practical part Pharmacology

University Of Fallujah
College Of Medicine

Lecture : drugs formulation part I

Stage : 3rd stage
Lecturer : Dr . Aula H .Obaid
Department: Pharmacology
Date: 25-9-2024
DRUG FORMULATIONS
What factors determine the dosage form?
1- Physicochemical Properties of the Drug

2- Route of Administration

3- Patient Factors

4- Desired Onset and Duration of Action

5- Target Site of Action

6- Economic and Manufacturing Considerations

 ENTERAL [ORAL] DRUG FORMULATIONS: I

I-SOLID FORMULATIONS
A- Tablets
Tablets are solid dosage forms in which the drug is compressed
with pharmacologically inert substances called Excipients . Tablets
are circular in shape with flat or convex surface, and film coated to
improve their appearance and stability and to mask unpleasant taste.
Advantages of tablet form:
- Precision of dosage
- Durability of physical characteristics
- Stability of chemical and physical activity
of drugs
- Convenience of administration.
 Tablets for oral use:
(a) Uncoated tablets (b) Coated tablets
(a) Uncoated tablets: Compressed powder, which may have flavoring or
coloring agents.
Sublingual or buccal tablets: Dissolved in buccal pouch or beneath the
tongue. e. g. nitroglycerine, nifedipine, methyl testosterone, clonidine.
Advantages : - Drug does not get destroyed in stomach.
- Poor absorption from stomach can be overcome.
- Liver can be bypassed and quick onset of action.
Disadvantages:- Can produce ulcers in mouth and other systemic
adverse effects.
- One has to spit the drug after the desired effect is achieved, to avoid side
effects.
 Chewable tablets: When chewed it disintegrates due to its creamy base. e. g.
Antacid tablets, Anthelmintic tablets & Vitamin C tablets.

Advantages : It is useful to children who have difficulty in swallowing and to

the adults who dislike swallowing.

Disadvantages: Compared to compressed tablet it is expensive.

Note :
Correct instruction for
effective use of this dosage form:
The tablet is to be broken and chewed
before swallowing. To be swallowed
with a glass of water with the patient
in upright posture either sitting or standing.
 Effervescent tablets: Prepared by compressing granular effervescent salts.
Advantages : It disintegrates fast when added to water and acts by releasing
carbon dioxide.
Effervescence masks the bad taste of drug. It may give psychological effect to
patient. e.g. alkaline tablet, antacid tablet, aspirin tablet.
Disadvantages : Very sensitive to moisture.
Expensive as compared to compressed simple tablets

Dispersible tablets: These are dispersible tablets, which are to be dissolved in

water prior to administration e.g. Amoxicillin dispersible tablet.
Advantages: They get easily dispersed in water and are sweet
in taste so especially used for pediatric patients.
Disadvantages: Cost is high.
Lozenges: These are disc shaped solid dosage forms. e.g. menthol,
dextromethorphan.
Advantages: Local action in oral cavity.
Slow and continuous effect of the drug on the mucous membrane of the
throat.
Disadvantages: cost is high.
Correct instruction for effective use of this dosage form:
Suck the lozenges. Do not chew.

Coated tablets:
Sugar coated tablets:
Advantages:Tablet is covered with colored / uncolored sugars so it masks the
bad taste of drug e.g. Chloroquine tablet.
Disadvantages: Action is slow and tardy so it is not suitable for emergency
Can not be used for unconscious/non co-operative patients
‫ة‬
 Enteric Coated tablet:
Advantages: Enteric coating resists dissolution in the stomach but not in the
intestine, is useful for drugs which are destroyed by gastric juice or are irritant
to gastric mucosa (e.g. Enteric coated aspirin and dipyridamole (antiplatelet
agents), sodium valproate)
Disadvantages:- If the coating is very hard, a tablet may pass out without
being dissolved in the gastrointestinal tract & may fail to produce the
therapeutic effect.
- Compared to uncoated tablet it is expensive.

Time released tablets :

Advantages :Maintain a steady plasma level of the drug so sustained

action of it is produced. (e.g. nifedipine, theophylline, indomethacin)

Disadvantages: If the coating is very hard, a tablet may pass out without being
dissolved in the gastrointestinal tract & may fail to produce the therapeutic
effect.
 Sustained release (controlled release/retard) tablets: Small granules of
drugs are coated with a film and compressed in a form of tablet e. g. isoxsuprine retard,
diclofenac sodium SR.
Advantages: It modifies the rate of release of drug into the gastro-intestinal tract.
It prolongs the effect of drug and also reduces the frequency of
administration.
Patient compliance is better.
Disadvantages: It is expensive as compared to uncoated tablets.

B- Capsules for oral use: They have shells of gelatin for administration of powder;
granules or liquid.Two types – hard and soft. Hard capsule consists of 2 cylinders which fit into
one another e.g. amoxicillin. Soft capsule is made of gelatin which is sealed by heat and mainly
contains a liquid e.g. nifedipine. Pearls are transparent or translucent capsules that contain liquid
or semisolid drugs e.g. Vitamin A & D.

Advantages: Masks the bad smell and taste of drugs.

Avoids destruction by gastric juice and avoids gastric irritation.
Disadvantages: More expensive than tablets.
‫ى‬
 Micro-encapsulation (sustained release)
Process of applying thin coatings to small particles of solids or droplets of
liquids. This provides the means of converting liquids into solids.

C -Powders for oral use: Powder is a solid form of drugs, which is

finely divided and intimately mixed. They are mainly of three types.
(i)Simple powders: contain one ingredient only e. g. glucose powder
.(ii)Compound powders: contain more than one ingredients e.g. O.R.S.
(iii)Effervescent powder – Antacid effervescent powder.

Advantages : They are flexible in compounding.

Powders have a good chemical stability.
Disadvantages: Needs proper instruction for preparing.
Time consuming to prepare.
It is not suitable for dispensing bitter drugs.
 Granules for oral use: Powder in the form of small granules
e.g. calcitriol.
Advantages: They are flexible in compounding.
They have a good chemical stability.

Disadvantages:
- More expensive than powders.
- Needs proper instruction
for preparing.
-Time consuming to prepare.
- It is not suitable for dispensing
bitter drugs.
II-LIQUID FOR ORAL USE
Liquids for oral use are usually dispensed in plastic or glass bottles.
Advantages of liquid preparations:
-Suitable for patients who cannot swallow solid forms
-They are more quickly acting than pills or tablets, which require previous
disintegration before absorption.
-Certain substances can only be given in the liquid form e.g. liquid paraffin.
-Certain chemical substances e.g. potassium chloride can cause gastric irritation if
taken in the form of powder or tablet.
-Patients are sometimes prone to doubt the efficacy of the treatment they are
receiving unless it includes something in the bottle (e.g. placebo effect).
-Usefulness of some substances are largely dependent upon administration of
diffussible form e.g. magnesium sulphate in the form of suspension.
 Solution
One or more soluble ingredients dissolved in water, intended for external or
internal use.
Syrups: They are liquid oral preparations in which the vehicle is concentrated
aqueous solution of sucrose or other sugar.
Advantages: They are sweet in taste so masking the bad taste of drugs,
especially suitable for children.
Quicker effect than tablets which require previous disintegration.
Disadvantages: Maintenance not easy.
They are costlier than tablets.
Elixir: They are clear pleasantly flavored liquid oral preparations containing
hydroalcoholic vehicle. e.g. bromhexine, promethazine, sugar, or glycerol.

Advantages: Potent or nauseous drugs are pleasantly flavored and usually

attractively coloured so patient compliance is better.
Disadvantages: Maintenance not easy.
They are costlier than tablets.
 Suspension: Fine solid particles of a drug suspended in aqueous solution. It is a liquid
medicament containing insoluble (diffusible or indiffusible) solid substances which are
homogeneously distributed throughout the vehicle with or without the help of a suspending
agent.
Advantages: They are chemically more stable than the syrup.
Mask the unpleasant taste and odor of the drugs.
Insoluble solids can be given in liquid form.
Disadvantages: A suitable preservative is required to avoid microbial contamination

Emulsions: They are liquid medicaments containing two immiscible liquids ‫غ ق ام‬, one of
which is broken into minute globules, each globule being surrounded by a thin film of
emulsifying agent and then dispersed throughout the other liquid. e. g. liquid paraffin emulsion.
Advantages: Oily drugs can be given in this form
Oil in finely dispersed state is quickly absorbed.
Emulsifying agents mask the unpleasant taste and smell of the drugs.
Disadvantages: A suitable preservative is required to avoid microbial contamination.
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 Drops: They are liquid medicines for pediatric use, dispensed in
dropper bottle e.g. multivitamin drops, iron drops.
Advantages: Accurate dose can be given.
The dose of the drug in small amounts can be easily
administered in infants and children.
Disadvantages: Cost is high.
--Correct instruction for effective use of this dosage form:
Prescribed amount of drops to be given by dropper.

Tincture
Alcoholic liquid containing (in a low concentration) the active
ingredient of the crude drug, e.g. tincture of iodine.
Gel/ Semi-solid aqueous preparation prepared with the aid of gelatin.
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