ansel's Pharmaceutical Dosage Forms and Drug Delivery Systems by Loyd V. Allen,
‎
Nicholas G. Popovich, ‎
Howard C. Ansel
2. Pharmaceutical Dosage Forms - Tablets By Larry L. Augsburger, ‎
Stephen W. Hoag
3. Pharmaceutical Dosage Forms: Capsules by Larry L. Augsburger, ‎
Stephen W. Hoag
4. Pharmaceutical Dosage Forms and Drug Delivery: Revised and Expanded by Ram I.
Mahato, ‎
Ajit S. Narang
5. Pharmaceutical Dosage Form: Basics and Beyond by Kamlesh J Wadher, ‎
Umekar J
Milind, ‎
Mishra R Mahesh ·
6. Internet sources: https://en.m.wikipedia.org/; https://www.britannica.com/;
https://www.webmd.com/; https://www.rxlist.com/

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Pharmaceutical Dosage Forms

  • 1. Mawlana Bhashani Science and Technology University Santosh, Tangail-1902 Department of Pharmacy Assignment No: 01 Assignment on Pharmaceutical Dosage Forms Course Code: PHAR 2205 Course Tittle: Pharmaceutical Technology I Submitted By Submitted To Md. Shakil Sarker Student ID: PHA-20008 2nd Year, 2nd Semester Session: 2019-2020 Department of Pharmacy Mawlana Bhashani Science and Technology University Santosh, Tangail-1902 Dr. Md. Mizanur Rahman Moghal Professor Department of Pharmacy Mawlana Bhashani Science and Technology University Santosh, Tangail-1902 Date of Submission: November 14, 2022
  • 2. Pharmaceutical Dosage Forms Introduction to Pharmaceutical Dosage Form Drugs are rarely delivered as pure chemical entities but are approximately usually provided as prepared formulations i.e. dosage form. After converting them into an appropriate dose formulation, they are delivered in several dosage forms.To create an alternative dosage form, non-medicinal chemicals (also known as pharmaceutical ingredients or excipients) are added. By adding pharmaceutical ingredients that solubilize or suspend or thicken or dilute or emulsify or stabilize or preserve them, drug dosage forms can be made more effective and appealing. Definition of Dosage Form Dosage forms are the mechanism by which drug molecules / APIs are administered to areas of action inside the body to generate maximum intended benefits and the lowest unwanted effects. OR The Dosage form is the combination of Active Pharmaceutical Ingredients (API) and Excipients in the formulation. Need Of Dosage Forms Mainly depend on Patient Safety and Drug Safety/ Benefits. 1. Deliver precise dosages in a safe and easy manner. Example – Tablets, capsules, syrups 2. Cover bitter taste or odor of drug substances. Example – Capsules, coated tablets, flavored syrups 3. Insoluble or unstable in the selected vehicle, provide a liquid formulation of the insoluble or unstable medication. Example –Suspension 4. Controlled-release methods prolong the duration of medication effect. Example – Controlled release tablets, capsules, suspensions 5. After oral delivery, a drug substance is protected from stomach acid. Example – Enteric-coated tablets 6. Provide optional drug action from topical administration sites. Example – Ointment, cream, ear and nasal preparations 7. Drugs can be injected into the body's tissues. Example – Implants 8. Inhalation treatment is the most effective way to get optimum medication activity. Example – Inhalants 9. Liquid dosage forms of chemicals soluble in the vehicle of your choice. Example – Solution 10. Provide for the introduction of medication into the body’s orifice. Example – Rectal and vaginal suppositories 11. Protection of a drug substance from atmospheric oxygen or moisture. Example – Coated capsules, sealed ampules.
  • 3. Definition of Drug (Active Pharmaceutical Ingredients) Drogue is an old French term that means "dry herb" and is sometimes used interchangeably with the word "drug". Chemical compounds intended for use in the diagnosis, prevention, treatment, and management of disease(s) in humans and other animals are referred to as "pharmaceutical products" or "pharmaceuticals". Chemical/organic synthesis, molecular modification, and biotechnology have all been used to produce medicines in recent years. OR The Active Pharmaceutical Ingredient (API) is the component of a medication that creates its action. Definition of Excipients They do not increase or affect the therapeutic action of the active components. They are also known as inactive components or excipients and have no pharmacological action in general. Examples of inactive components are dyes, preservatives, sweetening agents, binding materials, coloring agents and flavoring agents, etc Desirable properties of dosage form: Should: • Convenient to handle, use and store • Stable during storage and use • Withstand mechanical shock during transport • Flexibility in different drug strength • Provide expected therapeutic effect • Extent, drug release, onset, intensity, duration of action predictable • Economical and elegant Classification of Dosage Forms SOLID DOSAGE FORM: 1. UNIT DOSAGE FORM: ● TABLETS ○ Lozenges ○ Chewable Tablets ○ Modified Release Tablets ○ Effervescent Tablets etc ● CAPSULE ○ Hard gelatin Capsule ○ Soft Gelatin Capsule
  • 4. 2. BULK ● INTERNAL ○ Fine Powder ○ Granules and Effervescent Granules ● EXTERNAL ○ Dentifrices (Tooth Powder) ○ Ear Powder Liquid Dosage from 1. Biphasic ● Liquid in Liquid ○ Emulsions ● Solid in liquid ○ Suspensions 2. Monophasic ● Internal ○ Syrups ○ Elixirs ○ Linctus ○ Drops ● External ○ Liniments ○ Lotions ○ Gargles ○ Throat Paints ○ Mouth Washes ○ Sprays ○ Eye Lotions ○ Eye Drops ○ Nasal Drops ● Parenteral 3. Semisolid Dosage from ● Internal ● External ● Ointments ● Creams ● Pastes ● Jellies
  • 5.
  • 6.
  • 7. Solid dosage forms Powders Powders are the solid dosage form of medicament, which are meant for internal or external use. They are available in crystalline and amorphous form. In crystalline powders the constituent atoms and molecules are packed in a regularly ordered, repeating three-dimensional pattern. Amorphous powders are non-crystalline materials which possess no long-range order. Any material ranging in particle size from 0.1 to 10000 µ may be described as powder. However powders used in pharmacy generally have a size between 0.1 to 10 µ. The powders are generally used in the following forms: 1. Bulk powder for internal use, Eg: Fine powders or granules 2. Bulk powder for external use, Eg: snuffs, dusting powders and tooth powders. 3. Simple and compound powders for internal use. 4. Powders in the form of compressed tablets and tablet triturates. 5. Powders enclosed in cachets and capsules. 6. Insufflations: Micronized powders meant for being blown in the nasal tract, ears, tooth sokets, vagina etc. 7. Parenteral powders: Powders for dissolution into vehicles before injection. Dusting Powder Dusting powders are meant for application to the intact or broken skin. They are meant for external applications. Desired Property: 1. Ease of flow 2. Spreadability 3. The powder should adhere to the skin and possess good covering. 4. The dusting powder should protect the skin from drying and irritation. 5. Dusting powder should not have any irritant effect. Types: Dusting powders are of two types 1. MEDICAL 2. SURGICAL • Medical dusting powders are used mainly for superficial skin conditions whereas surgical dusting powders are used in body cavities and also on major wounds as a result of burns. • Surgical dusting powders must be sterile (free from bacteria or other living microorganisms) before their use.
  • 8. Formulation: It is generally prepared by mixing two or more ingredients one of which must be either starch, kaolin or talc. Talc and kaolin are most commonly used because these are chemically inert. Use: Dusting powders are mainly used for antiseptic (preventing the growth of disease-causing microorganisms.), astringent (a mild protein precipitant suitable for topical application to shrink tissues), adsorbent (Substance that binds to the drug surface), antiperspirant (a substance that is applied to the skin, especially under the arms, to prevent or reduce perspiration.) and antipruritic (used to relieve itching.)Action. Insufflations • Insufflations are meant for powders being blown in various body cavities, like nose, throat, ears etc. • They are generally applied with the help of insufflators. It sprays the powder into a stream of finely divided particles all over the site of application. Desired Quality 1. It should be finely divided powder. 2. They should be absolutely free from irritation and sensitizing quality. Disadvantages: 1. It is difficult to obtain a measured quantity of the drug as a uniform dose 2. Particles adhere to each other and to the wall of the insufflators due to the electrostatic force. Use: Used for local effects, as in the treatment of ear, nose and throat infections with antibiotics (a medicine such as penicillin or its derivatives that inhibits the growth of or destroys microorganisms.). Snuffs These are finely divided solid dosage forms of medicament which are inhaled into nostrils for its antiseptic, bronchodilator and decongestion action.
  • 9. Dentifrices Dentifrices or tooth powders are hygienic products of everyday use. They may also be medicated in order to exercise some definite action on individual person. These are applied with the help of tooth brush for cleaning the surface of the teeth. Formulation: They contain abrasive agents such as calcium sulphate, magnesium carbonate, sodium carbonate and sodium chloride. It may also contain some detergent and suitable flavor. Detergent action is given by incorporating surfactants. Flavour and taste qualities are very significant in the formulation of dentifrices. Granules The primary powder particles are made to adhere to form larger, multiparticle entities called granules and the process is known as granulation. The bitter, nauseous and unpleasant powders cannot be given in tablet form or in a capsule because a large number of them are required to be taken as a single dose. They also cannot be given as liquid form because of stability problem. Such medicaments are given in the form of granules. The drug is mixed with sugar, flavouring agent and a granulating agent to prepare a coherent mass, which is passed through a sieve to convert it into granules and then dried. These dried granules are supplied in single dose sachets which are dissolved in water before taking. Eg: Granules of antibiotics, such as erythromycin, and penicillin salts. Effervescent granules The effervescent granules are the specially prepared solid dosage form of medicaments, meant for internal use. They contain a medicament mixed with citric acid, tartaric acid and sodium bicarbonate. Sometimes saccharin or sucrose may be added as a sweetening agent. Before administration, the desired quantity is dissolved in water, the acid and bicarbonate reacts together and produce effervescence. The carbonated water produced from the release of carbondioxide serves to mask the bitter taste of drugs. Moreover carbon dioxide stimulates the flow of gastric juice and helps in the absorption of medicaments. 3NaHCO3 + C6H8O7.H2O = C6H5Na3O7 + 3CO2 + 3H2O Sodium Bicarbonate + Citric Acid = Sodium Citrate Tablet A tablet is a hard, compressed medication in round, oval or square shape. Solid dosage form containing unit dose of one or more medicament. Prepared by mould method or compression method. The excipients include: -Binders, glidants (flow aids) and lubricants to ensure efficient tabletting.
  • 10. -Disintegrants to ensure that the tablet breaks up in the digestive tract. -Sweeteners or flavours to mask the taste of bad-tasting active ingredients. -Pigments to make uncoated tablets visually attractive. A coating may be applied to: 1- hide the taste of the tablet's components. 2- make the tablet smoother and easier to swallow . 3- make it more resistant to the environment. 4- extending its shelf life. Types of tablets: Compressed Tablets ● Dispersible tablets ● Chewable tablets ● Film coated tablets ● Enteric coated tablets ● Effervescent tablets ● Immediate release tablets ● Sustained release tablets Molded tablets ● Hypodermic tablets ● Dispensing tablets Special Tablets ● Sub-lingual tablets ● Buccal tablets ● Vaginal tablets ● Rectal tablets BUCCAL AND SUBLINGUAL TABLET Sublingual and buccal medications are administered by placing them in the mouth, either under the tongue (sublingual) or between the gum and the cheek (buccal). The medications dissolve rapidly and are absorbed through the mucous membranes of the mouth, where they enter into the bloodstream. Avoid the acid and enzymatic environment of the stomach and the drug metabolizing enzymes of the liver. Examples of drugs administered by this route: e.g. vasodilators, steroidal hormones. EFFERVESCENT TABLET Effervescent tablets are uncoated tablets that generally contain acid substances (citric and tartaric acids) and carbonates or bicarbonates and which react rapidly in
  • 11. the presence of water by releasing carbon dioxide.They are intended to be dissolved or dispersed in water before use providing: A- Very rapid tablet dispersion and dissolution. B- pleasant tasting carbonated drink. CHEWABLE TABLET They are tablets that chewed prior to swallowing.They are designed for administration to children e.g. vitamin products. HYPODERMIC TABLETS Molded tablets made from completely and readily water-soluble ingredients; formerly intended for use in making preparations for hypodermic injection. They may be administered orally or sublingually when rapid drug substance availability is required. MODIFIED-RELEASE TABLETS Two categories of modified-release tablet formulations are recognized by USP. Delayed-release tablets: Tablets are sometimes formulated with acid-resistant or enteric (also called “gastro-resistant”) coatings to protect acid-labile drug substances from the gastric environment or to prevent adverse events such as irritation. Extended-release tablets: Extended-release tablets are formulated in such a manner as to make the drug substance available over an extended period of time following ingestion. Requirements for dissolution are typically specified in the individual monographs. ORALLY DISINTEGRATING TABLETS Orally disintegrating tablets are intended to disintegrate rapidly within the mouth to provide a dispersion before the patient swallows the resulting slurry where the drug substance is intended for gastrointestinal delivery and/or absorption. Some of these dosage forms have been formulated to facilitate rapid disintegration and are manufactured by conventional means or by using lyophilization or molding processes. Further details may be found in the CDER Guidance for Industry: Orally Disintegrating Tablets. SUBLINGUAL TABLETS Sublingual tablets are intended to be inserted beneath the tongue, where the drug substance is absorbed directly through the oral mucosa. As with buccal tablets, few drug substances are extensively absorbed in this way, and much of the drug substance is swallowed and is available for gastrointestinal absorption.
  • 12. TABLETS FOR ORAL SOLUTION Before administration, tablets for oral solution are intended to be solubilized in a liquid diluent. In some cases, tablets for oral solution also may be chewed or swallowed. TABLETS FOR ORAL SUSPENSION Tablets for oral suspension are intended to be dispersed in a liquid before administration as a suspension. The dosage form is tablets for oral suspension when either the drug substance or the excipients do not dissolve when dispersed in a liquid. In some cases, tablets for oral suspension also may be chewed or swallowed. TABLET TRITURATES Small, usually cylindrical, molded or compacted tablets. Tablet triturates traditionally were used as dispensing tablets in order to provide a convenient, measured quantity of a potent drug substance for compounding purposes, but they are rarely used today. Bolus Tablet Large, usually elongated, tablets intended for administration to large animals. Conventional tableting processes can be used to manufacture bolus tablets, but due to their size higher compression forces may be necessary. Dispersible Tablets Tablets that disintegrates within few seconds in liquid making homogenous mixture before administration to patient. e.g: Zinc DT 10 Capsules Capsules are solid dosage forms in which the drug substance and/or excipients are enclosed within a soluble container or shell or coated on the capsule shell. The shells may be composed of two pieces (a body and a cap), or they may be composed of a single piece. Two-piece capsules are commonly referred to as hard-shell capsules, and one-piece capsules are often referred to as soft-shell capsules. This two-piece and one-piece capsule distinction, although imprecise, reflects differing levels of plasticizers in the two compositions and the fact that one-piece capsules typically are more pliable than two-piece capsules.The shells of capsules are usually made from gelatin. However, they also may be made from cellulose polymers (e.g.,hypromellose)or other suitable material. Most capsules are designed for oral administration. When no deliberate effort has been made to modify the drug substance release rate, capsules are referred to as immediate-release.
  • 13. TWO-PIECE OR HARD-SHELL CAPSULES Two-piece capsules consist of two telescoping cap and body pieces in a range of standard sizes. ONE-PIECE OR SOFT-SHELL CAPSULES One-piece capsules typically are used to deliver a drug substance as a solution or suspension. Liquid formulations placed into one-piece capsules may offer advantages by comparison with dry-filled capsules and tablets in achieving content uniformity of potent drug substance(s) or acceptable dissolution of drug substance(s) with poor aqueous solubility. Because the contact between the shell wall and its liquid contents is more intimate than in dry-filled capsules, undesired interactions may be more likely to occur (including gelatin cross-linking and pellicle formation). MODIFIED-RELEASE CAPSULES The release of drug substance(s) from capsules can be modified in several ways. Two categories of modified-release capsule formulations are recognized by USP. Delayed-release capsules: Capsules are sometimes formulated to include enteric-coated granules to protect acid-labile drug substances from the gastric environment or to prevent adverse events such as irritation. Enteric-coated multiparticulate capsule dosage forms may reduce variability in bioavailability associated with gastric emptying times for larger particles (i.e., tablets) and may minimize the likelihood of a therapeutic failure when coating defects occur during manufacturing. Alternatively, a coating may be applied to the capsule shell to achieve delayed release of the contents. Extended-release capsules: Extended-release capsules are formulated in such a manner as to make the contained drug substance available over an extended period of time following ingestion. Requirements for dissolution are typically specified in the individual monograph. Methods for modifying drug substance release from capsules include coating the filled capsule shells or the contents, in the case of dry-filled capsules. PILLS Pills are small rounded solid dosage forms containing medicament and are intended to be administered orally. Pills are spherical in shape and sometimes coated with varnish, silver leaf, and gold leaf to improve the finish, mask the unpleasant tastes and increase stability. In olden days pills were preferred because of their spherical shape which can be easily swallowed. But now a days it is not used because of the following reasons: 1. Disintegration time of the pills is uncertain. 2. It is difficult to prepare pills of a uniform size. 3. It is difficult to prepare pills of uniform weight.
  • 14. Cachets Cachets are the solid unit dosage forms of medicaments in which drug is enclosed in tasteless sheet made by pouring mixture of rice flour and water between two hot, polished, revolving cylinders. Water is evaporated and sheet of water formed is known is cachet. TYPES Wet sheet cachet: Sealed by moistening the edges with water. Dry sheet cachet Administration: A cachet should be immersed in water for few seconds and then placed on the toungue and swallowed with draught of water. ADVANTAGE * They are quite useful for administering the drugs with unpleasant taste * A large dose can be enclosed in cachet than in a tablet or capsule. Examples: * Sodium amino salicylate cachet. * Isoniazid cachet. Lozenges Lozenges are solid oral dosage forms that are designed to dissolve or disintegrate slowly in the mouth. They contain one or more drug substances that are slowly liberated from the typically flavored and sweetened base. They are frequently intended to provide local action in the oral cavity or the throat but also include those intended for systemic absorption after dissolution. The typical therapeutic categories of drug substances delivered in lozenges are antiseptics, analgesics, decongestants, antitussives, and antibiotics. Molded lozenges are called cough drops or pastilles but these terms are not used in official article titles. Lozenges prepared by compression or by stamping or cutting from a uniform bed of paste are sometimes known as troches (a term not used in official article titles). Compressed or stamped lozenges are often produced in a circular shape. Lozenges can be made using sugars such as sucrose and dextrose, or can provide the benefits of a sugar-free formulation that is usually based on sorbitol or mannitol. Polyethylene glycols and hypromellose are sometimes included to slow the rate of dissolution. Suppositories Suppository is another way to deliver drugs.It’s a small, round or cone shaped object that put in body orifice, often into bottom. Once its inside, its melt and dissolves and releases the medicine and exert local or systemic effects.
  • 15. Type of suppository There are three type of suppository Rectal Suppository – into the rectum. Vaginal Suppository – into the vagina. Urethral Suppository – into male urethra. ADVANTAGES OF SUPPOSITORIES Over Oral Drug Administration: • Avoid first pass metabolism • Introduce drugs into the body • Does not cause nausea and vomiting due to gastric irritation in case of oral therapy • Used before surgery since oral therapy is restricted • Beneficial for patients suffering from severe vomiting • Can be administered to unconscious patients • Can be used as targeted drug delivery system • Localized action with reduced systemic distribution • Get to site of action with lower dose reducing systemic toxicity • Highly beneficial in haemorrhoids or vaginal infections • Prolonged drug action achieved Over parenteral drug administration: • Self-medication • No systemic side effects • No pain or site of action related issues Over Vaginal Tablets: • Suppositories dissolves faster • Total bioavailability achieved • No residue remains like tablet • No need of applicator • Non staining • Non itching DISADVANTAGES OF SUPPOSITORIES: • Mucosal irritation • Patient compliance • Erratic and undesired absorption • Placement too high into rectum may lead to first pass metabolism • Installation may trigger defecation reaction • GI state affects absorption, Diarrhoea & disease states affect absorption
  • 16. Poultices Solid dosage form converted to paste like preparation used externally in the skin to reduce inflammation. A Poultice is a soft, moist mass that is spread on a cloth and than applied on the skin to treat various ailments. Ailments such as insect bites , arthritis , boils, infections and more ...... It is also called CATAPLASM. FORMATION OF POULTICES A homemade poultice is made by mashing herbs, plant material, or another substance with warm or natural oils to make a paste. The paste is applied directly on skin and covered with a piece of clean cloth. TYPES OF POUTICES • Some major types of poultices are: • Onion poultice • Potato poultice • Mustard poultice • Plantain poultice • Comfrey poultice • Tumeric poultice USES • POULTICES are used to cure arthritis. • POULTICES are used to cure inflamation. • To relief itching. • To relief muscle pain muscle spasm • For desalination • In horses to treat joints pain. Liquid dosage forms The liquid dosage forms, whether for internal, parenteral or external use may be either monophasic or biphasic products. Monophasic products are represented by true or colloidal solutions and solubilised preparations. They are appeared to be similar in physical appearance and consists of only one phase. They may have water as the solvent or may be occasionally based on some other liquids. The biphasic products are exemplified by emulsions or suspensions and consists of two phases. In emulsions generally both the phases are liquids, while in suspensions the continuous phase is liquid and the dispersed phase is finely divided solids. Liquid preparations are easy to swallow and thus more useful for pediatrics and geriatrics. On the other hand drug in soluble state is chemically less stable than its insoluble state.
  • 17. Monophasic dosage forms are available as: 1. Liquid for internal use, Eg: Syrups, Elixirs, Linctus, drops and draughts. 2. Liquids for external use, which are of two types: A. Liquid to be applied to the skin, eg: liniments and lotions. B. Liquids for body cavities. Eg: Gargles, throat paints, mouth washes, eye drops, eye lotions, ear drops, nasal drops, spray and inhalations. Liquid for internal use: The largest proportion of the liquid formulations are liquid for internal use. Drug should have sufficient solubility in commonly used solvent, like water. Liquid Formulations for External Use: Monophasic liquids for external use may be categorised into following classes a. Liquids for application to the intact skin, such as liniments, lotions etc b. Liquids for the use in one or the other body cavities such as gargles, throat paints, eye drops, eye lotions, ear drops, ear douches, nasal drops, enemas etc. c. Liquids meant to be inhaled into or sprayed in nasal or respiratory tracts. Biphasic Liquid Dosage form: Liquids which consist of two phases are known biphasic liquids. Eg: Emulsions and suspensions. Collodions Liquid preparations for external use having nitro cellulose used to protect the skin. Collodion is a solution of nitrocellulose in ether or acetone, sometimes with the addition of alcohols. Its generic name is pyroxylin solution. It is highly flammable. As the solvent evaporates, it dries to a celluloid-like film. Compound Wart Remover consists of acetic acid and salicylic acid in an acetone collodion base used in Treatment of warts by keratolysis. Droughts Liquid preparations for oral containing medicaments available in single ose or multiple dose. A draught is an older term used to describe a liquid preparation formulated as a single dose, in a volume which is larger than generally utilised intraditional mixturebformulations. Each draught was usually supplied in a 50mL unit dose container. Example: Ipecacuanha emetic draughts-BPC(treatment of poison). The normal is 10 or 15ml and therefore multiple dose volume is prescribed. Malefern draught emulsion. Paraldehyde draughts- oxidized to acetic acid and cause death Precautions: Do not use, if the solution is discolored.
  • 18. Elixirs Liquid preparation for oral containing medicaments with suitable excipients. Elixirs are clear sweetened and flavoured hydroalcoholic solutions for oral use. Non medicated elixiers such as aromatic elixir are mainly used as flavoured vehicle. Medicated elixiers have their own therapeutic value. Alcohol content in elixiers varies from 3 to 40%. Due to high alcohol content, elixirs are not the choice of dosage forms for pediatrics. The main ingredients of elixirs are ethyl alcohol, water, glycerin, propylene glycol, flavouring agent, colouring agent and some preservative. The medicated elixirs usually contain a potent drug such as, antibiotics, antihistamines or sedatives. Eg: Piperazine Citrate Elixirs I.P (Piperazine Citrate) Emulsions Biphasic liquid dosage form for oral containing medicaments in which fine oil globules dispersed in continuous phase. Emulsions are thermodynamically unstable heterogeneous biphasic system consisting of two immiscible liquids, one of which is dispersed as minute globules into the others. This type of formulations are stabilized by using emulsifying agent. Internal phase droplets are generally ranged in diameter of 0.1 µm to 100 µm. Emulsions are mostly classified as oil in water (o/w) emulsions and water in oil (w/o) emulsions. Emulsions are used for 1. Oral administration, Eg: Liquid Paraffin Emulsion IP 2. Intravenous administration, Eg: Emulsion of vitamin A,D and K and 3. For external use, Eg: Emulsions for topical administration. Oral emulsion Oral emulsions are stabilized oil-in-water dispersions, either or both phases of which may contain dissolved solids either oil is dispersed in finely divided form in water or vice versa Suspensions Biphasic liquid dosage form for oral containing medicaments in which fine solid particles suspended in continuous phase.Suspensions are heterogeneous biphasic, thermodynamically unstable liquid dosage form of medicaments in which insoluble solid particles (as internal, discontinuous or dispersed phase) is uniformly distributed in liquid phase (External, continuous or dispersion phase). In suspensions finely divided particles ranging from 0.5 to 5 microns are dispersed in a liquid vehicle. Suspensions are used for oral, parenteral and external applications. Suspensions which are meant for external applications should have small particle size to avoid
  • 19. gritty feeling to the skin and to cover a larger area of the skin. Smaller particles also helps in the penetration of drug through the skin. Oral suspension Liquid preparations for oral use containing one or more active ingredients suspended in a suitable vehicle. may show a sediment which is readily dispersed on shaking to give a uniform suspension which remains sufficiently stable to enable the correct dose to be delivered Enemas Liquid preparation for rectal containing medicaments. An enema is the procedure of introducing liquids into the rectum and colon via the anus. Types of enema: 1- Evacuant enema: used as a bowel stimulant to treat constipation. E.g. soft soap enema & Mgso4 enema -The volume of evacuant enemas may reach up to 2 liters. - They should be warmed to body temperature before administration. 2- Retention enema: - Their volume does not exceed 100 ml. - No warming needed. - May exert: A- Local effect: e.g. a barium enema is used as a contrast substance in the radiological imaging of the bowel. B- Systemic effect: e.g. the administration of substances into the bloodstream. This may be done in situations where it is impossible to deliver a medication by mouth, such as antiemetics. e.g. nutrient enema which contains carbohydrates, vitamins &minerals. Gargles Concentrated aqueous solutions for external use used to treat throat infections. Gargles are clear aqueous solutions used in the posterior region of mouth by agitating the solution with exhaled air to produce local effect in throat and these are not to be swallowed in large amount. They are usually available in concentrated form with direction for dilution with warm water before use. They are brought into intimate contact with the mucous membrane of the throat and are allowed to remain in contact with it for a few seconds before they are thrown out of the mouth. They are used to relieve soreness in mild throat infection. Phenol or thymol is generally present in small concentration for its antibacterial activity. Potassium chlorate is also included in gargles for its weak astringent effect to tone up a relaxed throat. It also
  • 20. stimulates secretion of saliva which relieves dryness, eg: Phenol gargles, Potassium chloride and phenol gargles. Gels Aqueous colloidal suspensions containing medicaments used as antacids. Gels and jellies are transparent to opaque semisolid preparations meant for external application to the skin or mucous membrane. Considered to be more rigid than jellies. Jellies contain more fluid and less cross-linking agent. They are non-greasy and prepared from Natural gums, eg: Tragacanth, Pectin, Sodium Alginate etc. Synthetic derivatives of natural substances, eg: Methyl cellulose, Sodium carboxymethyl cellulose. Linctuses Viscous, liquid oral preparations used to relief cough. Linctuses are viscous liquid and oral preparations that are generally prescribed for the relief of cough. Mostly it contains ingredient with sedative action and some contains expectorants. Simple syrup is generally used as a vehicle for most of the linctuses. This give soothing to the sore mucous membrane of the throat. To obtain and prolong local action, linctuses should be taken undiluted and sipped and swallowed slowly. Eg: Codeine Linctus B.P.C (API: Codeine Phosphate) Lotions Liquid preparations for external application usually applied without friction. Lotions are suspensions, emulsions, combination of emulsion-suspension or aqueous or non-aqueous solutions designed to be applied to the unbroken skin without friction. Lotions are an emulsified liquid dosage form intended for external application to the skin. Historically, some topical suspensions such as calamine lotion have been called lotions but that nomenclature is not currently preferred. Lotions share many characteristics with creams. The distinguishing factor is that they are more fluid than semisolid and thus pourable. Duento their fluid character, lotions are more easily applied to large skin surfaces than semisolid preparations. Lotions may contain antimicrobial agents as preservatives. They are used for their epidermic effect, such as local cooling, soothing, protective, drying or moisturizing properties depending upon the ingredients used. They are directly applied to the skin with the help of some adsorbent material, such as, cotton wool. Eg: Calamine Lotion I.P Liniments Liquid preparations for external application usually applied with friction. The liniments are liquid or semi-liquid preparations meant for application to the skin. The liniments are usually applied to the skin with friction and rubbing of the skin. They are solutions or emulsions in an aqueous or oily vehicles. They are used as counter irritant, rubefacient and soothing. Alcohols are also used in the preparation of liniments. Alcohol in the liniments helps in the penetration of medicaments into the skin and
  • 21. also increases its counter irritant and rubefacient action. In oily liniments arachis oil is used commonly, which spread more easily on the skin. A liniment should not be applied to the broken skin because it may causes excessive irritation. Eg: Liniment of Camphor. Mixtures Liquid oral preparations containing one or more medicaments. A mixture is a liquidpreparation meant for oral administration in which medicament or medicaments are dissolved, suspended or dispersed in a suitable vehicle. CLASSIFICATION OF MIXTURES 1. Simple mixture containing soluble substances 2. Mixture containing diffusible solids 3. Mixture containing indiffusible solids 4. Mixture containing Precipitate forming liquids 5. Mixture containing Slightly soluble liquid SIMPLE MIXTURE CONTAINING SOLUBLE SUBSTANCES It contains only soluble ingredients.It is represented by true solution.It is a clear homogenous mixture. E.g. Carminative mixture, Expectorant mixture etc. MIXTURE CONTAINING DIFFUSIBLE SOLIDS Diffusible solids are insoluble in water. Uniformly dispersed in the vehicle on shaking. No need of suspending agent. Ex. Bismuth carbonate, Bismuth subnitrate,Magnesium carbonate. MIXTURE CONTAINING INDIFFUSIBLE SOLIDS Indiffusible solids are insoluble in vehicle. Not evenly distribute throughout the vehicle on shaking or not distribute in vehicle for sufficiently long time. So suspending agents are added in formulation.. Ex. Acetyl salicylic acid, Phenacetin, chalk powder. MIXTURE CONTAINING PRECIPITATE FORMING LIQUIDS These liquids are not only insoluble in water but they form indiffusible precipitates particularly when salts are present.They contain resinous matter and when it is mixed with water it leads to precipitation of resin and may stick to the sides of the bottle which will be difficult to rediffuse by shaking. To prevent this, a protective colloid is dispersed in the vehicle before tincture is added. MIXTURE CONTAINING SLIGHTLY SOLUBLE LIQUIDS
  • 22. The insoluble portion of slightly soluble liquids is not readily diffusible.So a suspending agent such as tragacanth powder or tragacanth mucilage are needed to dispense such mixtures. Ex. Paraldehyde liquid Mouth washes Concentrated aqueous solutions for external use used to treat mouth infections and oral hyginic. These are aqueous solutions with a pleasant taste and odour used to make clean and deodorise the buccal cavity. Generally they contain antibacterial agents, alcohol, glycerin, sweetening agents, flavouring agents and colouring agents. Eg: Sodium Chloride Mouth Wash, Compound B.P.C. Nasal drops Liquid preparations containing medicaments that are instilled in to the nose with a dropper used to treat nose infections and blockage of nose. Drugs in solution may be instilled into the nose from a dropper or from a plastic squeeze bottle. The drug may have a local effect, e.g. antihistamine, decongestant. Alternatively the drug may be absorbed through the nasal mucosa to exert a systemic effect.The use of oily nasal drops should be avoided because of possible damage to the cilia of the nasal mucosa. Paints Liquid preparations for external application to the skin or mucous membrane with soft brush. Paints are liquids for application to the skin or mucous membranes.Skin paints contain volatile solvent that evaporates quickly to leave a dry resinous film of medicament. Throat paints are more viscous due to a high content of glycerol, designed to prolong contact of the medicament with the affected site. Throat Paints Throat paints are viscous preparations of medicaments for local action in the pharynx. Glycerin is commonly used as a base because, being viscous, it adheres to mucous membrane for a long period and it possesses sweet taste. They are applied to the throat with a brush. Throat paints are used in treatment of inflammations of various areas of the mouth and throat. Solutions Clear liquid preparation containing with or without medicaments used to internal or external preparations. A solution is a preparation that contains one or more dissolved chemical substances in a suitable solvent or mixture of mutually miscible solvents. Because molecules of a drug substance in solution are uniformly dispersed, the use of solutions as dosagebforms generally provides assurance of uniform dosage upon administration and good accuracy when the solution is diluted or otherwise mixed. Substances in solutions are more susceptible to chemical instability than they are in
  • 23. the solid state and, dose-for-dose, arengenerally heavier and more bulky than solid dosage forms. These factors increase the cost of packaging and shipping relative to that of solid dosage forms. Some solutions are prepared and ready for use, and others are prepared as powders or other solids intended for reconstitution with an appropriate vehicle just before use . Solution dosage forms can be administered by injection, inhalation, and the mucosal, topical, and gastrointestinal routes. A solution administered by injection is officially titled “injection”. Some solutions are designed to form a mass in situ. These solutions comprise polymer, drug substance, and solvent for the polymer. The polymer solvent can be water or an organic solvent. After administration of the solution to a patient by subcutaneous or intramuscular administration, it forms a gel or a solid polymeric matrix that traps the drug substance andbextends the drug substance release for days or months. Solutions intended for oral administration usually contain flavorings and colorants to make the medication more attractive and palatable for the patient or consumer. When needed, they also may contain stabilizers to maintain chemical and physical stability and preservatives to prevent microbial growth. Solutions are sometimes placed on devices such as swabs, cloths, or sponges, that aid application. A solution that needs to be diluted prior to administration previously has been called aconcentrate. The term “concentrate” is no longer preferred. Oral solution Oral solutions are clear Liquid preparations for oral use containing one or more active ingredients dissolved in a suitable vehicle. Syrups Sweet, viscous, concentrated liquid preparations containing with or without sugar and medicaments. Syrups are sweet and viscous aqueous preparations. Simple syrup is a saturated solution of sucrose in purified water. The concentration of sucrose used is 66.7 % w/w (as per Indian Pharmacopoeia, IP). They are either flavoring syrups (syrups containing aromatic or flavored substances) and medicated syrups (Syrup containing medicinal substances). Syrups are used for formulating antibiotics, antitussives, antihistaminic, sedatives, vitamins etc. Most syrups are aqueous solutions of sucrose or dextrose. Artificial syrups are also in the market, where artificial sweetening agents (Eg: saccharine and sodium cyclamate) are used. The artificial syrups are having two points in their favour 1. They are free from carbohydrates and suitable for diabetics. 2. They have lesser stability problems as compared to sugar based syrups. Syrups are commonly used for the following reasons: 1. They are palatable
  • 24. 2. Syrups have high osmotic pressure which prevents growth of bacteria, fungi and prevent decomposition of many vegetable substances. Due to this syrups have the self-preservative activity. 3. Syrups retards oxidation because it is partly hydrolysed into reducing sugars, such as lavulose and dextrose. Semisolid dosage forms Semisolid dosage forms are dermatological products of semisolid consistency and applied to skin for therapeutic or protective action or cosmetic function. Semisolid dosage forms usually are intended for localized drug delivery. In the past few years, however, these forms also have been explored for the systemic delivery of various drugs. Semisolids constitute a significant proportion of pharmaceutical dosage forms. They can be applied topically to the skin, cornea, rectal tissue, nasal mucosa, vagina, buccal tissue,urethral membrane, and external ear lining. Eg: Ointments, creams, jellies and pastes etc. Advantages of semi-solid dosage form: • It is used externally • The probability of side effects can be reduced • First, pass gut and hepatic metabolism is avoided. • Local action and Site-specific action of the drug on the affected area. • Convenient for unconscious patients or patients to have difficulty in oral administration. • Suitable dosage form for bitter drugs. • More stable than a liquid dosage form. Disadvantages of semi-solid dosage form: • The accuracy can’t be measured, for the semisolid dosage form. • May cause staining. • They are bulky to handle. • Application with a finger may cause contamination. • Physico-chemical is less stable than a solid dosage form. • May cause irritation or allergy to some patients Ideal properties of semisolid dosage forms: • Smooth texture • Elegant in appearance • Non-dehydrating • Non-gritty • Non-greasy and non-staining
  • 25. • Non-hygroscopic Ingredients needed for semisolid dosage form: • Bases • Preservative • Humectants • Antioxidants • Emulsifier • Gelling agent • Permeation enhancer • Buffers Bases used in semisolid dosage form: It is one of the most important ingredients used in the formulation of the semisolid dosage form. Ointment bases do not merely act as the carriers of the medicaments, but they also control the extent of absorption of medicaments incorporated in them. Ideal characterization of bases used in semisolid dosage form: They should be: • Inert, non-irritating, and non-sensitizing. • Compatible with skin pH and the drug. • Good solvent and/or emulsifying agent. • Emollient, protective, non-greasy and easily removable. • Release medicament readily at the site of application. • Pharmaceutically elegant and possess good stability Classification of Bases: According to USP ointment bases are classified into four general groups: • Hydrocarbon bases (oleaginous bases) (Petrolatum, Paraffin, Lanolin, etc.) • Absorption bases (cold cream, anhydrous lanolin, etc.) • Water-removable bases ( oil in water) • Water-soluble bases (polyethylene glycol) Antioxidants used in semisolid dosage form: Oxygen has the capability to become a part of potentially damaging molecules called “free radicals.” Free radicals can attack the healthy cells of the body. It can break their structure and that’s why the function is also affected. Example: Butylated hydroxyanisole, Butylated hydroxytoluene Ingredients that increase permeation: Skin can act as a barrier. There are various penetration enhancers that can help the drug to penetrate through the skin.
  • 26. The emulsifier used in semisolid dosage form: Emulsifiers are used to improve the stability of an emulsion by increasing its kinetic stability. It reduces surface tension and prevents coalescence. It helps to increase the viscosity at low concentration. Emulsifying agents used in semisolid dosage form: Sodium lauryl sulfate: Oil/Water emulsion – Sodium stearate and calcium stearate. Glyceryl monostearate: This is a weak Water/Oil emulsifying agent and it is used as a stabilizer and emollient in the Oil/Water emulsion. Humectant used in semisolid dosage form: The humectant is a hygroscopic substance used to increase the solubility of the active ingredient to increase skin penetration. It’s also used to improve the hydration of the skin. Buffers used in semisolid dosage form: Buffers are added for various purposes. Such as • Compatibility with skin. • Drug solubility. • Drug stability. • Influence the ionization of drugs. Preservatives used in semisolid dosage form: Preservatives are used to inhibit the growth of contamination of microorganisms. Example: Para-hydroxybenzoate (parabens), phenols, benzoic acid, sorbic acid, etc. Ointments Semisolid dosage forms for external use containing with or without medicaments with suitable ointment base. Ointments are semisolid preparations with or without medicaments intended for application to the skin. Medicaments used in the formulation is dissolved, suspended or emulsified in an ointment base. Ointment bases recognized for use as vehicles fall into four general classes: hydrocarbon bases, absorption bases, water-removable bases, and water-soluble bases. HYDROCARBON BASE • The ointments are mainly used as protective or emollient for the skin. • Ointments may be used as- 1. Antibiotic ointments. Drug used: Neomycin. 2. Antifungal ointment. Drug used: Benzoic acid, salicylic acid, nystatin. 3. Anti-inflammatory ointment. Drug used: hydrocortisone, etc ENVIRONMENT Temperature: 20-300 C, Humidity: 30-60 %, DOCUMENTS:
  • 27. 1. Standard Operating Procedure (SOP) 2. Batch Manufacturing Record (BMR) 3. Batch Packaging Record (BPR) 4. In House specification Creams Semisolid dosage forms for external use containing with or without medicaments with suitable fatty base. These are viscous semisolid emulsions which are meant for external use. They usually contain a water soluble base due to which they can be easily removed from the skin.They are of softer consistency and have light weight in comparison to true ointments when applied to the skin. Cream leave no visible evidence of their presence on the skin. They are of mostly two types a. Aqueous cream, Eg: Cetrimide Cream B.P b. Oily cream, Eg: Proflavine cream BPC Creams are semi-solid emulsions, that is mixtures of oil and water. - They are divided into two types: A- oil-in-water (O/W) creams: which are composed of small droplets of oil dispersed in a continuous aqueous phase. Oil-in-water creams are more comfortable and cosmetically acceptable as they are less greasy and more easily washed off using water. B- water-in-oil (W/O) creams: which are composed of small droplets of water dispersed in a continuous oily phase. Water-in-oil creams are more difficult to handle but many drugs which are incorporated into creams are hydrophobic and will be released more readily from a water-in-oil cream than an oil-in-water cream. Water-in-oil creams are also more moisturising as they provide an oily barrier which reduces water loss from the stratum corneum, the outermost layer of the skin. Paste Semisolid dosage forms for external use containing high proportion of finely powdered medicaments with suitable fatty base. Pastes are basically ointments into which a high percentage of insoluble solid has been added.The extraordinary amount of particulate matter stiffens the system. Pastes are less penetrating and less macerating and less heating than ointment. Pastes make particularly good protective barrier when placed on the skin, the solid they contain can absorb and thereby neutralize certain noxious chemicals before they ever reach the skin. Like ointments, paste forms an unbroken relatively water – impermeable film unlike ointments the film is opaque and therefore can be used as an effective sun block accordingly.
  • 28. There are two types of paste: a) Fatty pastes (e.g: leaser's paste) . b) Non greasy pastes (e g: - bassorin paste). Fatty pastes that have a high proportion of hydrophilic solids appear less greasy and are more absorptive than ointments.They are used to absorb serous secretions and are often preferred for acute lesions that have a tendency toward crusting, vesiculation, or oozing. Dental pastes are applied to the teeth. Other orally administered pastes may be indicated for adhesion to the mucous membrane for a local effect. Although rare, pastes can be administered orally, for example to evaluate pharyngeal function. In veterinary medicine, pastes are typically administered orally and are intended for systemic delivery of drug substances. The paste is squeezed into the mouth of the animal, generally at the back of the tongue, or is spread inside the mouth. Gels Transparent semisolid dosage forms for external use containing hydrophilic or hydrophobic base with gelling agents Poultices Semisolid dosage forms for external use containing medicaments applied to the skin to hold the dressing and protective. Gaseous dosage forms Aerosols Suspension of fine solid or liquid particles with gas used to apply drug to respiratory tract having atomizer with in device. Aerosols are dosage forms packaged under pressure and contain therapeutic agent(s) and propellant(s) that are released upon actuation of an appropriate valve system. Upon actuation of the valve system, the drug substance is released as a plume of fine particles or droplets. Only 1 dose is released from the preparation upon actuation of a metered valve. In the case of topical products and depending on the nature of the drug substance and the conditions being treated, actuation of the valve may result in a metered release of a controlled amount of the formulation or the continuous release of the formulation as long as the valve is depressed. The aerosol dosage form refers only to those products packaged under pressure that release a fine mist of particles or droplets when actuated . Other products that produce dispersions of fine droplets or particles will be covered in subsequent sections (e.g., Sprays and Powders).
  • 29. TYPES OF AEROSOL DOSAGE FORMS Aerosol dosage forms can be delivered via various routes. The container, actuator, and metering valve, as well as the formulation, are designed to target the site of administration. Inhalation aerosols, commonly known as metered-dose inhalers (MDIs), are intended to produce fine particles or droplets for inhalation through the mouth and deposition in the pulmonary tree. The design of the delivery system is intended to release measured mass and appropriate quality of the active substance with each actuation. Nasal aerosols, commonly known as nasal MDIs, produce fine particles or droplets for delivery through the nasal vestibule and deposition in the nasal cavity. Each actuation of the valve releases a measured mass of the drug substance with appropriate quality characteristics. Lingual aerosols are intended to produce fine particles or droplets for deposition on the surface of the tongue. The design of the delivery system releases 1 dose with each actuation. Topical aerosols produce fine particles or droplets for application to the skin. Inhalations Internal liquid preparations containing medicaments dissolved in suitable solvent or if insoluble suspended in the propellent. Inhaler They are solutions, suspensions or emulsion of drugs in a mixture of inert propellants held under pressure in an aerosol dispenser. Release of a dose of the medicament in the form of droplets of 50 um diameter or less from the container through a springloaded valve incorporating a metering device. The patient then inhales the released drug through a mouthpiece. In some types. the valve is actuated by finger pressure, in other types the valve is actuated by the patient breathing in through the mouthpiece. It is commonly used to treat asthma and other respiratory problems. Nebulizer or (atomizer) A nebulizer is a device used to administer medication to people in forms of a liquid mist to the airways. It is commonly used in treating asthma, and other respiratory diseases. - It pumps air or oxygen through a liquid medicine to turn it into a vapor, which is then inhaled by the patient. As a general rule, doctors generally prefer to prescribe inhalers for their patients, because:
  • 30. 1-These are cheaper 2- more portable 3- carry less risk of side effects. Nebulizers, for that reason, are usually reserved only for serious cases of respiratory disease, or severe attacks. Sprays Gaseous preparations of drugs containing alcohol applied to mucous membrane of nose or throat with atomizer or nebulizer. Spray preparations may deliver either accurately metered or nonmetered amounts of formulation. A spray drug product is a dosage form that contains a drug substance in the liquid state as a solution or suspension and is intended for administration as a mist. Sprays are distinguished from aerosols in that spray containers are not pressurized. Most of the sprays are generated by manually squeezing a flexible container or actuation of a pump that generates the mist by discharging the contents through a nozzle. Depending on the design of the formulation and the valve system, the droplets generated may be intended for immediate inhalation through the mouth and deposition in the pulmonary tree, or for inhalation into the nose and deposition in the nasal cavity. The mechanism for droplet generation and the intended use of the preparation distinguish various types of spray drug products. A spray drug product may be composed of a pump, container, actuator, valve, nozzle, or mouthpiece in addition to the formulation containing the drug(s), solvent(s), and any excipient(s). The design of each component plays a role for the appropriate performance of the drug product and in determining the critical characteristics of the droplet size distribution. Droplet and particle size distributions, delivered dose uniformity, plume geometry, and droplet velocity are critical parameters that influence the efficiency of drug delivery. When the preparation is supplied as a multidose container, the addition of a suitable antimicrobial preservative may be necessary. Spray formulations intended for local or systemic effect typically have an aqueous base and may contain excipients to control pH and viscosity. In addition, depending on the route of administration, the formulation may be isotonic. Others Dosage Forms Magmas Two-phase system with large particle size or floccules of small distance particles. These water insoluble particles. Thick and viscous. Commonly known as milk magnesia .Magma is semi-solid dosage form. Route administration of magma: oral Plasters A plaster is a semisolid substance for external application that is supplied on a support material. Plasters are applied for prolonged periods to provide protection, support, or occlusion (maceration). This term is not preferred and should not be used
  • 31. for new drug product titles. Plasters consist of an adhesive layer that may contain active substances. This layer is spread uniformly on an appropriate support that is usually made of a rubber base or synthetic resin. Unmedicated plasters are designed to provide protection or mechanical support to the site of application. Plasters are available in a range of sizes or cut to size to effectively provide prolonged contact to the site of application. They adhere firmly to the skin but can be peeled off the skin without causing injury. Douches Douches are aqueous solutions intended to clean, deodorise, soothe or medicate body cavities. Eye douches, often termed as eyewashes, are used to remove foreign particles and discharges from the eyes. Douches are generally dispensed in the form of a powder or tablet with a specific directions for dissolving it in a specific quantity of warm water. Vaginal douches must be sterile. They are used for: a. Cleansing agents: Isotonic sodium chloride solution b. Antiseptics. Eg: Mercuric chloride (0.001%) c. Astringent, Eg: Alum (1% Tooth Paste Toothpaste is a paste or gel dentifrice used with a toothbrush to clean and maintain the aesthetics and health of teeth. Toothpaste is used to promote oral hygiene: it is an abrasive that aids in removing dental plaque and food from the teeth, assists in suppressing halitosis, and delivers active ingredients (most commonly fluoride) to help prevent tooth decay (dental caries) and gum disease (gingivitis). Owing to differences in composition and fluoride content, not all toothpastes are equally effective in maintaining oral health. The decline of tooth decay during the 20th century has been attributed to the introduction and regular use of fluoride-containing toothpastes worldwide.Large amounts of swallowed toothpaste can be toxic. Common colors for toothpaste include white (sometimes with colored stripes or green tint) and blue. Hand creams They are a high – viscosity product specifically designed to be used on the hands, to soften and moisturise dry and cracked hands. The high viscosity of the hand cream means that they have a higher percentage of oil as compared to water. As a result, hand creams don’t have the runny texture of lotions and are thicker. These are recommended for people with dry skin as it helps in giving them extra coverage. Hand creams are used most commonly in winter.
  • 32. Hand Washings liquid soap for washing one's hands. Handwash is formulated with a synthetic surfactants, or foaming bases, like SLS (sodium lauryl sulfate), SDS (sodium dodecyl sulfate), ALS (ammonium lauryl sulfate) or SLES (sodium lauryl ether sulfate). These surfactants are derived from petroleum or made synthetically. Either way, they are heavily processed. Synthetic surfactants are detergents that can be used as a base for handwash, body wash, dishwashing detergent, laundry detergent and car cleaning detergent. Hair cream Commonly termed as styling cream, adds natural shine to rough hair. It smoothens the tamed hair and holds them well so that they don't fall. In simple words, it removes frizz and fly-aways without making them heavy.a cosmetic preparation used to improve the condition of, and/or to style the hair. Hair dyes A natural or synthetic substance used to change the colour of a person's hair. Hair coloring, or hair dyeing, is the practice of changing the hair color. The main reasons for this are cosmetic: to cover gray or white hair, to change to a color regarded as more fashionable or desirable, or to restore the original hair color after it has been discolored by hairdressing processes or sun bleaching. Hair coloring can be done professionally by a hairdresser or independently at home. Today, hair coloring is very popular, with 75% of women[1] and 18% of men living in Copenhagen having reported using hair dye. Hair lotion It is a hair styling product that is generally applied to the hair and left on. Its purpose is typically to moisturize the hair, although hair lotion can also be used to treat dry scalp, eczema, dermatitis, and other skin conditions affecting the scalp. Medicated hair lotions may also play a part in many hair-retention and hair-regeneration programs marketed for those suffering from hair loss. While a wide range of hair lotions and oils are available for sale, it is also fairly easy to make these products at home. They often contain simple, readily-available ingredients such as eggs, sugar, and vegetable oil. Soaps and Shampoos Soaps and shampoos are solid or liquid preparations intended for topical application to the skin or scalp followed by subsequent rinsing with water. Soaps and shampoos are emulsions, suspensions, or surface-active compositions that readily form emulsions, micelles, or foams upon the addition of water followed by rubbing. Incorporation of drug substances in soaps and shampoos combines the
  • 33. cleansing/degreasing abilities of the vehicle and facilitates the topical application of the drug substance to affected areas, even large areas, of the body. The surface-active properties of the vehicle facilitate contact of the drug substance with the skin or scalp. Medicated soap and shampoo formulations frequently contain suitable antimicrobial agents to protect against bacteria, yeast, and mold contamination. Throat Paints Throat paints are viscous preparations of medicaments for local action in the pharynx. Glycerin is commonly used as a base because, being viscous, it adheres to mucous membrane for a long period and it possesses sweet taste. They are applied to the throat with a brush. Throat paints are used in treatment of inflammations of various areas of the mouth and throat. Eye drops Eye drops are saline-containing drops used as a vehicle to administer medication in the eye. Depending on the condition being treated, they may contain steroids, antihistamines or topical anesthetics. Eye drops sometimes do not have medications in them and are only lubricating and tear-replacing solutions. These are sterile solutions or suspensions of drugs that are instilled into the eye with a dropper.The eye drops are usually made in aqueous vehicle. It should be sterile, isotonic with lachrymal secretions and free from foreign particles to avoid irritation to the eye. A suitable preservative like phenyl mercuric nitrate (0.002%), Benzalkonium chloride (0.01%) may be used to prevent bacterial or fungal growth. Eye drops usually contain substances having antiseptic, anti-inflammatory, anesthetic and miotic properties. Ophthalmic ointment & gel These are sterile semi-solid. Preparations intended for application. To the conjunctiva or eyelid margin. Ear Drops Ear drops are solutions, suspensions or emulsions of drugs in water, glycerin or propylene glycol intended for instillation into the ear. These are used for removal of excessive cerumen, to treat infection, inflammation or pain and for cleaning and drying of ear. Ear drops are solutions, suspensions or emulsions of drugs that are instilled into the ear with a dropper. It is used to treat or prevent ear infections, especially infections of the outer ear and ear canal.
  • 34. Nasal Drops These are aqueous solutions of drops that are instilled into the nose with a dropper. Nasal drops should be isotonic with 0.9% sodium chloride having neutral pH and viscosity similar to nasal secretions by using0.5% methyl cellulose. Drugs in solution may be instilled into the nose from a dropper or from a plastic squeeze bottle. The drug may have a local effect, e.g. antihistamine, decongestant. Alternatively the drug may be absorbed through the nasal mucosa to exert a systemic effect.The use of oily nasal drops should be avoided because of possible damage to the cilia of the nasal mucosa. EYE LOTIONS Eye lotion are the sterile aqueous solutions used for washing of the eyes.The eye lotions are supplied in concentrated form and are required to be diluted with warm water immediately before use. They are usually applied with a clean eye-bath or sterilized fabric dressing and a large volume of solutions is allowed to flow quickly over the eye. o Eye lotions should be isotonic and free from foreign particles to avoid irritation to the eye.They are required to be prepared fresh and should not be stored for more than two days as the lotion may get contaminated. Films Films are thin sheets that are placed in the oral cavity. They contain one or more layers. A layer may or may not contain the drug substance. Typically, these thin sheets are formed by casting or extrusion that results in a dispersion of the components through the film. Films are classified by the site of application. “Oral films” can be formulated to deliver medication to the mouth such as oral hygiene products or to deliver medication to the gastrointestinal tract for absorption. “Buccal films” and “sublingual films” are formulated to facilitate absorption through the proximal mucosal membranes avoiding first pass metabolism or degradation in the gastrointestinal tract and providing a quick onset of action. Films can be formulated with edible polymers such as pullulan or with water-soluble polymers such as modified cellulose, edible gums, and copolymers. The dissolution rate of the film is controlled to facilitate incorporation of the medication into saliva or for absorption by the proximal mucosa. These films must be substantial enough to maintain their integrity during manufacture and packaging, and permit handling by the patient. Because of the rapid dissolution, taste and mouth feel are important considerations. Foams Foams are dispersions of gas in a liquid or solid continuous phase wherein the liquid or solid contains the drug substance and suitable excipients. Typical excipients intended for foam dosage forms include surfactants to ensure distribution of the gas/ propellant in the formulation, aqueous or nonaqueous vehicles, and propellants (for pressurized systems). Foams are produced by mechanical means or via interaction
  • 35. of propellant gas and the formulation under pressure. Foams dispensed from nonpressurized containers use mechanical force to mix the formulation and air resulting in foam generation. Foams dispensed from pressurized containers use the propellant(s) present in the gas phase to increase pressure inside the container. When the nozzle of the actuator is opened, the liquid phase is pushed out through specific actuators resulting in foam generation. Foams are primarily intended for application to the skin or mucous membranes. Foams can also be delivered by the injection route. Foams can be formulated to quickly break down into liquid or to remain as a foam to ensure prolonged contact. Medicated foams intended to treat severely injured skin, open wounds, or administered by injection must be sterile. Gases Medical gases are products that are administered directly as a gas. A medical gas has a direct pharmacological action or acts as a diluent for another medical gas. Gases used as excipients for administration of aerosol products, as adjuvants in packaging, or produced by other dosage forms, are not included in this definition. COMPONENTS Medical gases may be single components or defined mixtures of components. Mixtures also can be extemporaneously prepared at the point of use. ADMINISTRATION Medical gases may be administered to the patient using several methods: nasal cannulas, face masks, atmospheric tents, and endotracheal tubes for the pulmonary route; hyperbaric chambers for the pulmonary and topical routes of administration; jetted tubes that are directed at dental tissue to promote drying in preparation for fillings and crowns; tubes for expanding the intestines to facilitate medical imaging during colonoscopy; tubes for expanding the pelvis via transuterine inflation in preparation for fallopian tubal ligation; and tubes for expanding angioplasty devices. Gums Medicated gum is a pliable dosage form that is designed to be chewed rather than swallowed. Medicated gums release the drug substance(s) into the saliva. Medicated gums can deliver therapeutic agents for local action in the mouth or for systemic absorption via the buccal or gastrointestinal routes (e.g., nicotine or aspirin). Most gums are manufactured using the conventional melting process derived from the confectionary industry or alternatively may be directly compressed from gum powder. Medicated gums are formulated from insoluble synthetic gum bases such as polyisoprene, polyisobutylene, isobutyleneisoprene copolymer, styrene butadiene rubber, polyvinyl acetate, polyethylene, ester gums, or polyterpenes. Plasticizers and softeners such as propylene glycol, glycerin, oleic acid, or processed vegetable oils are added to keep the gum base pliable and to aid in the incorporation of the drug substance(s), sweeteners, and flavoring agents. Sugars as well as artificial
  • 36. sweeteners and flavorings are incorporated to improve taste, and dyes may be used to enhance appearance. Some medicated gums are coated with magnesium stearate to reduce tackiness and improve handling during packaging. A preservative may be added. Implants Implants are long-acting dosage forms that provide continuous release of the drug substance often for periods of months to years. They are administered by the parenteral route and are sterile. Some implants approved as animal drugs to be administered subcutaneously to the ears are not required to be sterile. Typically for systemic delivery, they may be placed subcutaneously, or for local delivery they can be placed in a specific region in the body (e.g., in the sinus, in an artery, in the eye, in the brain). Implants are usually administered by means of a suitable injector or by surgical procedure.Polymer implants can be formed as a single-shaped mass such as a cylinder. The polymer matrix must be biocompatible, but it can be either bioabsorbable or nonbioabsorbable. Shaped polymer implants are administered by means of a suitable special injector. Release kinetics are typically not zero-order, but zero-order kinetics are possible. Drug substance release can be controlled by the diffusion of the drug substance from the bulk polymer matrix or by the properties of a rate-limiting polymeric membrane coating. Polymer implants are used to deliver potent small molecules like steroids (e.g., estradiol for cattle) and large molecules like peptides [e.g., luteinizing hormone-releasing hormone (LHRH)]. Example durations of drug substance release are 2 and 3 months for bioabsorbable implants and up to 3 years for nonbioabsorbable implants. An advantage of bioabsorbable implants is that they do not require removal after the release of all drug substance content. Nonbioabsorbable polymer implants can be removed before or after a drug substance release is complete or may be left in situ. An implant can have a tab with a hole in it to facilitate suturing it in place (e.g., for an intravitreal implant for local ocular delivery). Such implants may provide therapeutic release for periods as long as 2.5 years. Drug substance-eluting stents combine the mechanical effect of the stent to maintain arterial patency with the prolonged pharmacologic effect of the incorporated drug substance (to reduce restenosis, inhibit clot formation, or combat infection). As an example, a metal stent can be coated with a nonbioabsorbable or bioabsorbable polymer-containing drug substance. The resultant coating is a polymeric matrix that controls the extended release of the drug substance. Injections An injection is an infusion method of putting liquid into the body, usually with a hollow needle and a syringe which is pierced through the skin to a sufficient depth for the material to be forced into the body.There are several methods of injection, including:
  • 37. Intravenous injection It is a liquid administered directly into the bloodstream via a vein. It is advantageous when a rapid onset of action is needed. Intramuscular injection It is the injection of a substance directly into a muscle.- Many vaccines are administered intramuscularly. Depending on the chemical properties of the drug, the medication may either be absorbed fairly quickly or more gradually. Intramuscular injections are often given in the deltoid, vastus lateralis, ventrogluteal and dorsogluteal muscles. - Injection fibrosis is a complication that may occur if the injections are delivered with great frequency or with improper technique. Subcutaneous injection Subcutaneous injections are given by injecting a fluid into the subcutis,the layer of skin directly below the dermis and epidermis. Subcutaneous injections are highly effective in administering vaccines and such medications as insulin. Inserts Inserts are solid dosage forms that are inserted into a naturally occurring (nonsurgical) body cavity other than the mouth or rectum . The drug substance in inserts is delivered for local or systemic action. Vaginal inserts are usually globular or oviform and weigh about 5 g each. Inserts intended to dissolve in vaginal secretions are usually made from water-soluble or water-miscible vehicles such as polyethylene glycol or glycerinated gelatin. Irrigations These are solutions of medicaments used to treat infections of the bladder, vaginal and less often the nose. Thin soft rubber tubes used for irrigation solutions administration are Catheter. (Bladder) A vulcanite or plastic pipe (Vagina), Special Glass Irrigator (nose). e.g: sterile water for irrigation. Liquids As a dosage form, a liquid consists of a pure chemical in its liquid state. Examples include mineral oil, isoflurane, and ether. This dosage form term is not applied to solutions. Pellets The use of the term “pellet” for implantable dosage forms is no longer preferred . In veterinary medicine, medicated articles and feeds may be pelletized but are not considered dosage forms. Pellets are small solid dosage forms that can be designed as single or multiple entities. They can have a spherical or nearly spherical shape,
  • 38. although such a shape is not required. Spherical pellets are sometimes referred to as beads. Pellets used in veterinary medicine may instead be cylindrical in shape. Pellets can provide several advantages, including physical separation for chemically or physically incompatible materials and for control of the release of drug substance. Pellets may be designed with the drug substance dispersed in a matrix or the pellets may be coated with an appropriate polymer. Pellets may be administered by the oral (gastrointestinal) route. Depending on the design, pellets for oral administration can: 1. Protect stomach tissues from irritation 2. Sometimes minimize variability associated with gastric retention of larger dosage forms 3. Solely extend the release of the drug substance 4. Solely delay the release 5. Both extend and delay the release of the drug substance Some pellets can be sprinkled on food. In the case of delayed-release formulations, the coating polymer is chosen to resist dissolution at the lower pH of the gastric environment but to dissolve in the higher pH of the intestinal environment. Pellets may be administered by injection. One or several pellets can be injected or surgically administered to provide continuous therapy for periods of months or years. In veterinary medicine, pellets may be used to improve palatability of the drug product and pellets for oral administration may be delivered on top of an individual animal’s food or feed. Rinses A flavored or medicated solution swirled in the mouth, used to treat halitosis, oral infections, apthous ulcers, stomatitis, or dental biofilm (plaque). Strips A strip is a dosage form or device in the shape of a long, narrow, thin, absorbent, solid material such as filter paper. Typically it is sterile and it may be impregnated with a compound or be gauged to allow measurements for diagnostic purposes, such as in measuring tear production. The term “strip” should not be used when another term such as “film” is more appropriate. Systems Systems are preparations of drug substance(s) in carrier devices, often containing adhesive backing, that are applied topically or inserted into body cavities. The drug substance is designed to be released in a controlled manner over a specified period of time or the drug substance is released based on its concentration in the formulation. Unless otherwise stated in the labeling, the carrier device is removed after use. The term “system” should not be used when another dosage form term is
  • 39. more appropriate (e.g., inserts and implants). The notation of strength is either defined in terms of the amount of the drug substance released from the system over a specific period of time or as the drug concentration within the formulation (e.g., the percentage of the drug). Various routes of administration are possible, so the route must always be indicated in the compendial name when a specific location for application is essential for proper use (e.g., “intrauterine”, “ocular”, or “periodontal” as the route of administration). For example, systems applied to the eye are called ocular systems. The route is named “transdermal” when, for example, systemic absorption of the drug substance may take place through the dermis without specifying the region of the body to which the system is applied. The term “patch” has sometimes been used but is not preferred for use in drug product monograph nomenclature when referring to a system. Intrauterine systems are intended for placement in the uterus. Release of the drug substance can be up to 5 years. Ocular systems are intended for placement in the lower conjunctival fornix from which the drug diffuses through a membrane at a constant rate. Periodontal systems are intended for placement in the pocket between the tooth and the gum. In some cases, periodontalsystems may be formed in situ in the periodontal pocket and release the drug substance(s) for several weeks. TDSs are placed onto intact skin to deliver the drug to the systemic circulation. They are designed for prolonged release (upto 7 days). Specific quality tests for TDS are found in (3). Injectable emulsions Emulsions intended for parenteral administration can be formulated using the same principles as creams and lotions. The formulation should be designed for ease of administration. The particle size of the dispersed phase can vary by route of administration. For example, emulsions intended for intravenous administration should comply with Globule Size Distribution in Lipid Injectable Emulsions . The procedure to assure sterility should be validated by media fills. Preservatives are generally not used in injectable emulsions. Tapes A tape is a dosage form suitable for delivering drug substances to the skin. It consists of a drug substance(s) impregnated into a durable yet flexible woven fabric or extruded synthetic material that is coated with an adhesive agent. Typically the impregnated drug substance is present in the dry state. The adhesive layer is designed to hold the tape securely in place without the aid of additional bandaging. Unlike TDSs, tapes are not designed to control the release rate of the drug substance. The term “tape” is not preferred and should not be used for new official article titles .The drug substance content of tapes is expressed as amount per
  • 40. surface area with respect to the tape surface exposed to the skin. The use of an occlusive dressing with the tape enhances the rate and extent of delivery of the drug substance to deeper layers of the skin and may result in greater systemic absorption of the drug substance. PASTILLES They are solid medicated preparations designed to dissolve slowly in the mouth. They are softer than lozenges and their bases are either glycerol and gelatin, or acacia and sugar. DENTAL CONES A tablet form intended to be placed in the empty socket following a tooth extraction, for preventing the local multiplication of pathogenic bacteria associated with tooth extractions. The cones may contain an antibiotic or antiseptic. Pessary Pessaries are solid medicated preparations designed for insertion into the vagina where they melt or dissolve. There are three types: A- Moulded pessaries: they are cone shaped and prepared in a similar way to moulded suppositories. B- Compressed pessaries: made in a variety of shapes and are prepared by compression in a similar manner to oral tablets. C- Vaginal capsules: are similar to soft gelatin oral Capsules differing only in size and shape. Inhalation Powders Inhalation Powders, commonly known as dry powder inhalers (DPIs), consist of a mixture of API(s) and typically the carrier; and all formulation components exist in a finely divided solid state packaged in a suitable container-closure system. The dose is released from the packaging by a mechanism and is mobilized into a fine dispersion upon oral inhalation by the patient. Nasal suppositories Called nasal bougies or buginaria meant for introduction in to nasal cavity. Ear cones Aurinaria and meant for introduction into ear. It is rarely used.
  • 41. NASAL POWDERS This dosage form may be developed if solution and suspension dosage forms cannot be developed e.g. due to lack of drug stability The advantages to the nasal powder dosage forms are the absence of preservative and superior stability of the formulation. However, the suitability of the powder formulation is dependent on the solubility particle size, aerodynamic properties and nasal irritancy of the active drug and/or excipients. Local application of drug is another advantage of this system but nasal mucosa irritancy and metered dose delivery are some of the challenges for formulation Generally, the absorption enhancers act via one of the following mechanisms: Inhibit enzyme activity: Reduce mucus viscosity or elasticity: Decrease muco-ciliary clearance; Open tight junctions: Solubilize or stabilize the drug. Absorption enhancers are generally classified as physical and chemical enhancers. Chemical enhancers act by destroying. Transdermal patch A transdermal patch or skin patch is a medicated adhesive patch that is placed on the skin to deliver a specific dose of medication through the skin and into the bloodstream. An advantage of a transdermal drug delivery route over other types such as oral, topical, etc is that it provides a controlled release of the medicament into the patient. The first commercially available patch was scopolamine for motion sickness. Ear Powder Ear Powder is an antibacterial and antifungal multi use powder, which works great not only for moist or yeast-infected ears but also on hotspots. It can be used on any moist, yeast-infected or scratched part of a dog’s body as a treatment or for faster healing. On top of that, it’s a great tool for pulling-out ear hair.This remedy is used to cleanse the ear of excess hair that could contain bacteria, and make cleaning easier. Ear Powder keeps ears clean and odor-free while reducing waxy build up leaving the ear canal open and clear. Colloids Colloids are the preparations of biphasic system in which one phase is dispersed as minute particles throughout the other phase. These are preparations for external use. These are applied with the help of a brush or rod. After application volatile solvent evaporates leaving flexible, protective film covering the site. e.g: aerosols, paints, etc
  • 42. INTERMEDIATE PRODUCTS USED IN COMPOUNDING Extracts These are concentrated preparations containing the active principals of vegetable or animal drugs which have been extracted with suitable solvents and concentrated to form liquid, soft or dry extract. Glycerins These are solutions of medicaments in glycerol with or withoutthe addition of water. Infusions These are dilute solutions containing the readily soluble constituents of crude drugs and prepared by diluting 1 part of concentrated infusion with 10 parts of water. Concentrated infusions are prepared by cold extraction of crude drugs with 25% ethanol. Oxymels These are preparations in which the vehicle is a mixture of acetic acid and honey. Spirits They are alcoholic or aqueous alcoholic solutions of volatile substances used as flavouring agents. Tinctures These are alcoholic preparations containing the active principals of vegetable drugs. They are relatively weak compared to extracts. Aromatic waters These are aqueous solutions, usually saturated of volatile oils or other volatile substances. Used as flavoring agents.
  • 43. References 1. Ansel's Pharmaceutical Dosage Forms and Drug Delivery Systems by Loyd V. Allen, ‎ Nicholas G. Popovich, ‎ Howard C. Ansel 2. Pharmaceutical Dosage Forms - Tablets By Larry L. Augsburger, ‎ Stephen W. Hoag 3. Pharmaceutical Dosage Forms: Capsules by Larry L. Augsburger, ‎ Stephen W. Hoag 4. Pharmaceutical Dosage Forms and Drug Delivery: Revised and Expanded by Ram I. Mahato, ‎ Ajit S. Narang 5. Pharmaceutical Dosage Form: Basics and Beyond by Kamlesh J Wadher, ‎ Umekar J Milind, ‎ Mishra R Mahesh · 6. Internet sources: https://en.m.wikipedia.org/; https://www.britannica.com/; https://www.webmd.com/; https://www.rxlist.com/