Introduction to DoSAge fOrmS

Dosage Forms (Part 2)

Siti Halimah Bux
Pharmacy Practice Department
Kulliyyah of Pharmacy, IIUM Kuantan.
Dosage Form - Design

Three (3) major considerations:
Physical and chemical properties of the drug
Biopharmaceutical aspect - route of
administration
- rate of absorption
- extent of absorption
Therapeutic Aspect (performance of the drug)
- bioavailability of the drug
1.Physical & Chemical Properties Of
The Drug
Stability
some drugs are not stable in solution form or are inactive when
hydrolysed e.g certain antibiotics
Drugs stable in solution need to consider stability under various pH
conditions, temperature etc.
Compatibility
whether compatible with other ingredients in the formula.
Solubility
Most drugs relatively soluble in aqueous soln. for it to be absorbed.
Depends on pH
Particle size
The smaller the size, the larger is the surface area, the better is the
absorption
2. Biopharmaceutical Aspect
-Route of Administration
Oral
Parenteral
Rectal / Vaginal
Respiratoral
Topical


Dosage Form Design 1
Tablets/Capsules
Delayed action and enteric coated
tablets
Designed to delay the release of drug in the stomach
so that:
- it would not be destroyed by gastric juices
- the stomach lining will be protected by irritating
effect of the drug
- promote absorption (for drug which is better
absorbed in the intestine)
Sugar-coated (dragee), film-coated and
chewable tablets
Designed to:
- protect the drug from air and humidity
- mask the drugs unpleasant taste or odour
- improve the drugs appearance
Sublingual tablets / capsules
Designed to:
- increase absorption bioavailability increase
- prevent drug from being destroyed by gastric juices


Dosage Form Design 2 Injectables /
Parenteral Preparations
Major Routes of Parenteral Administration:
1. I ntradermal Injection into skin between the
dermis and epidermis, mainly for diagnosis of
allergy and immunity e.g. Penicillin test dose
2. Subcutaneous Injection into tissue immediately
under the dermis e.g insulin inj.
3. I ntramuscular Injection into skeletal muscle,
usually deltoid muscles in shoulder or gluteal
muscles in the buttock
Injectables / Parenteral
Preparations
1. I ntravenous Injection directly into superficial
vein
2. I ntra-arterial Injection- directly into an artery,
usually for diagnostic procedure e.g. x-ray contrast
3. I ntraspinal Injection- into the intrathecal or
intracisternal e.g. spinal anaesthetics
4. I ntra-articular Injection- directly into synovial
fluid of a joint

Dosage Form Design 3 Suppositories
& Pessaries
Route of Administration : Rectal or Vaginal,
occasionally urethera
Used when normal routes are not suitable (when
drug is destroyed in the GIT, irritant to the stomach)
or inaccessible (when patient is unconscious or
vomitting)
To produce a local action e.g. haemorrhoid
preparations; laxative preparations
To produce a systemic effect e.g. paracetamol
suppositories for fever
Dosage Form Design 4 Respiratoral
Preparations (Inhalers)
Three types of inhalers available in Malaysia:
* Pressurised aerosol inhalers ( metered dose
inhaler) small, portable devices that deliver
medication in an aerosol form so it can be inhaled
* Dry powder inhalers dry micronised powders
inhaled directly into the lung
* Nebulizers - Respirator solutions are placed in a
chamber and the nebulizer produces a mist. This
mist is delivered to the patient via a mouth-piece or
face mask.
Dosage Form Design 5 Topical
Preparations
Creams semi-solid preparation used either for
therapeutic or prophylactic purposes; due to their
high water content it provides a moisturising effect
on dry skin.
Ointments greasy, semi-solid; act as protective
agent and has emollient ( soothing) effect
Lotions used for its cooling and soothing effect
Transdermal patches e.g. nicotine and
nitroglycerine patches. When supplements/drugs are
delivered transdermally they go directly to the blood
stream initially bypassing the liver (95% get to the
cells where needed)
I mplants may be inserted into various parts
of the body :
* to replace a diseased structure
* to improve appearance
* to maintain proper functioning of an internal
organ
* to treat certain disorders
* to deliver drugs or hormones
Other Dosage Form Designs
Radiopharmaceuticals
A radiopharmaceutical is a radioactive agent i.e. it
incorporates a radioactive isotope. They are used for:
a) Diagnostic purposes whereby the radioactive
agent is taken up by an organ of the body. The
radioactivity is detected and pictures are produced
by special imaging equipment.
b) Treatment of certain diseases e.g. cancer whereby
the radioactive agent is taken up in the cancerous
area and destroys the affected tissue
Enemas are aqueous oily solutions that are
introduced into the rectum for:
* cleansing e.g. removing faeces in constipation
* therapeutic effect e.g. it may contain an anti-
inflammatory drug which exerts a local effect in the
large bowel
* diagnostic purposes e.g. x-ray contrast media
administered as an enema to aid diagnostic
investigation of the large bowels
3. Therapeutic Aspect
Nature of the disease
- what is the most suitable dosage form
- which is the best route for administration
- what is the desired duration of action
- dose frequency

Age of the Patient child or adult
WORDS OF WISDOM
REMEMBER THE 3 Rs