This document provides an overview of basic information on pharmaceutical dosage forms and drug delivery systems. It discusses active drug substances and the need for dosage forms to deliver drugs effectively. Common dosage forms are described for oral, rectal, and other systemic routes of administration. These include tablets, capsules, liquids, and suppositories. Immediate and controlled release solid oral dosage forms are also covered. The document aims to familiarize readers with common dosage forms and factors influencing drug delivery through different systems.
Teaching the history of pharmacy to young people is a challenge but it can be done if delivered in an interesting and engaging way. These slides summarize what I share with my students.
Teaching the history of pharmacy to young people is a challenge but it can be done if delivered in an interesting and engaging way. These slides summarize what I share with my students.
Excipients have been defined in many ways, including as inert substances used as vehicles and diluents for drugs. The problem with this definition is that in recent years excipients have proved to be anything but inert, not only possessing the ability to react with other ingredients in the formulation, but also to cause adverse and hypersensitivity reactions in patients. These range from a mild rash to a potentially life-threatening reaction. Different brands of the same drug may contain different excipients, especially preservatives and colourants. The Consumer Medicines Information provides a list of excipients, and information on the safety of individual excipients can be found in drug reference guides.
Excipients have been defined in many ways, including as inert substances used as vehicles and diluents for drugs. The problem with this definition is that in recent years excipients have proved to be anything but inert, not only possessing the ability to react with other ingredients in the formulation, but also to cause adverse and hypersensitivity reactions in patients. These range from a mild rash to a potentially life-threatening reaction. Different brands of the same drug may contain different excipients, especially preservatives and colourants. The Consumer Medicines Information provides a list of excipients, and information on the safety of individual excipients can be found in drug reference guides.
This ppt is for pharmacology students of MBBS UG&PG and other healthcare persons who needs basic science like BDS, Nursing Ayurveda unani homeopathy etc.
Surfactants and their applications in pharmaceutical dosage formMuhammad Jamal
This presentation is very much helpful for the medical students,pharmacists, researchers and other health care providers. i hope it will provide important information regarding surfactants and their applications in pharmaceutical dosage forms.
It will provide you a complete journey through the routes of drug administration, with all the basics covered I hope this presentation will make your fundamentals crystal clear.
Evento organizado pelo Instituto de Estudos Avançados da USP, Polo Ribeirão Preto.
Mais informações: http://www.iearp.blogspot.com.br/2012/09/nanotecnologia-aplicada-saude-uma-nova.html
Dosage forms (also called unit doses) are pharmaceutical drug products in the form in which they are marketed for use, with a specific mixture of active ingredients and inactive components (excipients), in a particular configuration (such as a capsule shell, for example), and apportioned into a particular dose. For example, two products may both be amoxicillin, but one is in 500 mg capsules and another is in 250 mg chewable tablets. The term unit dose can also sometimes encompass non-reusable packaging as well (especially when each drug product is individually packaged[1]), although the FDA distinguishes that by unit-dose "packaging" or "dispensing".[2] Depending on the context, multi(ple) unit dose can refer to distinct drug products packaged together, or to a single drug product containing multiple drugs and/or doses. The term dosage form can also sometimes refer only to the pharmaceutical formulation of a drug product's constituent drug substance(s) and any blends involved, without considering matters beyond that (like how it is ultimately configured as a consumable product such as a capsule, patch, etc.). Because of the somewhat vague boundaries and unclear overlap of these terms and certain variants and qualifiers thereof within the pharmaceutical industry, caution is often advisable when conversing with someone who may be unfamiliar with another person's use of the term.
Depending on the method/route of administration, dosage forms come in several types. These include many kinds of liquid, solid, and semisolid dosage forms. Common dosage forms include pill, tablet, or capsule, drink or syrup, and natural or herbal form such as plant or food of sorts, among many others. Notably, the route of administration (ROA) for drug delivery is dependent on the dosage form of the substance in question. A liquid dosage form is the liquid form of a dose of a chemical compound used as a drug or medication intended for administration or consumption.
Various dosage forms may exist for a single particular drug, since different medical conditions can warrant different routes of administration. For example, persistent nausea, especially with vomiting, may make it difficult to use an oral dosage form, and in such a case, it may be necessary to use an alternative route such as inhalational, buccal, sublingual, nasal, suppository or parenteral instead. Additionally, a specific dosage form may be a requirement for certain kinds of drugs, as there may be issues with various factors like chemical stability or pharmacokinetics. As an example, insulin cannot be given orally because upon being administered in this manner, it is extensively metabolized in the gastrointestinal tract (GIT) before reaching the blood stream, and is thereby incapable of sufficiently reaching its therapeutic target destinations. The oral and intravenous doses of a drug such as paracetamol will differ for the same reason
Notes made by PU student:
INTRODUCTION TO DRUG AND DIFFERENT DOSAGE FORMS
Drug
Pharmaceutical Preparations Manufactured by Pharmaceutical Industry
Pharmaceutical Preparations Compounded Individually
SOLID DOSAGE FORMS
LIQUID DOSAGE FORMS
SEMI-SOLID DOSAGE FORM
NEW DRUG DELIVERY SYSTEMS
Tablets-
Tablets are unit dosage form in which one usual dose of the drug has been accurately placed.
Advantages
Unit dosage form, greatest dose precision and least content variability.
Lowest cost
Lightest and most compact form
Easiest and cheapest to package
Product identification is also cheap no additional processing required
Provide greatest ease of swallowing.
Special release profile can formed
Chemical, Mechanical and microbiologic stability.
Suitable for large scale production
Disadvantages
Some drugs not suitable for compression (amorphous, flocculents , low density )
Drugs with por wetting , slow disslution, intermediate to large dosage are difficult to formulate into tablet.
Bitter tasting, objectional odor, drugs sensitive to oxygen may require coating
( capsule prefer at low cost)
Tablets used for Ingestion
Compressed Tablets or Standard compressed Tablets
Standard uncoated tablets made by compression- wet granulations, double compaction or direct compression.
Rapid disintegration & drug release
Most of tablets containing drugs which gives local effect.( GIT- Water insoluble drugs – Antacids and adsorbents)
Some drugs produced systemic effect ( aqueous solubility- Disintegrate and dissolve in GI contents)
2. Multiple compressed Tablets
Either two components or three components systems
A tablet within a tablet
Tablet within tablet within a tablet.
3. Chewable Tablets
Chew in mouth prior to swallowing & not intended to be swallowed intact.
Infants and children or for elderly
Bitter and foul tasting drugs not suitable.
E.g.- Antacid tablets
( large dose of antacid can be given and better acid neutralization)
4. Sugar and Chocolate coated
5. Film coated Tablets
Polymers such as Hydroxypropyl cellulose (HPC), Hydroxypropyl methyl cellulose(HPMC), widely used with suitable plasticizer.
Advantages
Better mechanical strength
Avoid sugar for significant segments of population
Retain debossed markings
Tasteless Tablet
- Disadvantge
Physical appearnce ( Elegancy) not match with sugar coated tablets.
6. Repeat action Tablets
The core of tablet is coated with shellac or an enteric polymer so drug not releases into stomach.
Second dose added into sugar coatings.
7. Delayed action And Enteric coated Tablets
Enteric coated Tablets are a type of delayed action tablet.
But not all types of delayed type of tablets are enteric.
Why enteric coating?
Some drugs irritate gastric mucosa (Aspirin)
Some drugs destroyed in stomach (Erythromycin)
For local effect in intestine( antibacterial, Vermifuge)
Cellulose acetate phthalate, polyvinyl acetate phthalate, HPMC phthalate
Acid esters ( insoluble in GI media)
Esterases in intestinal fluid break down ester linkages.
8. Controlled release Tablets
Tablets used for oral cavity
1. Buccal & Sublingual Tablets
These tablets are small & somewhat flat
Buccal tablets intended to be held between the cheek and teeth or in the cheek pouch
Sublingual tablets intended to held beneath the tongue.
Drugs admi
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Embracing GenAI - A Strategic ImperativePeter Windle
Artificial Intelligence (AI) technologies such as Generative AI, Image Generators and Large Language Models have had a dramatic impact on teaching, learning and assessment over the past 18 months. The most immediate threat AI posed was to Academic Integrity with Higher Education Institutes (HEIs) focusing their efforts on combating the use of GenAI in assessment. Guidelines were developed for staff and students, policies put in place too. Innovative educators have forged paths in the use of Generative AI for teaching, learning and assessments leading to pockets of transformation springing up across HEIs, often with little or no top-down guidance, support or direction.
This Gasta posits a strategic approach to integrating AI into HEIs to prepare staff, students and the curriculum for an evolving world and workplace. We will highlight the advantages of working with these technologies beyond the realm of teaching, learning and assessment by considering prompt engineering skills, industry impact, curriculum changes, and the need for staff upskilling. In contrast, not engaging strategically with Generative AI poses risks, including falling behind peers, missed opportunities and failing to ensure our graduates remain employable. The rapid evolution of AI technologies necessitates a proactive and strategic approach if we are to remain relevant.
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2. Introduction Drug ?
Active drug substance (active pharmaceutical ingredient - API)
– chemical compound with pharmacological (or other direct effect ) intended for used in diagnosis,
treatment or prevention of diseases
– International nonproprietary names (INN, „generic“ names)
Why you should be familiar with the basic properties of pharmaceutical dosage forms?
Direct clinical use of the active drug substances „as they are“ is rare due to the
number of good reasons:
– API handling can be difficult or impossible (e.g., low mg and g doses)
– Accurate drug dosing can be difficult or impossible
– API administration can be impractical, unfeasible or not according to the therapeutically
aims
– Some API can benefit from reducing the exposure to the environmental factors (light,
moisture…), or they need to be chemically stabilised due to the inherent chemical
instability
– API can be degraded at the site of administration (e.g., low pH in stomach)
– API may cause local irritations or injury when they are present at high concentrations at
the site of administration
– API can have unpleasant organoleptic qualities (taste, smell – compliance!)
– Administration of active substance would mean to have no chance for modification
(improvement) of its PK profile
Besides the choice of the active drug substance, you need to also make a responsible decision
regarding the route of administration and the DOSAGE FORM (drug delivery system) – wrong
choice can cause failure of therapy
You should also be able to handle and administer the drug properly or advise the patient
about it – wrong use can cause failure of therapy
3. From drug substance to
pharmaceutical preparation
Active drug substance (active pharmaceutical ingredient - API)
Excipients (inactive pharmaceutical ingredients)
– Technological, biopharmaceutical and/or stability reasons
– Diluents/fillers, binders, lubricants, desintegrants, coatings, preservants and stabilizers,
colorants and flavourings
– Should always be stated in SPC (important in the case of allergies)
Pharmaceutical dosage form
– determines the physical form of the final pharmaceutical preparation
– is a drug delivery system which is formed by technological processing (drug formulation)
– must reflect therapeutic intentions, route of administrations, dosing etc.
Pharmaceutical preparation (PP)
– particular pharmaceutical product containing active and inactive
pharmaceutical ingredients formulated into the particular dosage form.
– Packed and labelled appropriately
– Two major types of PP according the origin:
Manufactured in large scales by pharmaceutical industry (original and generic
preparations)
Compounded individually in compounding pharmacies
4. Pharmaceutical preparations
manufactured by pharmaceutical industry
Currently certainly the most frequent and favourable approach
MUST be approved by national authority (FDA, SUKL…); in the EU - there is an important role
of central authority (EMEA)
Rigorous quality control (QC) and quality assurance (QA) during manufacturing - with
surveillance of national authorities to ensure the safety and effectiveness
Original pharmaceutical preparations
– undergo full and very extensive pharmacological/toxicological and pharmaceutical pre-
clinical and clinical development and evaluation
– particularly important is the proof of effectiveness and safety
Generic pharmaceutical preparations („authorised copies of original preparations“)
– Can be released after the expiration of the patent protection of the original preparation
– The approval for clinical use is easier due to the prior experience with the original
preparation
– Must be pharmaceutically equivalent: same API, dose, pharmaceutical dosage
form and the same route of administration as in original preparation
– Must be clinically bioequivalent: i.e. it must be of very close PK profile as
original preparation. PK parameters (Cmax, tmax, AUC) are within 80-125 %
range as compared with the original preparation.
– The proof of therapeutic equivalence (comparing directly the clinical effectiveness) is not
commonly required (due to the technical, financial and ethical issues). Hence, it can be
only assumed from the bioequivalence
– Decrease the costs of pharmacotherapy and thus make the drugs more
available
5. Pharmaceutical preparations
compounded individually
These PP are compounded individually for a particular patient according to the
physician's prescription in a pharmacy licensed for compounding
In contrast to the past, they are used rather rarely and mostly in specific situations
It is highly advisable that whenever the particular suitable PP is approved and
commercially available it should be preferred over the compounding
The main advantage of compounded PP is the opportunity to individualize the
pharmacotherapy
– Although the choice of commercially available PP manufactured by pharmaceutical
industry is quite rich it need not cover all individual demands
– Hence, the individually compounded PP can be a justified choice when:
The drug in a particular dosage form is not commercially available on the market
The extraordinary low or high dose is needed (young children, elderly people, special situations –
e.g., intoxications). In this case right dosage strength need not be readily commercially available
for every patient
The patient suffers from the allergy on a specific excipients (e.g., lactose – a filler, some
colorizing/flavouring or antimicrobial agents - parabens) or another drug appearing in the PP
Patient is unable to use a PP in its commercially available dosage form (e.g., children, elderly)
The major disadvantage is the lack of standardization (it is always a „single-patient
batch“), unavailability of rigorous QC testing and the appropriate clinical evaluation.
6. Classification of pharmaceutical dosage
forms according to its physical properties
Dosage forms
– Homogenous systems
– Dispersion systems – one phase (dispersed phase) is distributed
throughout another one (continuous phase, dispersion medium)
According to the size of dispersed particles (1 nm- 0,5 mm) a molecular,
colloidal and coarse dispersions can be distinguished
May require shaking before administration
According to the overall physical properties of dosage forms (both
homogenous and dispersion systems) one can distinguish
– Gaseous dosage forms
– Liquid dosage forms
– Semisolid dosage forms
– Solid dosage forms
7. Gases
– Gases – medicinal gases, inhalation/volatile anaesthetics (vaporised
before administration by inhalation)
– Aerodispersions of solid particles (e.g., inhalation antiasthmatics) or
liquid particles (inhalation antiasthmatics or sprays)
Liquids
– Solutions – one homogenous phase, prepared by dissolving one or
more solutes in a solvent
– Emulsions
a dispersion system consisting of two immiscible liquids
o/w or w/o
cloudy appearance
– Suspensions
A dispersion system where solid particles are dispersed in liquid phase
Not intended for systemic administration of drugs with high potency
Classification of pharmaceutical dosage
forms according to its physical properties
o
w
8. Volume/weight for estimation of dose of
liquid dosage forms
Dosing measure
Aprox. volume
(ml)
Aprox. weight
(g)
1 drop 0,05 0,05
1 teaspoonful 5 5
1 tablespoonful 15 15
20 drops of aqueous solution 1 1
60 drops of ethanolic solution 1,25 1
9. Classification of pharmaceutical dosage
forms according to its physical properties
Semisolid dosage forms
– Unshaped (without specific physical shape)
Gels -A semisolid systems in which a liquid phase is constrained within a 3D cross-
linked matrix.
Creams – semisolid emulsion systems (o/w, w/o) containing more than 10% of
water.
– o/w creams - more comfortable and cosmetically acceptable as they are less greasy and
more easily water washable
– w/o creams – accommodate and release better lipophilic API, moisturizing, Cold creams
Ointments – semisolid dosage forms with the oleaginous (hydrocarbon), water-
soluble or emulsifying base
– Oleaginous (hydrocabon) base: Petrolatum (Vaseline – white, yellow)
– Water-soluble base: Polyethylenglycol (PEG)- ointment – syn. macrogol ointments
Pastes – semisolid dispersion system, where a solid particles (> 25%, e.g. ZnO)
are dispersed in ointments – mostly oleaginous (Petrolatum)
– Shaped
Suppositories (for rectal administration)
– different shapes
– Melting/dissolving at body temperature
– Oleaginous (cacao butter, adeps neutralis) or aqueous (PEGs, glycerinated gelatine)
Pessaries (vaginal suppositories)
– Similar as above, PEGs or glycerinated gelatine are often used as base.
10. Solid dosage forms
– Unshaped (without specific shape)
- powders for external/internal use
– Shaped
- Tablets
- Capsules
- Implantates
- Transdermal patches…
Classification of pharmaceutical dosage
forms according to its physical properties
11. Dosage forms
– for systemic administration
p.o.
s.l. and buc.
rectal
parenteral
transdermal
inhalation
– for local administration
Topical (on the skin or mucosa)
– Into/onto - the eye, nose, ear
- the oral cavity
- the vagina, rectum
- the brochi
- the skin
Local parenteral (viz Parenteral above)
Classification of pharmaceutical dosage forms
according to the route of administration
12. Pharmaceutical dosage forms
for systemic administration
Generations of dosage forms
– 1st gen. – conventional (unmodified) release of API
– 2nd gen. – controlled release of API (CR)
– 3rd gen. – targeted distribution drug delivery systems
13. Conventional vs. controlled release
dosage forms
I. Gen. – disintegration ( desegregation) of the dosage form and dissolution
of API is spontaneous process;
– drug absorption and distribution is based only on physico-chemical properties of
API
II. Gen. The release of API is under control of the drug delivery system
(temporal control)
– Advantages:
Avoids fluctuations of plasma drug concentration better safety and efficacy
Decreased frequency of drug administration (often once daily admin) better
compliance
May overcome some problems with BAV
Can be much more economical (better cost-effectiveness)
– Sustained release (SR) – release of the initial API dose & further prolonged
release
– Controlled release (CR) – properly controlled (0. order) release of API
– Pulsatile release
14. Targeted drug delivery
The PK of the drug is not primarly determined by the physico-chemical properties of the API
Drug delivery system provides altered PK profile - namely the targeted distribution of the
drug to the particular organ/tissue (spatial control of the drug delivery)
– Improved selectivity of action (especially important where pharmacodynamic selectivity is poor)
– Can overcome unfavourable PK properties (rapid metabolic biotransformation or elimination)
– Improved efficacy
– Improved tolerability/decreased toxicity
Passive targeting
- The enhanced permeability and retention (EPR) concept
Passive accumulation of the drug at the site of pathology due to the leaky vasculature and poor
venous/lymphatic drainage – solid tumours (fenestrations as large as 800nm while in most of
normal tissues they are 60 nm) !!! (potentially also tissues suffering from inflammation or
ischemia)
Drug delivery systems within nanometre range ( 100 nm)
– A need to prevent opsonization and RES clearence (surface of hydrophilic nature) otherwise once can have monocyte-
phagocyte targeted drug delivery
– How to exploit the concept of passive targeting?
Conjugation of the API with a macromolecule (a drug is bound to biomacromolecules or
synthetic polymers via biodegradable linker)
Liposomal encapsulation – PEGylated (stealth liposomes)
Other nanoparticles
Active targeting
– Drug delivery system (liposomes, drug-polymer conjugates) with a specific ligand (Ab, Fab, peptide,
protein, hormone) with high affinity to the receptor exposed selectively on the target cells (e.g.,
cancer cells)
16. Dosage forms for systemic administration
– ORAL (p.o.) solid dosage forms
Tablets - Compressed product (API+ excipients – e.g., fillers, desintegrants)
– Conventional – Desintegration/Desagregation/Dissolution, can be divided (half/quarters)
– Coated (not to be divided)
To mask unpleasant taste or smell of API
To avoid of adhesion in oesophagus (to facilitate swallowing and/or avoid release of API
and local adverse reactions)
To ensure drug stability
To provide enterosolvent coating
– To overcome – possible degradation of API in the stomach and possible local
irritation/adverse reactions in the stomach
Effervescent tablets – not a final dosage form (drug is administered as the solution), CO2
produced by chemical reaction of acid and NaHCO3. Hygroscopic!!!
– Rapid absorption rapid on-set of action
– Avoids potential tablet adhesion to mucosa and local irritation
!!! Besides tablets for p.o. there are also special tablets for s.l. a bucc.; however, these
are different and presents different route of administration!!!
Capsules (not to be divided, can also be compounded individually)
- API + excipients - enclosed in the hard/soft water soluble container made of gelatin.
- Consist of cap and body – filled with powders, pellets, granules (paste, oil)
- In the GIT gelatin shell softens, swells and dissolve – particles are dispersed disintegration
API dissolution absorption
- Hygroscopic
- Enteric coating available
17. CR (SR) tablets and capsules
Reservoir type (not to be divided)
– Core consisting of API and excipients is encapsulated by
wall/membrane determining the rate of release
– Mechanisms of release
Dissolution of the outer/inner layer
Diffusion (permeation) throughout membrane pores
Osmosis (OROS system)
Matrix type (tablets)
– Drug is dispersed within the polymer
Polymer matrix can be biodegradable – drug is released
continuously
Polymer matrix can form pore – drug can gradually diffuse
18. Dosage forms for systemic administration
– ORAL (p.o.) liquid dosage forms
Solutions (drops) – aqueous, oils
– Syrups – aqueous sol. with sugar (or sugar substitute) with/without flavouring
agents
– Elixirs – sweetened hydroalcoholic sol., can accomodate less watter sol. API
– Tinctures – alcoholic or hydroalcoholic sol. – herbal extracts…
Emulsions
Suspension – should not be used for drugs with high potency (dosing!)
• Advantages: easier for administration (children, elderly people), good
compliance (can be flavoured), rapid absorption, flexible dosing
• Disadvantages: stability (chemical, microbial… - a need for preservatives),
accurate dosing???
A note: Two liquid drug preparations need not be automatically bioequivalent
Common API classes: antibiotics, analgesics (spasmoangesics), NSAIDs, antipyretics,
antitussive agents, expectorants, vitamins…
19. Rectal suppositories
– Solid dosage form under r.t., which are melted at the body temperature
– Different size – children and adult supp. !!!
– Suppository basis (i.e., basic excipients) – oleum cacao, adeps neutralis,
glycerogelatine – melting point, non-irritating, chem. stable and inert
– Different shape – mostly „torpedo“-like, formed by mould casting
– Both manufactured and compounded
– Solid suppository is melted within the ampula recti, API is dissolved and is
absorbed
It can gets into the systemic circulation (Middle & inferior haemorrhoidal veins Iliac vein
inferior vena cava – bypassing liver there is no first pass effect)
It can pass through portal circulation: via Superior haemorrhoidal veins Inferior
mesenteric vein Hepatic portal Liver (First Pass effect can take place). It
becomes to be more important when supp. is position too high in rectum.
• Advantages: offers an alternative to p.o. – especially useful when patient can not swallow
the drug (unconsciousness, vomiting patents, serious GIT disturbances. Children) or when
we need to avoid local adverse reactions (e.g., NSAIDs).
• Disadvantages: poor compliance, some API can cause local irritation of rectal mucosa,
stability of the dosage form during high temp., the melted supp. matter may come out
– Storage: cool place!
Other rectal dosage forms for systemic administration: rectal tablets, capsules
Common API classes: opioid analgesics, NSAIDS, antipyretics (paracetamol), antiemetics
(thiethylperazine)
Dosage forms for systemic administration
rectal route dosage forms
20. How to use suppositories?
1. Wash your hands.
2. Remove a suppository from the packet (foil or plastic wrapping ).
3. Moisten the suppository with water or water-based lubricating gelly.
4. Lie on your side with one leg bent and the other straight.
5. With your finger, gently insert the suppository into the rectum
pointed end first
6. Lower your legs and lie (or sit) still for a few minutes.
7. Wash your hands again.
8. Try not to empty your bowels for at least an hour, unless the
suppository is a laxative.
21. Dosage forms for systemic administration
Parenteral route dosage forms
Injectables – dosage forms which are intended to for administration using a hypodermic
(hollow pointed) needle (1853 by Dr. A wood). Can be formulated as liquids or powders/lyophilisate
for preparation of the solution (stability issues, follow the instructions given by manufacturer!!!)
– Injections (available as ampoules, vials with rubber head)
Solutions, emulsions or suspensions which MUST BE
–STERILE – free of microorganisms (microbiological tests)
–PYROGEN-FREE (test for pyrogens)
–ISOTONIC (NaCl usually as the additive)
I.V. injections
–Must be PARTICLE-FREE (visual inspection prior administration!)
–Not intended for API inducing clotting or haemolysis
–Isoacidity is desirable – but different pH often needed to assure solubility of API or
chemical stability (may cause local reaction – phlebitis or pain at the site of injection)
–Moderately irritating compounds can be administered (e.g., anticancer drugs)
–Vehicle – sterile water for injections, co-solvents may be added (ethanol, PEG 300/400,
propylenglycol, Cremophor) to solubilize poorly soluble API
–Slow administration to avoid problems with „concentration wave“
I.M. and S.C.
–Isoacidity should be guaranteed (to avoid risk of inflammation/necrosis of the tissues)
–API and excipients should be non-irritating
–Suspension/emulsion injectables can be administered (depot forms), oil-based vehicles
may be used
–The volume administered depends on site of administration (e.g., up to 5 ml i.m.)
22. – Infusions (avialable in plastic bags)
I.v. and s.c. route (the demands are as above)
Higher volumes over much larger times (from min to days)
Infusion pump, tubing and flexible canule is needed!
Advantages
– It can be a approach of choice in the case of
Problems with oral absorption (poor/erratic)
Problems with stability of API in GIT (pH, enzymes)
Uncooperative patients (unconsciousness, vomiting…)
Urgent need for rapid onset of action (emergencies)
Disadvantages
Non-compliance (phobias, children..)
Pain/irritation at the site of injection
– accidental extravasation of some drugs (number of anticancer drugs) may cause
serious problems – tissue inflammation, necrosis…
Certain degree of heamolysis may occur
Need for trained personnel using aseptic procedures (problems with chronic treatment
of outpatients – s.c. route may be usable)
Higher risk of adverse severe adverse reactions (inc. hypersensitivity on excipients)
Parenterals for local use – similar demands as given above)
Dosage forms for systemic administration
Parenteral route dosage forms
23. Implants
– Controlled drug delivery for over a long time (months/years)
– Principle
Reservoir (Osmotic/diffusion) systems
Matrix systems
– Non-biodegradable
– Biodegrable polymeric materials with dispersed drug
• Advantages – largely overcomes problems with individual
compliance
• Disadvantages – mini-surgery is needed, uneasy to simply
discontinue the therapy, local reactions
– Examples: hormones/contraception
Dosage forms for systemic administration
Parenteral route dosage forms
24. Dosage forms for systemic administration
Transdermal drug delivery sytems (TDDS)
TDDS (transdermal patches) are designed for affixing on healthily
and clean skin in order to assure controlled drug delivery into the
systemic circulation
Barrier function of the skin (particularly stratum corneum)!!!
TDDS
– Reservoir/membrane systems
– Matrix systems
– New „micro-invasive“ systems – microneedle arrays
25. Dosage forms for systemic administration
Transdermal drug delivery sytems (TDDS)
Advantages
– Elegant alternative to injectables
Pain and stress-free
No need for trained specialist
Long-term drug delivery with minimal fluctuations of drug concentrations
– Good compliance
– Unlike other controlled drug delivery systems, the delivery of the API can be
immediately discontinued (e.g., upon occurrence of adverse reactions…)
Disadvantages
– Not feasible for all API !
Mr < 500
Well balanced lipohilicity
High potency (high doses can not be accommodated and delivered)
Penetration enhancers can help!
– Local relations (irritation, disruption of barrier skin function)
– Need not be practical/comfortable
– Need not be cost-effective
Examples of clinical use: hormones (HRT, contraceptives), opioid analgesics (e.g.,
fentanyl), nitroglycerine, nicotine (RT), clonidine or scopolamine
26. Dosage forms for local drug administration
Into/onto
– the eye, nose, ear
– the oral cavity
– the vagina, rectum
– the brochi
– the skin/hairs
27. Dosage forms for local drug administration
into the eye Eye liquid dosage forms
– Drops (smaller volumes, 10-20 ml) and Lotions (up to 100 ml)
Can be both manufactured and compounded (however, higher tech. demands!)
Must be
– Sterile (sterile ingredients/preparation) – proper handling, storage and
administration to avoid contamination
Often deserves to employ antimicrobial agent (may be a source of allergy)
– Isotonic with tears (to avoid eye irritation due to the hypotonic preparations)
– Vehicle – sterile water (oil)
Advantages: high local concentration, lower systemic adverse reactions, minor effects
on vision
Disadvantages: local hypersensitivity, rapid tear eash-out!
Eye semisolid drug formulation
– Gels, creams and ointments
MUST also be sterile and clear (partuculate free)
Direct application into the conjuctiva to avoid contamination (do not use
fingers)
Advantages: API exposure is longer!
Disadvantages: can hinder vision (useful for overnight treatment), dosage accuracy
Eye solid drug formulations
– Eye inserts (soluble, insoluble, biodegradable) – slow release of API
Examples: antiglaucoma drugs (pilocarpin, timolol), antimicrobial agents, vasoconstriction
agents and antihistamines, mydriatics/myotics
28. Nasal/ear drops and prays
– Usually isotonic
– Vehicles and API must be non-irritating
– Vehicle – isotonic aqueous solutions/oils
– Technique of (self)-administration
May require special dropping device
When kept under lower temp. It should be warmed in hands (ear)
Nasal/ear semisolid dosage forms - gels, creams and ointments
– More complicated administration into the ear
Example
– Nose – decongestants, antihistamines, antiinflamatory, antiseptic
agents and ATB
– Ear: atb
Dosage forms for local drug administration
into the nose/ear
29. Dosage forms for local drug administration
into the vagina/rectum
Vaginal dosage forms
– Tablets
Compressed products disintegrating in vagina (may also form foam)
Markedly different appearance to oral ones
Application devices
– Capsules
– Pessars (vaginal suppositories) – hydrophilic bases are more frequent (more
comfortable)
Both manufactured and compounded
– Vaginal foams
Examples: namely antimicrobial agents (antibacterial, antimycotic, antiprotozoal)
Rectal dosage forms
– Suppositories (as given previously for systemic administration)
– Gels and creams
– Enemas
Examples: antihemeroidal drugs (also inc. local anaesthetics), antiseptics and
laxatives
30. Dosage forms for local drug administration
onto the skin/hairs
Aerodispersion (macro) - sprays
Aquous dosage forms – lotions, medicated shampoo, foam
Semisolid dosage forms
– Gels
– Creams
– Ointments
Used as:
emollients
for skin hydration
to form a protective barrier
as a vehicle for incorporation of API
Solid dosage forms
– Dusting powder (starch and talc as a vehicle)
Example: atb (e.g., neomycine + bacitracine)