Introduction To Dosage Forms
Introduction To Dosage Forms
DEFINITION OF DRUG
A drug may be defined as an agent, intended for use in the diagnosis, mitigation,
treatment, cure or prevention of disease in man or in animals.
DOSAGE FORM
Drugs are rarely administered in their original pure state. They are converted into
suitable formulation which are called dosage forms. Every dosage form is a
combination of the drug and other non-drug components.
The non-dug components are known as “additives”. The additives are used to give
a particular shape to the formulation, to increase its stability and also to increase
its palatability as well as to give more elegance to the preparation.
Ans. Transformation of drug into different dosage forms is done for the following
reasons:
1. To protect the drug from oxidation (e.g. Vitamin C, Ferrous sulfate), hydrolysis
(aspirin) and reduction. e.g. coated tablets, sealed ampoules.
2. To protect the drug from destructive effect of gastric juice (HCl) of the stomach
after oral administration e.g. enteric coated tablets.
3. To provide a safe and convenient delivery of accurate dosage.
4. to conceal the bitter (e.g. chloramphenicol), salty or obnoxious taste or odour of a
drug substance e.g. capsules, coated tablets and flavoured syrups etc.
5. To provide for the optimum drug action through inhalation therapy. e.g.
inhalation aerosols and inhalants.
6. To provide for the drug into one of the body-cavities e.g. rectal suppositories.
7. To provide for the maximum drug action from topical administration sites. e.g.
creams, ointments, ophthalmic preparations and E.N>T. (ear, nose and throat)
preparation.
8. To provide sustained release action through controlled release mechanism. e.g
sustained release tablets, capsules and suspensions.
9. To provide liquid dosage form of the drugs soluble in a suitable vehicle e.g.
solutions.
CLASSIFICATION OF DOSAGE FORMS
DOSAGE FORM
Route of administration Dosage forms
Oral Powders, tablets, capsules, solutions, emulsions, syrups,
elixirs, magmas, gels, cachets, pills.
Parenteral Solutions, suspensions, emulsions.
Transdermal Ointments, creams, powders, pastes, lotions, plaster
Rectal Suppositories, tablets, ointments, creams, douches, foams.
Urethral suppositories
Sublingual Lozenges, tablets
Intranasal Solutions, sprays, inhalations.
Conjunctival Ointments
Intra-ocular Solutions
Intra-respiratory Aerosols
DOSAGE FORM
SOLID SEMISOLID LIQUID GAS MISCELLANEOUS
Cachets Creams Applications Aerosols Transdermal drug
Capsules Jellies Aromatic water inhalation delivery systems
Powders Ointments Collodion
Insufflations Pastes Draught Sustained release drug
Dentrifices Ophthalmic Ear drops delivery system
Effervescent ointments eye drops
granules Nasal drops Ophthalmic drug
Lozenges Elixirs delivery systems.
Pessaries Mixtures
Tablets Emulsions Implants
Suppositories Suspensions
Enemas
Gargles
Gels
injections
Irrigations
Linctuses
Liniments
Lotions
Mouthwashes
Spirits
Sprays
Syrups
Tinctures
Paints
CACHETS
Cachets consists of a dry powder enclosed in a shell. The shell is prepared from a
mixture of rice flour and water by moulding into suitable shape and then dried.
Two types of cachets are there:
(i) Wet seal cachets:
lower half of the cachet is filled with powdered drug. Then the flange of the empty
upper half of the cachet is moistened with water, and pressed over the lower half.
The cachet is dried for 15 minutes.
(ii)Dry seal cachets:
Drug powder is filled in the lower half and the upper half is pressed over it just like
a capsule.
Use:
They are used for administering the drug with unpleasant taste and a large dose.
Before administration, a cachet should be immersed in water for few seconds and
then placed on the tongue and swallowed with water.
e.g. Sodium aminosalicylate cachets
Sodium aminosalicylate and isoniazid cachtets.
CAPSULES
Capsule are the solid unit dosage form of medicament in which the drug or drugs
are enclosed in a practically tasteless, hard or soft soluble container of shell made
up of gelatin.
Hard gelatin capsules are made up of two cylindrical halves, one slightly larger in
diameter but shorter in length known as cap and the other slightly shorter in
diameter but longer in length known as base.
Soft gelatin capsules are flexible in nature. They may be spherical, ovoid
cylindrical or tubes. The small spherical capsules are also known as ‘pearls’. soft
gelatin capsules are used to enclose solids, semisolids or liquids.
for oral administration the capsule is placed on the tongue and swallowed with a
drink of water.
Examples of hard gelatin capsules: Ampicillin capsules, multivitamin capsules.
Examples of soft gelatin capsules: chloramphenicol soft gelatin capsules.
DUSTING POWDER
These are meant for external application on to the skin and are generally applied
in a very fine state of subdivision to avoid local irritation.
Dusting powders are of two types:
(i) Medical
(ii) Surgical
Medical dusting powders are mainly used for superficial skin conditions and for
antiseptics, anti-pruritic, astringent, anti-perspirant, absorbent, protective and
lubricant purposes.
e.g. dicophane dusting powder
zinc and salicylic acid dusting powder
zinc, starch and talc dusting powder.
Surgical dusting powders are used in body cavities, and also on major wounds as a
result of burns and umbilical cords of infants. Surgical dusting powders must be
sterilised before their use.
Dusting powders are generally prepared by mixing two or more ingredients on of
which must be either starch, kaolin or talc as one of the ingredients of the
formulations. Talc and kaolin are commonly used because they are chemically
inert. however, since these materials are usually contaminated with pathogenic
bacteria, these must be sterilised.
e.g. Neosporin powder.
INSUFFLATIONS
These are finely divided powders meant for introduction into the body cavities such
as ears, nose, tooth sockets and vagina with the help of an apparatus known as
‘insufflator’, without which it will be difficult to apply the powders directly.
Insufflator sprays the powder into stream of finely divided particles all over the site
of application. The following difficulties are generally faced while using the
insufflators:
(i) It is difficult to obtain a measured quantity of the drug as a uniform dose.
(ii) It gets blocked when it is slightly wet or the powder used is wet.
Use: The insufflations are used to produce a local effect, as in the treatment of ear,
nose and throat infection with antibiotics or to produce a systemic effect from a
drug that is destroyed in the gastrointestinal tract.
EFFERVESCENT GRANULES
The effervescent granules are specially prepared solid dosage form of medicament,
meant for oral intake. they contain a medicament mixed with citric acid, tartaric
acid and sodium bicarbonate. Sometimes saccharin or sucrose may be added as a
sweetening agent.
Ingredients used;
(i) Sodium bicarbonate: It reacts with the acids when the preparation is added to
water. The evolved carbondioxide produces effervescence.
(ii) Citric acid and tartaric acid: The quantity of these is slightly more than is
necessary to neutralise the sodium bicarbonate because effervescent preparations
are more palatable if slightly acidic.
Tartaric acid is anhydrous but citric acid has one molecule of water of
crystallization. heating liberates this water and the moist condition thus produced
allows partial interaction between the acids and bicarbonates, during which more
water is formed -
The water of crystallization of the citric acid and the water from the reactions
makes the material coherent.
(iii) Medicaments: often inorganic salts containing water of crystallisation are
incorporated. e.g. magnesium and sodium sulphates, sodium phosphate and
lithium citrate.
Methods of preparation
There are two methods of preparation : 1. Hot method and 2. Wet method
Hot method: A large evaporating dish is heated on water bath. All the powders are
taken in that hot dish to ensure rapid evaporation of water liberated from citric
acid. Thus a coherent damp mass is prepared.
The water required for granulation is provided from two sources:
1. From one molecule of water of crystallisation of citric acid which is liberated
during heating.
2. The water produced from the reactions of citric acid and tartaric acid with sodium
bicarbonate.
Wet method: in this method the mixed ingredients are moistened with non-aqueous
liquid (e.g. Alcohol) to prepare a coherent mass.
The coherent damp mass from both the methods is then passed through a No. 8
sieve and dried in an oven at a temperature not exceeding 60 0C. The dried
granules are again passed through the sieve to break the lumps which may be
formed during drying. The dried granules are packed in an air tight container.
Use: Before administration, the desired quantity is dissolved in water, the acid and
bicarbonate react together producing effervescence.
The carbonated water produced from the release of carbondioxide serves to mask
the bitter and saline taste of drugs.
More over carbondioxide stimulates the flow of gastric juice and helps absorption
of medicament.
LOZENGES
Lozenges are solid dosage form of medicaments which are meant for slow
dissolution in the mouth. Along with medicament they contain a sweetening agent,
flavouring agent and a strong binding agent.
They may be prepared either by moulding or by compression.
Examples are compound bismuth lozenges, liquorice lozenges.
PESSARIES
Pessaries are solid unit dosage form of medicament meant for introduction into
vagina. The bases used for the manufacture of pessaries are such that at room
temperature they retain the original shape but when inserted into the body cavity
either it melts or dissolve in the cavity fluids to release the medicament.
They may be prepared either by moulding or by compression.
e.g. lactic acid pessaries, nystatin pessaries.
POWDERS
Powders are solid dosage form of medicament meant for internal and external use.
The powders meant for internal use are known as oral powders whereas those
meant for external use are known as dusting powders.
The powders may be simple or compound.
When the powders are dispensed in large quantities in a container and the patient
is asked to measure a specified quantity as a dose then these powders are known
as bulk powders.
e.g.
1. Bulk powder for internal use;
e.g. Compound sodium chloride and dextrose oral
powder.
Compound rhubarb oral powder
2. Bulk powder for external use;
e.g. Snuffs
Talc dusting powders
Tooth powder.
TABLETS
Tablets are unit solid dosage form of medicament or medicament with or without
suitable diluents. They are prepared usually by compression.
Tablets are generally meant for oral administration but may be used by other
routes of administration.
e.g. aminophylline tablets
paracetamol tablets
antacid tablets.
SUPPOSITORIES
Suppositories are special shaped solid dosage form of medicament for insertion
into body cavities other than mouth. These products are so formulated that after
insertion, they will either melt of dissolve in the cavity fluids to release the
medicament.
Suppositories vary in shapes, sizes and weights. General suppositories from 1 to 2
gm are prepared with either cocoa-butter or glecero- gelatin base.
e.g. aminophylline suppositories
glycerol suppositories.
CREAMS
Creams are viscous liquid or semisolid emulsions intended for application to the
skin i.e. for external use.
Creams are of two types, aqueous creams and oily creams. In case of aqueous
creams the emulsions are oil-in-water type and in case of oily creams emulsions
are of water-in-oil type.
Due to the presence of water soluble bases they can be easily removed from the
skin.
The aqueous creams have a tendency to grow bacterial and mold growth,
therefore a preservative must be added in their formulation.
e.g. cetomacrogol cream, cetrimide cream, hydrocortisone cream, zinc cream BPC.
Advantages of creams:
1. Creams are more acceptable to the patients because they are less greasy and are
easier to apply.
2. They interfere less with skin functions.
3. o/w type of creams (superior to w/o type) can be rub onto the skin more readily
and are easily removed by washing. w/o can be spread more evenly.
4. o/w type of cream are less likely to soil clothes.
5. Evaporation of water from o/w type of cream causes cooling sensation.
6. o/w creams absorbs the discharges from the wound (liquid exudate) very quickly.
7. w/o creams (e.g. cold creams) restricts evaporation from the skin, it can be used
on non-weeping surfaces to prevent dehydration ( in dry season), restore
suppleness (softness) - this property is said to be ‘emollient’.
Disadvantages:
1. Since it is a semisolid preparation and containing oil in large amount, some of
which are inedible, hence creams are not used for internal use. Basically creams
are meant for application onto the skin.
2. the aqueous phase is prone to the growth of molds and bacteria hence
preservatives should be used.
3. Sometimes rancidification of oils take place.
JELLIES
Jellies are transparent or non-greasy semisolid preparations meant for external
application to the skin or mucous membrane. They are used for medication or
lubrication purposes.
e.g. contraceptive jellies (spermicidal action)
ichthammol jelly etc.
they are used for lubricating catheters, surgical gloves and rectal thermometers.
The gelling agents may be gelatin, or a carbohydrate such as starch, tragacanth,
sodium alginate or cellulose derivative.
OINTMENTS
Ointments are the soft semisolid, greasy preparations meant for external
application onto the skin or mucous membrane (rectum and nasal mucosa).
They usually contain a medicament dissolved, suspended or emulsified in the base.
Ointments are used for their emollient and protective action to the skin.
e.g. compound benzoic acid ointment, cetrimide emulsifying ointment
PASTES
Pastes are semisolid preparations meant for external application to the skin. they
generally contain large amount of finely powdered solids such as starch, zinc
oxide, calcium carbonate etc.
They provide a protective coating over the areas to which they are applied.
The base may be anhydrous (liquid or soft paraffin) or water-soluble (glycerol or a
mucilage). Their stiffness make them useful as protective coatings.
e.g. magnesium sulfate paste.,
zinc and coal tar paste
OPHTHALMIC OINTMENTS
Ophthalmic ointments are meant for application to the eye. They should be sterile
and free from irritation. They should be packed in sterile containers which should
keep the preparation sterile until whole of it is used up.
e.g. atropine eye ointment
chloromycetin eye ointments
Difference between paste and ointments;
Paste Ointment
1. Contains a large amount of (50%) of finely
1. Ointments contain very less amount of
powdered solids. As a result they are often powdered solids. They are soft.
very stiff.
2. When applied on the skin the paste adhere
2. Ointments are less viscous, hence spread
well and remain confined in the area of beyond the area of application.
application.
3. They are porous so the perspiration
3. Non-porous - hence perspiration cannot
(sweat)can escape through it. escape through it.
4. They are less greasy than ointments. 4. More greasy than pastes.
LIQUIDS
APPLICATIONS:
Applications are liquid or viscous preparations intended for application to the skin.
usually, they are suspensions or emulsions.
Most of the official preparations contain paraciticides and are intended for only a
limited number of applications.
They should be dispensed in coloured fluted bottles in order to distinguish them
from preparations meant for internal use. The container should be labeled “FOR
EXTERNAL USE ONLY”.
Examples of applications are calamine application compound B.P.C.
dicophane application B.P.C.
MONOPHASIC LIQUID DOSAGE FORMS
Monophasic liquid dosage forms are represented by true or colloidal
solutions.
The components of the solution which is present in a larger quantity is known as
“solvent”, whereas the component present in a smaller quantity is termed as
“solute”.
Classification
1. Liquid for internal use e.g. syrups, elixirs, linctus, drops and draughts.
2. Liquids for external use which are of two types:
(a) Liquids to be applied to the skin e.g. liniments and lotions etc.
(b) Liquids meant for body cavities e.g. gargles, throat paints, mouth washes, eye
drops, eye lotions, ear drops, nasal drops, sprays and inhalation.
1. AROMATIC WATERS
Aromatic waters are also known as medicated waters. They are dilute , usually
saturated, aqueous solutions of volatile oils (e.g. peppermint oil, cinnamon oil) or
volatile substances (e.g. camphor).
Uses:
(i) Some of them have a mild therapeutic action but
(ii) mainly they are used as flavouring agents in preparations meant for internal use.
SYRUPS
Syrups are liquid oral preparations in which the vehicle is a concentrated aqueous
solution of sucrose or other sugar.
N.B. Syrups generally are not issued directly to the patients when it is issued to
the patients:
(i) if it is clear it is called elixir and
(ii) if it is suspension it is called mixtures.
Advantages of syrups
1. Syrups retards oxidation because it is partly hydrolyzed into reducing sugar such
as dextrose and levulose.
2. It prevents decomposition of many vegetable substances. Syrups have high
osmotic pressure which prevents the growth of bacteria, fungi and molds which
are the chief causes of decomposition in solutions of vegetable matter.
3. They are palatable. Due to the sweetness of sugar it is a valuable vehicle for the
administration of unpalatable substances.
ELIXIRS
Definition: Elixirs are clear, liquid, oral preparations of potent or nauseous drugs.
They are pleasantly flavoured and usually attractively coloured and are very stable.
Elixirs usually contains potent drugs, such as antibiotics, antihistamines and
sedatives.
Vehicles used in elixirs are alcohol, glycerol and propylene glycol.
They are used
(i) for the production of clear solution. Essential oils from flavoring agents may
produce faint opalescence, hence alcohol 10 20% is useful for keeping oils in
solution.
(ii) When potent medicaments of low solubility is required to be dispensed, a mixture
of solvents that will give complete solution is used.
e.g. Phenobarbitone is virtually insoluble in water but a clear product can be made by
dissolving it in alcohol and then diluting with glycerol and water.
e.g. One part of paracetamol is soluble in 70 parts of water, 7 parts of alcohol, 9 parts
of propylene glycol or 40 parts of glycerol. In paracetamol elixir a mixture of
alcohol, propylene glycol and glycerol is used as vehicle.
LINCTUSES
Linctuses are viscous, liquid, oral preparations that are usually prescribed for the
relief of cough.
They contain medicaments which have demulcent (which soothes the inflammed
mucous membrane preventing contact with air in the surroundings), sedative or
expectorant action. The viscous vehicle soothes the sore membrane of the throat.
The usual dose is 5 ml. Linctuses should be taken in small doses, sipped and
swallowed slowly without diluting it with water in order to have the maximum and
prolonged effect of medicaments.
Simple Syrup is generally used as a vehicle. For diabetic patients Sorbitol solution
is used instead of Simple Syrup.
GLYCERIN OR GLYCERITES
Glycerites are the viscous preparations in which the drug is dissolved in glycerin
with or without heating. They are generally used as antiseptic or anti-inflammatory
preparations.
e.g. icthammol glycerin
tannic acid glycerin
phenol glycerin
COLLODION
Collodions are liquid preparations meant for external application to the skin. They
are convenient for application on small cuts and abrasions and are also used when
a prolonged contact between the skin and the medicament is required.
The vehicle is volatile and evaporates on application to the skin, leaving a flexible,
protective film covering the site.
Preparations
Volatile solvents used are ether and alcohol.
Film producing ingredient is pyroxylin (nitrocellulose)
Plasticizer giving the flexibility is castor oil.
Preparation
The solution is made by shaking the ingredients in a closed container, allowing to
stand for few days while impurities settle and then decanting the supernatant
liquid, because the solution is too volatile for filtration.
Storage
Collodions are stored in small light-resistant, well closed containers.
LINIMENT
Liniments are liquid, semi-liquid or occasionally semi-solid preparations intended
for application on the skin.
They may be alcoholic or oily solutions or emulsions.
Most are massaged onto the skin e.g. counter-irritant type.
Some are applied on warm dressing or with a brush. e.g. analgesic and soothing
type.
Liniments must not be applied to broken skin because they would be very
irritating.
e.g. Soap Liniment BPC
Camphor Liniment BP
Methyl salicylate liniment BPC
Alcohol is the main vehicle. In increases the penetration of counter-irritant
molecules through skin.
LOTIONS
Lotions are liquid preparations for external application without friction.
They are either dabbed on the skin or applied on a suitable dressing and covered
with water proof material to reduce evaporation.
e.g. Copper and zinc sulfate lotion is used for impetigo
Zinc sulfate and salicylic acid for ulcer
Salicylic acid lotion for dandruff
Salicylic acid and mercuric chloride lotion for follicular infection
N.B. Copper and Zinc sulfate have astringent action.
Salicylic acid has keratolytic action.
GELS
Gels are aqueous colloidal suspensions of the hydrated forms of insoluble
medicaments e.g. aluminium hydroxide gel, used as antacid.
EXTRACTS
Extracts are concentrated preparations containing the active principles of
vegetable or animal drugs. The drugs are extracted with suitable solvents and the
product is concentrated o one of three types of extract
Liquid Extract of which 1 ml usually contains the active constituents from 1 g of
drug.
Dry Extract obtained by completely removing the solvent under, reduced pressure.
Soft Extract obtained by evaporation to a plastic mass.
TINCTURES
These are alcoholic preparations containing the active principles of vegetable
drugs.
They are weaker than extracts.
They are usually prepared by maceration and percolation, or may be prepared by
dissolving the corresponding liquid extract of chemical substances (e.g. iodine) in
alcohol or hydroalcohol solvent.
e.g. Belladonna tincture
Aromatic cardamom tincture
Iodine tincture
SPIRITS
Spirits are alcoholic or hydroalcoholic solutions of volatile substances.
Most are used as flavouring agents but a few have medicinal value.
e.g. Chloroform Spirit, Lemon Spirit, Compound Orange Spirit.
INFUSIONS
(i) Fresh Infusions are made by extracting vegetable drugs for a short time with
cold or boiling water (cf. making of tea). They quickly deteriorate as a result of
microbial contamination and therefore must be used within 12 hours.
(ii) Concentrated infusions are made by cold extraction with 25 % alcohol. The
alcohol preserves the product for an indefinite period.
Dilution of 1 part of concentrated infusions with 10 parts of water gives a
preparation corresponding fresh infusion.
e.g. Concentrated Compound Gentian Infusion
concentrated Senega Infusion