3. • At the end of the session the phase II learner should be able to
1. Enumerate the drug formulations
2. identify the drug formulations
3. Drug delivery system.
4.
5. VARIOUS DOSAGE FORMS & DRUG DELIVERY SYSTEMS
1. Solid dosage forms
Powders and granules
Capsules
Tablets
Solid oral modified-release
dosage forms
2. Semi-solid dosage forms
Ointment, Cream, Gel
Miscellaneous preparations:
Pastes, plasters, liniments.
Transdermal drug delivery
system
6. 4. Liquid dosage forms
3. Suppositories, Inserts,
Sticks
a) solutions
syrup
elixir
spirit
Aromatic water
Tincture/fluid extractor
Lotion
Injections
b) Disperse systems
Suspension
Emulsion
Gel or magma
Aerosol
Foam
7. 5. Sterile dosage forms and delivery systems.
6.Novel and advanced dosage
forms delivery systems and
devices
a) For topical administration
Iontophoresis
Phonophoresis
b) For oral administration
• Mucoadhesive systems
Medicated Chewing Gums (MCG)
8. c) For vaginal administration
Intravaginal drug delivery systems
d) For ophthalmic administration
ophthalmic ointments
ophthalmic inserts
e) For parenteral
administration
Liposomes
stealth liposomes
f) Miscellaneous
Implant
Auto injection systems/pre-
filled injections
9. 1. SOLID DOSAGE FORMS
Powders and Granules
A powder is defined as a dosage form composed of a solid
or mixture of solids reduced to a finely divided state. It is
intended for internal or external use.
For internal use, it can be taken orally, administered
through nose as snuffs or blown into a body cavity as
insufflations.
For external use, solid powders are applied to
compromised areas of the body.
10. SBI CLRD AQ
Powders can be made into solutions for topical and oral
use. Also used as douches.
Newer delivery systems include powders containing a
bio adhesive material.
These are applied to a specific body area such that the
medication has a prolonged drug effect.
Powder dosage form allows to easily alter the quantity
of medication for each dose.
In cases of infants and young children who cannot swallow
tablets or capsules, powders can be mixed with appropriate
food.
Powder dosage form is preferred when a drug is too bulky to be
prepared as a capsule or tablet.
Powders have a rapid onset of action because they are readily
dispersed.
They have a large surface area and usually require only
dissolution.
11. Insufflated powders are finely divided powders They are applied in
body cavity like ears, nose, vagina, tooth socket, or throat using an
insufflators or 'puffer'.
12. 'Hygroscopic powders' absorb moisture from the air.
'Deliquescent powders' absorb moisture from the air to the extent
that they liquefy.
•For example, Potassium citrate, Sodium iodide, Sodium nitrate, Zinc
chloride. Such powders are dispensed in air-tight containers with
proper instructions on the label for storage in dry places.
13. •Granule is as a dosage form composed of dry aggregates of powder
particles. They may be irregular or spherical in shape. They may be swallowed
as such, dispersed in food, or dissolved in water. They are frequently
compacted into tablets or filled into capsules.
Ex- Granules of Lactobacillus acidophilus for diarrhea.
14. ‘Effervescent granulated salts’
contains ingredients that when in contact with water, rapidly release carbon
dioxide. The dosage form is dissolved m water to initiate the effervescence
prior to ingestion.
Ex- Mixture of sodium bicarbonate, citric acid, and tartaric acid.
15. Capsules, Tablets, and their Modified-release Dosage Forms
Capsules and tablets are one of the preferred oral dosage forms for adults. They
are easy to dispense and carry, are readily identified, and conveniently taken.
They are manufactured in various shapes, colors, and sizes. They can be
administered orally, sublingually, buccally, or vaginally.
They have varied characteristics of weight, hardness, thickness, disintegration, and
dissolution depending on their intended use. Ex- Tramadol 50mg capsule
16. TABLET
Their bioavailability is affected by food.
Tablets that are not scored must not be broken or cut as they have special coatings or drug release features. Breaking
them would compromise the tablet's physical integrity.
Sugar-coated tablets are coated with a sugar layer which quickly dissolves on swallowing.
Gelatin-coated tablet is a capsule-shaped compressed tablet. It is smaller than a capsule filled with an equivalent
amount of powder. Also the gelatin coating facilitates swallowing.
For example, tetracycline and doxycycline preparations should not be taken with dairy products. Calcium in dairy
products binds with these antibiotics to.
17. • Lozenges or troches are disc-shaped solid dosage forms. They contain medicinal agent along with a
flavoring substance in sugar base. They are intended to be slowly dissolved in the oral cavity for local effects.
Chewable tablets have a creamy base and are flavored. They are useful for administration of large tablets to
children and adults who have difficulty in swallowing dosage forms. For ex: Iron chewable tablets.
• Ex - TUSQ, Clotrimazole troche, lozenges for sore throat.
• Immediate-release tablets disintegrate and release their medication with no special rate-controlling
features as of special coatings and other techniques. Ex- Guaifenesin.
18. 2.SEMI-SOLID DOSAGE FORMS
Semisolid dosage forms are used either for local or systemic effects.
Ointment, Cream, Gel
• These are semisolid dosage forms for topical application. Application include direct on the skin, placed
on the surface of the eye, applied nasally, vaginally, or rectally.
• They may be medicated or unmedicated. The unmedicated ones are used for their physical effects as
protectants or lubricants.
• Ointment is a preparation with a fatty or hydrocarbon base. E.g., Neosporin ointment.
• Creams contain one or more medicinal agents dissolved or dispersed in either water- in-oil (W/O)
emulsion or oil-in-water (O/W) emulsion. E.g., fusidic acid and salicylic acid.
19. EMLA (Eutectic Mixture tion' refers to grinding a drug of Local Anesthetics).
melting point of the mixture is less than either of the ingredients.
Ex.
1. Eutectic mixture of Lidocaine & Prilocaine (EMLA; eutectic mixture of local anesthetics)
2. Mixture of camphor and menthol rubbed topically to soothe chest congestion and relieve cough caused by
common cold.
20. Vanishing creams' are oil-in-water emulsions. After application, the water evaporates, leaving
behind a thin residue film on the skin or mucous membrane.
Eg - Cold cream is an example of a water-in-oil type of cream. Gels are jelly-like preparations
consisting of dispersion of small or large molecules in an aqueous vehicle. Gels may thicken on
standing. Hence they must be shaken before use.
• Gels should be stored in tight containers to prevent water loss. E.g., anti-acne gels.
• Pastes are intended for application to the skin.
21. Plasters are solid or semisolid adhesive masses spread
on paper, fabric, plastic or any other suitable backing
material. These are applied to the skin to provide
prolonged contact at the site.
• Non-medicated plasters -protection or mechanical
support at the site of application. E.g., Plaster of Paris
cast.
• Medicated plasters provide effects at the site of
application, such as analgesic or vasodilatation.
• E.g., plaster patches containing lignocaine or
diclofenac sodium for relieving pain , band aids.
22. • Liniments are semi-liquid or liquid or solid preparations meant for application on skin by rubbing.
Rubbing allows for penetration of active ingredients. They are also called heat rubs.
• (TDDS)
This facilitates the passage
of drug through the skin
into the general circulation
for their systemic effects.
23. SUPPOSITORY (in Latin = 'to place under') is a solid dosage form
intended to insert into body orifices. It melts, softens, or dissolves
inside the body and exerts local or systemic effects.
INSERT is a solid dosage form that is inserted into a naturally
occurring (that is nonsurgical) body cavity other than the mouth or
rectum. This includes cavities of the vagina and urethra.
STICKS are a convenient form for administering topical drugs.
Shape and size of a suppository is determined by the orifice it is
intended for.
inserted into the orifice without causing un due distension. Once
inserted it must be retained for the desired duration.
24. Rectal suppositories
for adults are about 1.5 inch long. They are cylindrical, bullet, torpedo
(cigar shaped), or little finger in shape. And in infants & children are about
half the size of the adult suppositories & are pencil-like shape.
Suppositories are adversely affected by heat and high humidity so it must be
stored in cool and dry place (not in the bathroom).
Should be placed at room temperature or in refrigerator as directed on the
label.
The patient must be clearly informed regarding whether to moisten the
suppository prior to insertion, how far to insert it, and how long to remain
inactive after insertion.
Female urethral suppositories
are about half the length and weight of the male urethral suppository. (d)
Medication sticks are cylindrical in shape.
a) They are packaged in an applicator tube for topical administration.
Vaginal inserts or pessaries
are globular, oviform, or cone shaped. Used as antiseptics, contraceptives.
Urethral inserts or bougies
are slender, pencil-shaped suppositories.
25. 3.LIQUID DOSAGE FORM SOLUTIONS
Solution is a liquid preparation that contains one or more chemical substances dissolved in a
suitable solvent. Apart from medicinal component, the solutions also contain agents to provide
color, flavor, sweetness, and stability.
Syrup is an aqueous solution containing a sugar. E.g., Paracetamol syrup.
Elixir is a sweetened hydro alcoholic solution.
E.g., elixir for allergy, elixir for bronchitis, and paracetamol elixir.
26. • Spirit is solution of aromatic substance in alcohol.
E.g., Aromatic spirit of ammonia.
• Aromatic water is solution of aromatic substance in water.
E.g., peppermint water.
Tincture is a fluid extract prepared by extracting active constituents from crude drugs.
E.g., tincture of ginger, tincture of iodine.
• Lotion is a low-viscosity topical preparation intended for application on the skin.
E.g., calamine lotion .
Injection is sterile, pyrogen-free solution intended for parenteral administration.
E.g., streptomycin injection .
27. • Suspensions: are preparations containing finely divided drug particles
distributed uniformly in a vehicle in which the drug exhibits a minimum
degree of solubility.
• The advantage of this preparation is that disagreeable taste of certain drugs
in solution form is overcome when the drug is administered as undissolved
particles in oral suspension.
• For example, simethicone antacid suspension, paracetamol suspension.
28. Emulsion: is dispersion of two immiscible liquids.
Small globules of dispersed phase are distributed
evenly in the dispersion phase.
• An emulsifying agent is necessarily added to
prepare a stable emulsion.
• It may either be a liquid or a semi-solid
preparation meant for oral, parenteral, or
topical use.
• It includes lotions, liniments, creams, and
ointments. The process of mixing two
immiscible liquids with the help of an
emulsifying agent is called as emulsification.
29. small-volume (e.g. insulin) & large-volume (e.g. dextrose) injectable
preparations.
irrigation fluids (e.g. sodium chloride solution) to body wounds or surgical
openings dialysis solutions ophthalmic, nasal, or otic preparations.
Biologic preparations (substances obtained from living organisms) –
antibiotics, hormones, vitamins vaccines, toxoids, and antitoxins. For
example, BCG vaccine.
Sterility in above preparations is essential because they are placed in direct
contact with the internal body fluids.
30. Medicated foam
• is an emulsion containing gas bubbles dispersed
in liquid phase containing the active ingredient.
Surfactants are added to ensure proper dispersion &
foam formation. It is packaged in a pressurized container
and is intended for application to the skin or mucous
membranes.
•It is fluffy and semi-solid in consistency.
Ex- clobetasol foam for dermatitis
31. Metered-dose inhalers (MDIs) for as It has 4 parts: Canister,
Actuator, Mouthpiece, Dust-Cap
canister to be held in upside-down position between index
finger and thumb
after complete exhalation, mouthpiece is placed between
the lips
the actuator is pressed down with simultaneous inhalation
breath should be held for as long as possible to achieve
maximum effects of the drug
remove the mouth piece and exhale slowly.
Translingual aerosol (Nitro lingual spray) used for acute
angina
it is aerosol formulation
not to be inhaled
when required, metered spray emissions are done
32. NOVEL & ADVANCED DOSAGE FORMS
DELIVERY SYSTEMS & DEVICE
1. FOR TOPICAL ADMINISTRATION
(i) Ionotophoresis (IP):
It is an electrochemical method that enhances the transport of ionic drugs into the skin by
creating a potential gradient across the skin with an applied electrical current or
voltage. E.g., lidocaine for topical anaesthesia.
(ii)Phonophoresis or ultra phonophoresis:
It is a combination of ultrasound therapy with topical drug therapy to obtain therapeutic drug concentrations at
selected sites in the skin.
Basic principles of Phonophoresis -Ultrasound pulses are passed through the drug delivery under the probe into
the skin fluidizing the lipid guidance of USG.
33. •Advantages of IP and Phonophoresis include:
• The delivery rate of a drug can be controlled by variations of current or ultrasound.
Elimination of gastrointestinal incompatibility, erratic absorption, and first-pass metabolism.
Reduction of side effects and variation among patients.
Risks of infection, inflammation, and fibrosis associated with repeated injections or continuous
infusion.
patient compliance is enhanced
34. 2. FOR ORAL ADMINISTRATION
Mucoadhesive System: A buccal system is designed to adhere to the gum or inner cheek
to provide a controlled and sustained release of drug through the buccal mucosa.
E.g., for fentanyl buccal film.
Medicated Chewing Gums (MCG): It is a semisolid preparation that is designed to be
chewed rather than swallowed. It releases active ingredient into the saliva for both local action or
for systemic absorption.
E.g., nicotine chewing gum .
35. • Osmotic Pump: It is designed for constant-rate and programmed delivery
of a drug. It consists of a flexible impermeable diaphragm surrounded by a
sealed layer containing an osmotic agent that is enclosed within a
semipermeable membrane. E.g., for prazocin osmotic pump .
36. 3.FOR VAGINAL ADMINISTRATION INTRAVAGINAL DRUG DELIVERY SYSTEM
Vaginal administration of drugs has the following advantages:
Self-insertion and removal continuous drug administration at an effective dose level
side.
Effects resulting from oral peak and valley drug administration are minimized by this
system due to continuous release and local absorption of the drug.
Good patient compliance For example, Progesterone Vaginal Insert , Estrogen
containing estradiol, Crinone Gel containing progesterone, Intrauterine Progesterone
Drug Delivery System .
37. 4. FOR OPHTHALMIC DRUG ADMINISTRATION
•One of the major problems associated with the use of ophthalmic solutions is that
majority of it is lost through tears and the action of nasolacrimal drainage very soon
after installation. Novel drug delivery systems include:
ophthalmic ointments
ophthalmic inserts
•Such systems have increased viscosity which allows greater contact time between the
medication and the corneal surface.
38. 5. FOR PARENTERAL ADMINISTRATION
Novel parenteral systems include:
Liposomes:
are small vesicles containing a bilayer of phospholipid encapsulating an
aqueous space. The water-soluble drugs are present in the aqueous
spaces, and lipid- soluble drugs in the membrane
39. ADVANTAGES OF LIPOSOMES
Liposome-encapsulated drugs reach the targeted tissue intact and are released when the liposome
is destroyed there by enzymes.
Other tissues and cells of the body are protected from the drug. Thus, side effects are minimized.
Liposomes carry both hydrophilic and lipophilic drugs without chemical modification.
40. Disadvantage of liposome preparations
They are taken up by cells of the reticuloendothelial system (RES) and
destroyed by the phagocytes.
•(ii) Stealth liposomes: These are designed to evade detection by RES.
•The liposomes are coated with polymer polyethylene glycol (PEG).
•This extends the half-life of liposomes in the body .
41. Miscellaneous Novel Preparations
(i) Implant
It is a long-acting dosage form that provides
continuous release of the drug, often for
periods of months to years.
Route of administration:
parenteral route
subcutaneous
Types of implants
Pellets
Resorbable microparticles
Polymer implants
In situ-forming gel/solid implants
Metal/plastic implants
Drug-eluting stents
42. E.g.,
Etonogestrel implant is a small plastic rod containing progestin. It is inserted sub-dermally in upper
arm, just inside and above the elbow. It provides long-term contraception for 3 years.
(ii) Autoinjection Systems/Pre-filled Injections
For example:
Insulin Pen - for self-administration of prescribed quantity of Insulin,
Epipen - for delivering Epinephrine during emergencies like anaphylactic shock.
43. Novel drugs include radiopharmaceuticals and products of biotechnology.
Radiopharmaceuticals
Radiopharmaceuticals are a radioactive pharmaceutical agent used for diagnostic or therapeutic
procedures.
For diagnostic purpose commonly applied in cardiology (investigating myocardial perfusion), oncology
(tumor imaging and localization), neurology (investigating cerebral perfusion), and nephrology (for
infection imaging).
For therapeutic purpose their role is evolving in form of nuclear medicine. For example, in treatment of
thyroid cancer, Graves disease, hyperthyroidism, and bone pain palliation in cases of bone metastasis.
44. Products of Biotechnology
Biotechnology refers to any technological application in biological
systems, living organisms, or derivatives thereof to make or modify
products or processes for specific use. It encompasses the use of
tissue culture, living cells, or cell enzymes to make a defined product
45. A distinct advantage of the biotechnologic proteins over proteins from natural sources is
enhanced purity.
Techniques used to produce products of biotechnology include:
rDNA technology
MAb (monoclonal antibody) technology
polymerase chain reaction
gene therapy
nucleotide blockade
antisense nucleic acids
peptide technology
47. NANOTECHNOLOGY
• involves the use of particles ranging from 1- to 100-nm.
Their unique physicochemical properties include ultra-small size, large surface area- to-mass ratio,
and high reactivity.
•Has the following advantages:
solubility of poorly water-soluble
immunogenicity is reduced
prolonged duration of action and hence reduced frequency of dosing
minimal systemic side effects due to targeted therapy (see Fig. 1.88)
For example, it is used in the treatment of cancer, diabetes, pain relief, asthma, and allergy.
Targeted drug delivery is a method of delivering medication in a manner that increases the
concentration of the medication in desired part of the body relative to others.
49. Q1.. Paracetamol is commonly self-administered by patients for fever.
Is it labelled as a 'drug' or a 'poison'? Why?
A2. Paracetamol is a 'drug' as long as it is taken in recommended doses.
If taken in larger amounts it might result in serious side effects and
hence termed as 'poison' then.
