Dosage Formulation of Drugs

Dr. A. Hossain
MBBS, BCS, MPhil (Pharmacology)
Lecturer
Faridpur Medical College
TYPES OF DOSAGE FORMS
 Dosage forms
Definition: Dosage forms are the means by
which drug molecules are delivered to sites of
action within the body.
Medicine
• Excipients (inactive pharmaceutical
ingredients): Excipients are pharmacologicaly
inactive substansces which are mixed with the
active ingredient.
• These are manitol, sodium sacchrin, starch
paste, peppermint oil, magnesium stearate,
corn starch, methylcellulose, orange.
Why excipients are used?
• To make a stable, acceptable and convenient
form.
• To make helpful to administer to patient.
 Excipients
Excipients (inactive pharmaceutical ingredients)
• Diluents
• Binders
• Lubricants
• Disintegrants
• Coatings
• Preservants and stabilizers
• Colorants and flavourings.
 The need for dosage forms:
1. Accurate dose.
2. Protection e.g. coated tablets, sealed ampules.
3. Protection from gastric juice.
4. Masking taste and odour.
5. Placement of drugs within body tissues.
6. Sustained release medication.
7. Controlled release medication.
8. Optimal drug action.
9. Insertion of drugs into body cavities (rectal,
vaginal)
10. Use of desired vehicle for insoluble drugs.
 Why so many dosage forms?
1. A single formulation does not allow us to
administer a drug via different routes.
2. API handling can be difficult or impossible
(e.g. low mg or µg).
3. It conceals the bitter, salty, or offensive taste
or odor of drug.
4. The damage of drug from moisture can be
prevented (film-coated tablet).
5. It protects the drug from the destructive
influence of gastric acid (Benzyl penicillin).
6. The adverse effects are reduced (enteric
coated tablet).
7. Increase patient compliance (time-controlled
drug, masking the better taste by film coating,
).
Types of dosage formulation
Solid dosage form:
1. Tablet
2. Capsule
3. Powder
4. Granule
5. Modified released dosage forms
(tablet/capsule)
6. Lozenges (torches)
Semisolid dosage forms
1. Creams
2. Ointments
3. Pastes – e.g. ZnO.
4. Gel/jelly
5. Suppository
6. Transdermal drug delivery system
• Liquid dosage form:
Non Sterile liquid Sterile liquid
1. Solution 1. Injectable
2. Suspension 2. Intravenous bolus dosage form
3. Syrup 3. Eye/otic drops
4. Linctus
• Gaseous dosage form:
1. Aerosol
2. Gas
3. Volatile liquid.
 Tablet
➢ Tablet is a solid dosage form in which powder,
crystalline, or granular form of drug is
compressed in a disk or molded.
➢ A tablet is a hard, compressed medication in
round, oval or square shape.
 Tablet

For systemic effect: Local effects:

Tablet Antacid, Anthelmintics

Released in GIT

Absorption into circulation.

Tablet is usually swallowed with a cup of water (about

250 ml).
 Caplets- Tablets
• Coated tablets in the shape of a capsule.
• Easier to swallow.
 Types of tablet:
Uncoated tablet- Coated tablet-
1. Chewable tablet - Antacid 1. Enteric-coated tablet - Aspirin
2. Effervescent tablet - Aspirin 2. Film- coated tablet -
3. Lozenge tablet - Nystatin Ciprofloxacin
4. Sublingual tablet - Nitroglycerine 3. Suger- coated tablet

Modified- release tablet- Aminophylline, diclofenac.

• Controlled-release
• sustained-release
• time- release
• slow-release
• sustained-action
• prolonged- action.
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.
Enteric-coated tablet:
Advantages of enteric-coated tablet:
• Prevent destruction of API by gastric juice.
• Prevent irritation of gastric mucosa by API.
Broken or crushed form of the enteric-coated
tablet causes destruction of drug by gastric
juice or irritation to the stomach.
 Chewable tablet
• The tablet – disintegrate smoothly in the
mouth.
• Pleasant taste.
• E.g. Antacid, Albendazole, vitamin tablet.
 Effervescent tablet:
• The tablet contains acid substance and
carbonate or hydrogen carbonate.
• Sodium bicarbonate, citric acid, tartaric acid –
make the tablet effervescent.
• In presence of water – release carbondioxide.
causing effervescence (BUBBLING)
• E.g. Aspirin.
 Lozenge tablet:
• Consisting of sugar and gum.
• Gum giving strength and cohesiveness to the
lozenge and facilitating slow release of the
active ingredient.
• There is no disintegrating agent.
• E.g. nystatin, benzocaine.
 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 ------- absorbed
through the mucous membranes of the mouth ------
enter into the bloodstream.
➢ Avoid --- i) acid and enzymatic environment of the
stomach.
ii) the drug metabolizing enzymes of the liver.
➢ Examples of drugs administered by this route: e.g.
vasodilators (nitroglycerin).
Film-coated tablet:
• E.g. metronidazole.
Modified-released tablet:
• It is either uncoated or coated.
• A modified-release tablet contains greater
amount of drug than a conventional form. E.g.
diclofenac tablet, the conventional form
contains 50 mg whereas the modified-release
tablet contains 100 mg.
 Capsule:
A capsule is a medication in a gelatin container.
➢ Advantage: overcomes the problem of
disintegration, stability, taste.
The two main types of capsules are:
1. hard-shelled capsules.
2. soft-shelled capsules – Vitamin A, vitamin E.
Hard gelatin capsule Soft gelatin capsule
 Tablets & Capsule:

Sustained-release tablet / Capsule:

➢ For continuous release of small doses of the
drug over an extended time period to increase
duration of action.
➢ Decrease dosing frequency.
➢ Increase compliance.
 Suppository:

• Drug mixed with a fatty base and molded

into shapes suitable for insertion into the ----
rectum-- Analgesics, glycerin suppository
vagina
urethra.
➢ A urethral suppository is called a ---- bougie.
➢ A vaginal suppository is called a ----- pessary.
 Semisolid dosage forms:
• For local effects:
skin
eye
• systemic effect
transdermal application
(e.g. nitroglycerine)
 Semisolid dosage forms:
1.Ointments:
• Ointments are semi-solid, greasy preparations
for application to the skin.

• The base is usually anhydrous and immiscible

with skin secretions.

• Ointments may be used as emollients

2. Creams:

They are divided into two types:

A. oil-in-water (O/W) creams; more comfortable
and cosmetically acceptable as they are less
greasy and more easily water washable.
E.g. Saving cream, hand cream, foundation cream.
B. water-in-oil (W/O) creams: accommodate and
release better lipophilic API, moisturizing, Cold
creams.
 Transdermal patch:
• A transdermal 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.
• The first commercially available patch was
scopolamine for motion sickness.
• Clonidine (to control hypertension)
• nitroglycerine (for treatment and prevention
of angina).
 Liquid preparations
• Solution:
• Oral solutions are homogenous liquid
preparations for oral use containing one or
more active ingredients dissolved in a suitable
vehicle.
• E.g. antibiotic dry powder or granules are
prepared into solution by adding water.
• Suitable for use – 14 days when kept at 4º C.
• Suspension:
• A suspension is a heterogenous system of
liquid dosage form of drug in which the finely
divided solid particles ranging from 0.5 to 5.0
µm are suspended or dispersed in a liquid
vehicle.
• The suspension is chemically more stable than
the solution.
• Used for oral, external or parenteral use.
• E.g. antacids, cotrimoxazole.
• Syrup:
• It is a concentrated aqueous solution of a
sugar, usually sucrose.
• Flavored syrups are a convenient form of
masking disagreeable tastes.
• Linctuses:
• Linctuses are viscous, liquid oral preparations
that are usually prescribed for the relief of
cough.
• They usually contain a high proportion of
syrup and glycerol which have a demulcent
effect on the membranes of the throat.
• The dose volume is small (5ml) and, to
prolong the demulcent action, they should be
taken undiluted.
 Formulation/Dosage form:
• Tablet – necessary to disintegrate and
dissolution before absorption.
• Capsule – only dissolution is necessary.
• Suspension –no disintegration or dissolution is
necessary.
• The rate of absorption of drug is greater from
suspension than from capsule or tablet.
Gaseous dosage form:
• Aerosols:
Aerosols are particles dispersed in a gas, the
particles being small enough to remain in
suspension for a long time.
• Gas: Oxygen, Nitrous oxide, Carbon dioxide.
• Volatile liquid: Halothane, Eather,
Chloroform.