Oral Dosage Forms

Introduction
• The science of dosage forms and their design is known as
pharmaceutics.

• Dosage forms are the means by which drug molecules/APIs are

delivered to sites of action within the body to produce optimum desired
effects and minimum adverse effect.

• Dosage form (Medicines) = API + Excipients

• The Active Pharmaceutical Ingredient (API) is the part of any drug that
produces its effects.
Excipients:

• Do not increase or affect the therapeutic action of the active ingredient.

• Inactive ingredients may also be referred to as inert ingredients or

excipients, and generally have no pharmacological effect.

• Examples of inactive ingredients include binding materials, dyes,

preservatives, and flavoring agents, sweetening agents, coloring agents
etc.

• Serve as a vehicle or medium for the drug.

State the factors help in deciding the selection of
dosage form
1. Disease condition

2. Acceptability to the patient (compliance)

3. Suitability of administration
Advantages and limitations of oral drug delivery
Advantages:
• Simple & convenient to use
• Good patient compliance
• Accurate self dosing is possible
• Non invasive & painless
• No need of assistance or any equipment
• Constraints of sterility are minimal
• Usually economical
• Limitations
• Onset of action is slower & hence not suitable for emergencies
• Can’t be used for pts with diarrhoea/vomiting or in unconscious or
uncooperative pts
• Swallowing may be difficult for children
• Bioavailability is affected by a variety of factors
• Interindividual variation can be seen for controlled release
preparations
Solid dosage forms
• Tablet (dispersible, effervescent, chewable, film coated, enteric coated,
sustained release, sublingual)
• Capsule (hard & soft gelatin)
• Spansule
• Powder
• Granules
• Lozenges
• Chewing gum
• Liquid
Liquid dosage forms
• Solution
• Suspension
• Emulsion
• Syrup
• Linctus
• Elixir
• Tincture
• Spirit
• Aromatic water
• Extract
• Decoction
• Oxymel
Comparison solid and liquid oral dosage
forms
Solid Liquid

• Absorption is slower as it is dependent Absorption is faster as it is dependent

on both disintegration time and only on dissolution rate.
dissolution rate.
• Difficult to swallow • Easy to swallow
• Difficult to use in children • Preferred in children
• CR & enteric coated dosage forms • CR & enteric coated dosage forms
can be made cannot be made
Solid dosage forms
• Tablets
• A tablet is unit dose of one or more medicament.
• Prepared by compression or mould method.
• Common excipients used in tablet are :
• Diluents – Provide bulkiness of tablet.
• Disintegrants – To ensure that the tablet breaks up in the digestive tract.
• Binder – Important for granulation of powder.
• Glidants and Lubricants – Provide good flow and ensure efficient
tabletting.
• Sweeteners and Flavors – To mask the taste of APIs.
• Pigments – To mask uncoated tablets visually attractive.
• A coating may be applied to mask taste, smooth tablet for easy
swallow, expanding shelf life, and prevent gastric degradation of drug.
Sublingual tablets

• Sublingual tablets placing under the tongue.

• Medicaments rapidly dissolve in mouth and absorbed
through the mucous membrane of mouth.
• Drug reaches in systemic circulation without being affected by gastric
juices and metabolizing enzymes of the liver – bypasses first pass
metabolism
• Tablet can be spitted out when desired effect is achieved
• Example – Isosorbide mononitrate (anti-anginal medication)
Dispersible tablets
• Disintegrate completely within three minutes
• The rapid disintegration improves bioavailability.
• Intended to be dispersed in water before administration.
• Advantages:
• Commonly used in children & pts having difficulty in swallowing
• Rapid action is achieved
• Eg. Aspirin , Diclofenac
Effervescent tablets

• Effervescent tablets are uncoated and generally contain acid

substances (citric and tartaric acids) and carbonates or bicarbonates ,
which react rapidly in presence of water and release carbon dioxide.
• They are intended to be dissolved or dispersed in water before use, it
provide :
• Tablet immediately dissolve or dispersed
• Disadv . Need to be rigorously protected from moisture
• eg.-tablets of Zinc sulfate, Aspirin
Chewable Tablets
• These are intended to be chewed .
• They contain flavouring agents to leave a pleasant taste.
• They are good for children & patients who find swallowing difficult.
• Eg. Antacid preparations, Vit C, Albendazole
Enteric coated tablets
• Coating is applied to core tablet & designed to prevent disintegration in
the acidic environment of stomach.
• They disintegrate only when they reach the intestines (at alkaline pH)
• Eg. of enteric coating materials Cellulose acetate phthalate, Acrylic
resins.
• Adv.
1.When the active drug is acid lablile . Eg. Erythromycin,
Methenamine mandelate
2.When drug is irritant to gastric mucosa
Eg. Aspirin ,Diclofenac
3.When disintegration in the stomach is unnecessary
Eg. Bisacodyl
• Disadv. - Occasionally the coating may fail to dissolve adequately in
the intestine.
Film coated & Sugar coated tablets
• They are covered with a thin layer of water soluble polymeric substance
and sugar respectively.
• Adv. Such coating
1) protects the drug from atmospheric conditions
2) masks the unpleasant taste and odour of drug
3) gives attractive appearance
4) imparts mechanical strength to tablets
• Eg. Valsartan
• Diclofenac
• Ibuprofen
Controlled/Sustained/Extended release tablets
• These are formulated by special procedures to release the drug slowly
and uniformly over a prolonged period of time.
Adv.
1) Reduce frequency of administration and improves compliance
2) Can be beneficial for drugs having short half life.
3) Frequency or intensity of S/E may be reduced due to elimination of
sharp peak in plasma concentration
• Disadv:
• 1) Generally more costly
• 2) Show greater interpatient variation in bioavailability
• 3) Occasionally may fail to release adequately
• Eg. Aspirin, Theophylline
Capsules
• Capsules are solid unit dosage forms containing active medicaments
enclosed in a gelatin shell & intended to be swallowed whole.
• Advantages of capsules :
• Unpalatable drugs can be administered.
• Disintegration not required
• May be adapted for delayed or controlled release.
• Oily materials can be given in the form of soft gelatin capsules.
• Affords greater flexibility in combining drugs over tablets.
Oral capsules are of two types:
• 1)Hard Gelatin shell contains powders or granules
• 2) Soft Gelatin shell contains liquid (oily) drugs
Spansules
• They are controlled release capsules designed to provide slow and
steady release of drug.
• Coatings of different thicknesses are applied to active ingredients and
coloured differently.
• These coloured pellets are then packed in gelatin shell.
Eg.
• Ferrous Sulphate
• Prochlorperazine
Powders and Granules
Powders
• These are solid dosage forms in which the medicament is in the form
of finely divided solid particles
• Simple powder contains one active medicament & compound powder
contains multiple active medicaments.
• Eg. Oral Rehydration Salts, Sodium Bicarbonate powder
Granules
• These are small aggregates of powder held together by binding agent.
Eg. Vitamin D3 granules
Lozenges
• These are tablet like preparations containing active medicaments in
flavored base.
• Designed to dissolve slowly in the mouth while sucking.
• Eg. Vicks or Strepsils Lozenges (pharyngeal demulcents) commonly
used in cough and sore throat
Chewing gums
• Medicaments are incorporated in a gums like polymeric matrix from
which they are released slowly as the gum is chewed.
• Eg. Nicotine gum
Liquid oral dosage forms
Solution
• These are homogeneous liquid preparations containing one or more
ingredients dissolved in suitable solvents.
• Oral solutions are generally aqueous in nature.
Eg. Ondansetron oral solution,
• Theophylline oral Solution, Salicylate solution
Suspension
• Liquid preparations containing an insoluble solid dispersed in finely
divided particulate form throughout a liquid with or without help of
suspending agent.
Eg. Paracetamol oral suspension
• Convenient for administering poorly water soluble drugs.
• Solute settles down at the bottom on prolonged
standing thus importance of shake well before use
Emulsions
• Homogenous liquid preparations of two immiscible liquids one of which
is dispersed in finely divided droplets uniformly throughout the other
with the help of emulsifying agent.
• They are needed to shaken well before use.
• They are of two types
- water in oil type emulsions where the oily phase is continuous.
- oil in water type emulsions where the aqueous phase is continuous
• Eg. Liquid paraffin emulsion, Vit A emulsion
Syrups
• They are concentrated solutions of sugars in water .

• Syrup masks the unpleasant tastes of drug

• They need to be cautiously used in diabetics

Eg. Cough syrups, Vitamin Syrups

Linctus
• Liquid oral preparations containing demulcent (sub that relives
inflammation or irritaion like menthol and medication
• It is taken by licking in small doses without dilution
• Eg. Compound codeine linctus
Elixirs
• They are sweetened & flavoured hydroalcoholic liquid preparations ,
generally of potent & nauseating drugs.
• Alcohol content is not more than 20%
Eg. Potassium chloride elixir
Tinctures
They are alcoholic liquid preparations of non volatile substances (70-90%
of alcohol)
Eg. Opium tincture
Spirits
• They are alcoholic or hydroalcoholic solutions of volatile substances.
• They are used as flavouring agents,
Eg. Aromatic ammonia spirit
Aromatic waters
They are aqueous solutions of volatile substances or aromatic oils.
Used as vehicles for various oral preparations.
Eg. Peppermint water, Chloroform water.
Extracts
• They are concentrated preparations of vegetable or animal drugs
made by extracting the active constituents with suitable solvents. (Fluid
extract)
• Dry extract is prepared by evaporating the solvent of fluid extract.
Eg. Pituitary extract.
Decoctions
These are preparations of crude drugs made by boiling them in water.
Many herbal preparations are in decoction forms.
Oxymel
• These are liquid preparations containing a mixture of honey & acetic
acid as vehicle.
• They are similar to syrups except they contain honey, instead of sugar
syrup, as a base.