(4my5151) Semisolid Dosage Forms

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SEMISOLID DOSAGE FORMS
(a) Ointments:-Type of ointments, classification and selection of dermatological vehicles.
Preparation and stability of ointments by the following processes: (i) Trituration, (ii) Fusion, (iii)
Chemical reaction, (iv) emulsification.
(b) Pastes: Differences between ointments and pastes. Bases of pastes. Preparation of pastes and
their preservation.
(c) Jellies: An introduction to the different types of jellies and their preparation.
(d) An elementary study of poultice.
(e) Suppositories and pessaries: Their relative merits and demerits, types of suppositories,
suppository bases, classification, properties, preparation and packing of suppositories. Use of
suppositories for drug absorption.
Ointments are soft semisolid preparations meant for external application to the skin or mucous
membrane.
They usually contains medicament which is either dissolved or suspended in the base.
They have emollient and protective action.
Creams are semisolid emulsions and are generally of softer consistency and lighter than
ointments.
They are less greasy and are easy to apply.
Pastes are semisolid preparations for external application that differ from similar products in
containing a high proportion of finely powdered medicaments.
They are stiffer and are usually employed for their protective action and for their ability to absorb
serous discharges from skin lesions.
Thus when protective, rather than therapeutic action is desired, the formulation pharmacists will
favour a paste, but when therapeutic action is required, he will prefer ointments and creams.
Jellies are transparent or translucent, non-greasy, semisolid preparation mainly used externally.
The gelling agent may be gelatin, starch, tragacanth, sodium alginate or cellulose derivative (e.g.
carboxy methyl cellulose).
OINTMENT
Definition: Ointments are semisolid preparations for application to the skin or mucosae. The
ointment bases are almost always anhydrous and generally contains one or more medicaments in
suspension or solution.
Characteristics of an ideal ointment:
1. It should be chemically and physically stable.
2. It should be smooth and free from grittiness.
3. It should melt or soften at body temperature and be easily applied.
4. The base should be non-irritant and should have no therapeutic action.
5. The medicament should be finely divided and uniformly distributed throughout the base.
Classification of ointments
According to their therapeutic properties based on penetration of skin.
According to their therapeutic uses.
Ointments classified according to their therapeutic properties based on penetration are as follows:
(a) Epidermic, (b) Endodermic, (c) Diadermic
(a) Epidermic ointments
These ointments are intended to produce their action on the surface of the skin and produce local
effect.
They are not absorbed.
They acts as protectives, antiseptics and parasiticides.
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(b) Endodermic ointments
These ointments are intended to release the medicaments that penetrate into the skin. They are
partially absorbed and acts as emollients, stimulants and local irritants.
(c) Diadermic ointments
These ointments are intended to release the medicaments that pass through the skin and produce
systemic effects.
According to therapeutic uses the ointments are classified as follows:
(i) Acne treatment :resorcinol, sulfur.
(ii) Antibiotics :Used to kill microorganisms.
e.g. bacitracin, chlortetracycline, neomycin.
(iii) Antieczematous :Used to stop oozing and exudation from vesicles on the skin.
e.g. hydrocortisone, coal tar, ichthamol, salicylic acid.
(iv) Antifungal :Used to inhibit or kill the fungi.
e.g. benzoic acid, salicylic aid, nystatin, clotrimazole, etc.
(v) Anti-inflammatory :Used to relieve inflammatory, allergic and pruritic conditions of the skin
e.g. betamethasone valerate, hydrocortisone, triamcinolone acetonide
(vi) Antipruritic :Used to relieve itching.
e.g. benzocaine, coal tar.
(vii) Antiseptic :Used to stop sepsis.
e.g. ammoniated mercury, zinc oxide.
(vii) Astringent :Reduces the secretion of glands or discharge from skin surface.
e.g. calamine, zinc oxide, aluminium acetate and subacetate, acetic acid and tannic acid.
(ix) Counter irritant These are applied locally to irritate the intact skin, thus reducing or relieving
another irritation or deep seated pain. e.g. capsicum oleoresin, iodine (Iodex), methyl salicylate.
(x) Dandruff treatment :e.g. salicylic acid and cetrimide (cetyl trimethyl ammonium bromide)
(xi) Emollient :Used to soften the skin (for example in the dry season).
e.g. soft paraffin
(xii) Keratolytic Used to remove or soften the horny layer of the skin.
e.g. resorcinol, salicylic acid and sulfur.
(xi) Keratoplastic :Tends to increase the thickness of horny layer e.g. coal tar.
(xii) Parasiticide :These ointments destroy or inhibit living infestations such as lice and ticks.
e.g. benzyl benzoate, gamma-benzene hexachloride (GBH), sulfur etc.
(xiii) Protective :Protects the skin from moisture, air, sun rays or other substances such as soaps
or chemicals.
e.g. silicones, titanium dioxide, calamine, zinc oxide, petrolatum.
OINTMENT BASES
The ointment base is that substance or part of an ointment preparation which serves as carrier or
vehicle for the medicament.
An ideal ointment base should be inert, stable, smooth, compatible with the skin, non-irritating
and should release the incorporated medicaments readily.
Classification of ointment bases:
1. Oleaginous bases
2. Absorption bases
3. Water-miscible bases
4. Water soluble bases
OLEAGINOUS BASES
These bases consists of oils and fats. The most important are the
Hydrocarbons i.e. petrolatum, paraffins and mineral oils.
The animal fat includes lard.
The combination of these materials can produce a product of desired melting point and viscosity.
(a) Petrolatum (Soft paraffin)
This is a purified mixture of semi-solid hydrocarbons obtained from petroleum or heavy
lubricating oil.
Yellow soft paraffin (Petrolatum; Petroleum jelly)
This a purified mixture of semisolid hydrocarbons obtained from petroleum. It may contain
suitable stabilizers like, antioxidants e.g. a-tocopherol (Vitamin E), butylated hydroxy toluene
(BHT) etc.
Melting range : 38 to 560C.
White soft paraffin (White petroleum jelly, White petrolatum)
This a purified mixture of semisolid hydrocarbons obtained from petroleum, and wholly or
partially decolorized by percolating the yellow soft paraffin through freshly burned bone black or
adsorptive clays.
Melting range : 38 to 560C.
Use: The white form is used when the medicament is colourless, white or a pastel shade. This
base is used in
Dithranol ointment B.P.
Ammoniated Mercury and Coal tar ointment B.P.C.
Zinc ointment B.P.C.
(b) Hard paraffin (Paraffin)
This is a mixture of solid hydrocarbons obtained from petroleum.
It is colourless or white, odorless, translucent, wax-like substance. It solidifies between 50 and
570C and is used to stiffen ointment bases.
(c) Liquid paraffin (Liquid petrolatum,; White mineral oil)
It is a mixture of liquid , hydrocarbons obtained from petroleum. It is transparent, colourless,
odourless, viscous liquid.
On long storage it may oxidize to produce peroxides and therefore, it may contain tocopherol or
BHT as antioxidants.
It is used along with hard paraffin and soft paraffin to get a desired consistency of the ointment.
Tubes for eye, rectal and nasal ointments have nozzles with narrow orifices through which it is
difficult to expel very viscous ointments without the risk of bursting the tube. To facilitate the
extrusion upto 25% of the base may be replaced by liquid paraffins.
Advantages of hydrocarbons bases:
(i) They are not absorbed by the skin. They remain on the surface as an occlusive layer that
restricts the loss of moisture hence, keeps the skin soft.
(ii) They are sticky hence ensures prolonged contact between skin and medicament.
(iii) They are almost inert. They consist largely of saturated hydrocarbons, therefore, very few
incompatibilities and little tendency of rancidity are there.
(iv) They can withstand heat sterilization, hence, sterile ophthalmic ointments can be prepared
with it.
(v) They are readily available and cheap.
Disadvantages of hydrocarbon bases;
(i) It may lead to water logging followed by maceration of the skin if applied for a prolonged
period.
(ii) It retains body heat, which may produce an uncomfortable feeling of warmth.
(iii) They are immiscible with water; as a result rubbing onto the surface and removal after
treatment both are difficult.
(iv) they are sticky, hence makes application unpleasant and leads to contamination of clothes.
(v) Water absorption capacity is very low, hence, these bases are poor in absorbing exudate from
moist lesions.
ABSORPTION BASE
The term absorption base is used to denote the water absorbing or emulsifying property of these
bases and not to describe their action on the skin.
These bases (some times called emulsifiable ointment bases) are generally anhydrous substances
which have the property of absorbing (emulsifying) considerable quantity of water yet retaining
its ointment-like consistency.
Preparations of this type do not contain water as a component of their basic formula but if water
is incorporated a W/O emulsion results.
Wool Fat (anhydrous lanolin)
It is the purified anhydrous fat like substance obtained from the wool of sheep.
It is practically insoluble in water but can absorb water upto 50% of its own weight. Therefore it
is used in ointments the proportion of water or aqueous liquids to be incorporated in hydrocarbon
base is too large.
Due to its sticky nature it is not used alone but is used along with other bases in the preparation
of a number of ointments.
e.g. Simple ointment B.P. contains 5% and the B.P. eye ointment base contains 10% woolfat.
Hydrous Wool Fat (Lanolin)
It is a mixture of 70 % w/w wool fat and 30 % w/w purified water. It is a w/o emulsion.
Aqueous liquids can be emulsified with it.
It is used alone as an emollient.
Example:- Hydrous Wool Fat Ointment B.P.C., Calamine Coal Tar Ointment.
Wool Alcohol
It is the emulsifying fraction of wool fat. Wool alcohol is obtained from wool fat by treating it
with alkali and separating the fraction containing cholesterol and other alcohols. It contains not
less than 30% of cholesterol.
Use:-
It is used as an emulsifying agent for the preparation of w/o emulsions and is used to absorb
water in ointment bases.
It is also used to improve the texture, stability and emollient properties of o/w emulsions.
Examples :- Wool alcohol ointment B.P. contains 6% wool alcohol and hard, liquid and soft
paraffin.
Beeswax
It is purified wax, obtained from honey comb of bees.
It contains small amount of cholesterol. It is of two types: (a) yellow beeswax and (b) white
beeswax.
Use:-
Beeswax is used as a stiffening agent in ointment preparations.
Examples:-Paraffin ointment B.P.C. contains beeswax.
Cholesterol
It is widely distributed in animal organisms. Wool fat is also used as a source of cholesterol.
Use:- It is used to increase the water absorbing power of an ointment base.
Example:- Hydrophilic petroleum U.S.P. contains:
Cholesterol 3%
Stearyl alcohol 3%
White beeswax 8%
White soft paraffin 86%
Advantages of absorption bases:
(i) They are less occlusive nevertheless, are good emollient.
(ii) They assist oil soluble medicaments to penetrate the skin.
(iii) They are easier to spread.
(iv) They are compatible with majority of the medicaments.
(v) They are relatively heat stable.
(vi) The base may be used in their anhydrous form or in emulsified form.
(vii)They can absorb a large quantity of water or aqueous substances.
Disadvantages: Inspite of their hydrophilic nature, absorption bases are difficult to wash.
WATER MISCIBLE BASES
They are miscible with an excess of water. Ointments made from water-miscible bases are easily
removed after use.
There are three official anhydrous water-miscible ointment bases:-
Example:-
Emulsifying ointment B.P. - contains anionic emulsifier.
Cetrimide emulsifying ointment B.P. - contains cationic emulsifier
Cetomacrogol emulsifying ointment B.P. - contains non-ionic emulsifier
Uses: they are used to prepare o/w creams and are easily removable ointment bases
e.g. Compound Benzoic Acid Ointment (Whitfields Ointment) - used as antifungal ointment.
Advantages of water miscible bases:
(i) Readily miscible with the exudates from lesions.
(ii) Reduced interference with normal skin function.
(iii) Good contact with the skin, because of their surfactant content.
(iv) High cosmetic acceptability, hence there is less likelihood of the patients discontinuing
treatment.
(v) Easy removal from the hair.
WATER SOLUBLE BASES
Water soluble bases contain only the water soluble ingredients and not the fats or other greasy
substances, hence, they are known as grease-less bases.
Water soluble bases consists of water soluble ingredients such as polyethylene glycol polymers
(PEG) which are popularly known as carbowaxes and commercially known as macrogols.
They are a range of compounds with the general formula:
CH2OH . (CH2OCH2) n CH2OH
The PEGs are mixtures of polycondensation products of ethylene and water and they are
described by numbers representing their average molecular weights. Like the paraffin
hydrocarbons they vary in consistency from viscous liquids to waxy solids.
Example:-
Macrogols 200, 300, 400 - viscous liquids
Macrogols 1500 - greasy semi-solids
Macrogols 1540, 3000, 4000, 6000 - waxy solids.
Different PEGs are mixed to get an ointment of desired consistency.
Advantages of PEGs as ointment base:
(a) They are water soluble; hence, very easily can be removed from the skin and readily miscible
with tissue exudates.
(b) Helps in good absorption by the skin.
(c) Good solvent properties. Some water-soluble dermatological drugs, such as salicylic acid,
sulfonamides, sulfur etc. are soluble in this bases.
(d) Non-greasy.
(e) They do not hydrolyze, rancidify or support microbial growth.
(f) Compatibility with many dermatological medicaments.
Disadvantages:
(a) Limited uptake of water. Macrogols dissolve when the proportion of water reaches about 5%.
(b) Reduction in activity of certain antibacterial agents, e.g. phenols, hydroxybenzoates and
quaternary compounds.
(c) Solvent action on polyethylene and bakelite containers and closures.
Certain other substances which are used as water soluble ointment bases include tragacanth,
gelatin, pectin, silica gel, sodium alginate, cellulose derivatives, etc.
FACTORS GOVERNING SELECTION OF AN IDEAL OINTMENT BASE
1. Dermatological factors
2. Pharmaceutical factors
1. Dermatological factors
(a) Absorption and Penetration:
Penetration means passage of the drug across the skin i.e. cutaneous penetration, and
absorption means passage of the drug into blood stream.
Medicaments which are both soluble in oil and water are most readily absorbed though the skin.
Whereas animal and vegetable fats and oils normally penetrate the skin.
Animals fats, e.g. lard and wool fat when combined with water, penetrates the skin.
o/w emulsion bases release the medicament more readily than greasy bases or w/o emulsion
bases.
(b) Effect on the skin
Greasy bases interfere with normal skin functions i.e. heat radiation and sweating. They are
irritant to the skin.
o/w emulsion bases and other water miscible bases produce a cooling effect due to the
evaporation of water.
(c) Miscibility with skin secretion and serum
Skin secretions are more readily miscible with emulsion bases than with greasy bases. Due to this
the drug is more rapidly and completely released to the skin.
(d) Compatibility with skin secretions:
The bases used should be compatible with skin secretions and should have pH about 5.5 because
the average skin pH is around 5.5. Generally neutral ointment bases are preferred.
(e) Non-irritant
All bases should be highly pure and bases specially for eye ointments should be non-irritant and
free from foreign particle.
(f) Emollient properties
Dryness and brittleness of the skin causes discomfort to the skin therefore, the bases should keep
the skin moist. For this purpose water and humectants such as glycerin, propylene glycol are
used. Ointments should prevent rapid loss of moisture from the skin.
(g) Ease of application and removal
The ointment bases should be easily applicable as well as easily removable from the skin by
simple washing with water. Stiff and sticky ointment bases require much force to spread on the
skin and during rubbing newly formed tissues on the skin may be damaged.
2. Pharmaceutical factors
(a) Stability
Fats and oils obtained from animal and plant sources are prone to oxidation unless they are
suitably preserved. Due to oxidation odour comes out. This type of reactions are called
rancidification. Lard, from animal origin, rancidify rapidly. Soft paraffin, simple ointment and
paraffin ointment are inert and stable. Liquid paraffin is also stable but after prolonged storage it
gets oxidized. Therefore, an antioxidant like tocopherol (Vit -E) may be incorporated. Other
antioxidants those may be used are butylated hydroxy toluene (BHT) or butylated hydroxy
hydroxy anisole (BHA).
(b) Solvent properties
Most of the medicaments used in the preparation of ointments are insoluble in the ointment bases
therefore, they are finely powdered and are distributed uniformly throughout the base.
(c) Emulsifying properties
Hydrocarbon bases absorbs very small amount of water.
Wool fat can take about 50% of water and when mixed with other fats can take up several times
its own weight of aqueous solution.
Emulsifying ointment, cetrimide emulsifying ointment and cetomacrogol emulsifying ointment
are capable of absorbing considerable amount of water, forming w/o creams.
(d) Consistency
The ointments produced should be of suitable consistency. They should neither be hard nor too
soft. They should withstand climatic conditions. Thus in summer they should not become too soft
and in winter not too hard to be difficult to remove from the container and spread on the skin.
The consistency of an ointment base can be controlled by varying the ratio of hard and liquid
paraffin.
PREPARATION OF OINTMENTS
A well-made ointment is -
(a) Uniform throughout i.e. it contains no lumps of separated high melting point ingredients of
the base, there is no tendency for liquid constituents to separate and insoluble powders are evenly
dispersed.
(b) Free from grittiness, i.e. insoluble powders are finely subdivided and large lumps of particles
are absent. Methods of preparation must satisfy this criteria.
Two mixing techniques are frequently used in making ointments:
1. Fusion, in which ingredients are melted together and stirred to ensure homogeneity.
2. Trituration, in which finely-subdivided insoluble medicaments are evenly distributed by
grinding with a small amount of the base or one of its ingredients followed by dilution with
gradually increasing amounts of the base.
1. Ointments prepared by Fusion method:
When an ointment base contain a number of solid ingredients such as white beeswax, cetyl
alcohol, stearyl alcohol, stearic acid, hard paraffin, etc. as components of the base, it is required to
melted them. The melting can be done in two methods:
Method-I
The components are melted in the decreasing order of their melting point i.e. the higher m.p.
substance should be melted first, the substances with next melting point and so on. The
medicament is added slowly in the melted ingredients and stirred thoroughly until the mass cools
down and homogeneous product is formed.
Advantages:
This will avoid over-heating of substances having low melting point.
Method-II
All the components are taken in subdivided state and melted together.
Advantages:
The maximum temperature reached is lower than Method-I, and less time was taken possibly
due to the solvent action of the lower melting point substances on the rest of the ingredients.
Cautions:
(i) Melting time is shortened by grating waxy components (i.e. beeswax, wool alcohols, hard-
paraffin, higher fatty alcohols and emulsifying waxes) by stirring during melting and by lowering
the dish as far as possible into the water bath so that the maximum surface area is heated.
(ii) The surface of some ingredients discolors due to oxidation e.g. wool fats and wool alcohols
and this discolored layers should be removed before use.
(iii) After melting, the ingredients should be stirred until the ointment is cool, taking care not to
cause localized cooling, e.g. by using a cold spatula or stirrer, placing the dish on a cold surface
(e.g. a plastic bench top) or transferring to a cold container before the ointment has fully set. If
these precautions are ignored, hard lumps may separate.
(iv) Vigorous-stirring, after the ointment has begun to thicken, causes excessive aeration and
should be avoided.
(v) Because of their greasy nature, many constituents of ointment bases pickup dirt during
storage, which can be seen after melting. This is removed from the melt by allowing it to
sediment and decanting the supernatant, or by passage through muslin supported by a warm
strainer. In both instances the clarified liquid is collected in another hot basin.
(vi) If the product is granular after cooling, due to separation of high m.p. constituents, it should
be remelted, using the minimum of heat, and again stirred and cooled.
Example:
(i) Simple ointment B.P. contains
Wool fat 50g
Hard paraffin 50g
Cetostearyl alcohol 50g
White soft paraffin 850g
Type of preparation: Absorption ointment base
Procedure:
Hard paraffin and cetostearyl alcohol on water-bath. Wool fat and white soft paraffin are mixed
and stirred until all the ingredients are melted.
If required decanted or strained and stirred until cold and packed in suitable container.
(ii) Paraffin ointment base
Type of preparation : Hydrocarbon ointment base
(iii) Wool alcohols ointment B.P.
Type of preparation: Absorption base
(iv) Emulsifying ointment B.P.
Type of preparation: Water-miscible ointment base.
(v) Macrogol ointment B.P.C
Type of preparation: Water soluble ointment base
Formula: Macrogol 4000
Liquid Macrogol 300
Method: Macrogol 4000 is melted and previously warmed liquid macrogol 300 is added. Stirred
until cool.
2. OINTMENT PREPARED BY TRITURATION
This method is applicable in the base or a liquid present in small amount.
(i) Solids are finely powdered are passed through a sieve (# 250, # 180, #125).
(ii) The powder is taken on an ointment-slab and triturated with a small amount of the base. A
steel spatula with long, broad blade is used. To this additional quantities of the base are
incorporated and triturated until the medicament is mixed with the base.
(iii) Finally liquid ingredients are incorporated. To avoid loss from splashing, a small volume of
liquid is poured into a depression in the ointment an thoroughly incorporated before more is
added in the same way. Splashing is more easily controlled in a mortar than on a tile.
Example:
(i) Whitfield ointment (Compound benzoic acid ointment B.P.C.)
Formula: Benzoic acid, in fine powder 6gm
Salicylic acid, in fine powder 3gm
Emulsifying ointment 91gm
Method: Benzoic acid and salicylic acid are sieved through No. 180 sieves. They are mixed on the
tile with small amount of base and levigated until smooth and dilute gradually.
(ii) Salicylic acid sulphur ointment B.P.C.
3. OINTMENT PREPARATION BY CHEMICAL REACTION
Chemical reactions were involved in the preparation of several famous ointments of the past, e.g.
Strong Mercuric Nitrate Ointment, both of the 1959 B.P.C.
(a) Ointment containing free iodine
Iodine is only slightly soluble in most fats and oils but readily soluble.
Iodine is readily soluble in concentrated solution of potassium iodide due to the formation of
molecular complexes KI.I2, KI.2I2, KI.3I2 etc.
These solutions may be incorporated in absorption-type ointment bases.
e.g. Strong Iodine Ointment B.Vet.C (British Veterinary Pharmacopoeia) is used to treat
ringworm in cattle. It contains free iodine. At one time this type of ointments were used as
counter-irritants in the treatment of human rheumatic diseases but they were not popular
because:
(i) They stain the skin a deep red color.
(ii) Due to improper storage the water dries up and the iodine crystals irritate the skin, hence
glycerol was some times to dissolve the iodine-potassium iodide complex instead of water.
Example: Strong Iodine Ointment B. Vet.C.
Iodine
Woolfat
Yellow soft paraffin
Potassium iodide
Water
Procedure:
(i) KI is dissolved in water. I2 is dissolved in it.
(ii) Woolfat and yellow soft paraffin are melted together over water bath. Melted mass is cooled to
about 400C.
(iii) I2 solution is added to the melted mass in small quantities at a time with continuos stirring
until a uniform mass is obtained.
(iv) It is cooled to room temperature and packed.
Use: - Ringworm in cattle.
(b) Ointment containing combined iodine
Fixed oils and many vegetable and animal fats absorb iodine which combines with the double
bonds of the unsaturated constituents, e.g.
CH3.(CH2) 2.CH = CH.(CH2) 7.COOH + I2 CH3.(CH2) 2.CHI CHI.(CH2) 7.COOH
Oleic acid di-iodostearic acid
Example: Non-staining Iodine Ointment B.P.C. 1968 Iodine
Arachis Oil
Yellow Soft Paraffin
Method:
(a) Iodine is finely powdered in a glass mortar and required amount is added to the oil in a glass-
stoppered conical flask and stirred well.
(b) The oil is heated at 500C in a water-bath and stirred continually. Heating is continued until
the brown color is changed to greenish-black; this may take several hours.
(c) From 0.1g of the preparation the amount of iodine is determined by B.P.C. method and the
amount of soft paraffin base is calculated to give the product the required strength.
(d) Soft paraffin is warmed to 400C. The iodized oil is added and mixed well. No more heat is
applied because this causes deposition of a resinous substance.
(e) The preparation is packed in a warm, wide-mouthed, amber color, glass bottle. It is allowed to
cool without further stirring.
4. PREPARATION OF OINTMENTS BY EMULSIFICATION
An emulsion system contain an oil phase, an aqueous phase and an emulsifying agent.
For o/w emulsion systems the following emulsifying agents are used:
(i) water soluble soap
(ii) cetyl alcohol
(iii)glyceryl monostearate
(iv) combination of emulsifiers: triethanolamine stearate + cetyl alcohol
(v) non-ionic emulsifiers: glyceryl monostearate, glyceryl monooelate, propylene glycol stearate
For w/o emulsion creams the following emulsifiers are used:
(i) polyvalent ions e.g magnesium, calcium and aluminium are used.
(ii) combination of emulsifiers: beeswax + divalent calcium ion
The viscosity of this type of creams prevent coalescence of the emulsified phases and helps in
stabilizing the emulsion.
Example:
Cold cream:
Procedure:
(i) Water immiscible components e.g. oils, fats, waxes are melted together over water bath
(700C).
(ii) Aqueous solution of all heat stable, water soluble components are heated (700C).
(iii) Aqueous solution is slowly added to the melted bases with continuous stirring until the
product cools down and a semi-solid mass is obtained.
N.B. The aqueous phase is heated otherwise high melting point fats and waxes will immediately
solidify on addition of cold aqueous solution.
STABILITY OF OINTMENTS
The ointments should remain stable from the time of preparation to the time when the whole of it
is consumed by the user.
(i) To stop microbial growth preservatives are added. Preservatives for ointment includes : p-
hydroxy benzoates, phenol, benzoic acid, sorbic acid, methyl paraben, propyl paraben, quaternary
ammonium compounds, mercury compounds etc.
(ii) The preservatives should not react with any of the component of the formulation. Plastic
containers may absorb the preservative and thereby decreasing the concentration of preservative
available for killing the bacteria.
(iii) Some ingredients like wool fat and wool alcohols are susceptible to oxidation. Therefore, a
suitable antioxidant may be incorporated to protect the active ingredients from oxidation.
(iv) Incompatible drugs, emulsifying agents and preservatives must be avoided. The drugs which
are likely to hydrolyze must be dispensed in an anhydrous base.
(v) Humectants such as, glycerin, propylene glycol and sorbitol may be added to prevent the loss
of moisture from the preparation.
(vi) Ointment must be stored at an optimum temperature otherwise separation of phases may
take place in the emulsified products which may be very difficult to remix to get a uniform
product.
PASTE
Syllabus:
Differences between ointments and pastes.
Bases of pastes
Preparation of paste and their preservation.
Differences between pastes and ointments;
(i) Pastes generally contains a large amount (50%) of finely powdered solids. So they are often
stiffer than ointments.
(ii) When applied to the skin pastes adhere well, forming a thick coating protects and soothes
inflamed and raw surfaces and minimizes the damage done by scratching in itchy conditions
such as chronic eczema. it is comparatively easy to confine pastes to the diseased areas whereas
ointments, which are usually less viscous, tend to spread on to healthy skin, and this may result
in sensitivity reactions if the preparations contain a powerful medicament such as dithranol.
(iii) Because of the powder contents pastes are porous; hence, perspiration can escape. Since the
powders absorbs exudate, pastes with hydrocarbon base are less macerating than ointments with
a similar base.
(iv) They are less greasy than ointments but since their efficacy depends on maintaining a thick
surface layer they are far from attractive cosmetically.
(v) Most of the pastes are unsuitable for treating scalp conditions because they are difficult to
remove from the hair.
BASES OF PASTES:
1. Hydrocarbon base:
Soft paraffin and liquid paraffin are commonly used bases for the preparation of paste.
Name of the preparation
Active ingredients
Base
Use
1. Compound Zinc Paste B.P.
2. Compound Zinc & Salicylic acid Paste B.P.
(Lassars Paste)
3. Coal tar paste
4. Dithranol paste compound
5. Aluminium paste B.P.C.
(Baltimore Paste)
Zinc oxide
Zinc oxide & Salicylic acid
Coal tar
Dithranol
Aluminium oxide
Soft paraffin
Soft paraffin
Soft paraffin
Soft paraffin
Liquid paraffin
Eczema, psoriasis.
Eczema, psoriasis.
Eczema
Ring worm or psoriasis
Protectant
2. Water miscible base:
Base
Use
1. Resorcinol & sulfur Paste B.P.C.
2. Zinc & Coal tar Paste
3. Magnesium sulfate paste B.P.C.
(Morisons paste)
4. Titanium dioxide paste B.P.C.
Emulsifying ointment
Emulsifying wax
Magnesium sulfate -45%
Phenol in glycerol
Suspension of TiO2, ZnO, light kaolin and red Fe2O3 in glycerol + water.
Dandruff, and are easily removable from the hair.
Eczema
Used to treat boils, because of their powerful osmotic effect of the salt and the glycerol.
Absorbs exudates from weeping skin conditions.
3. Water soluble bases
Water soluble bases are prepared from mixtures of high and low molecular weight polyethylene
glycols (or macrogols).
Base
Use
1. Water soluble dental pastes
2. Triamcinolone Dental paste B.P.C.
Neomycin sulfate
Triamcinolone acetonide
in an adhesive paste
(NaCMC, pectin, + gelatin)
Sterilizing infected root canal
Anti-inflammatory
METHODS OF PREPARATION:
Like ointment, pastes are prepared by trituration and fusion methods. Trituration method is used
when the base is liquid or semisolid.
Fusion method is used when the base is semisolid and/or solid in nature.
Preparation 1.
Name: Compound Zinc Paste
Formula Zinc oxide, finely sifted 25 g
Starch, finely sifted 25 g
White soft paraffin 50 g
Type of preparation: Paste with semi-solid base prepared by fusion and trituration.
Procedure;
(a) Zinc oxide and starch powder are passed through No. 180 sieve.
(b) Soft paraffin is melted on a water bath.
(c) The required amount of powder is taken in a warm mortar, triturated with little melted base
until smooth. Gradually rest of the base is added and mixed until cold.
Preparation 2.
Name: Zinc and Coal tar Paste B.P.C.
Formula: Zinc oxide, finely sifted
Coal tar
Emulsifying wax
Starch
Yellow soft paraffin.
Type of preparation: Paste with semi-solid base prepared by fusion.
Procedure:
Method-I
(a) Emulsifying wax is melted in a tared dish (700C).
(b) The coal tar is weighed in the dish. Stirred to mix.
Soft paraffin is melted in a separate dish (700C) and about half is added to the tar-wax mixture;
stirred well. Remainder is added; stirred again until homogeneous.
Allowed to cool at about (300C) and zinc oxide (previously passed through 180 mesh) and starch,
in small amount with constant stirring. Stirred until cold.
Method-II
Wax and paraffin melted together, mixed well and stirred until just setting. Powders are mixed on
a slightly warm tile and the tar is incorporated. This method eliminates the risk of over heating.
JELLIES
Definition:
Jellies are transparent or translucent, non-greasy, semisolid preparation generally applied
externally.
They are used for medication, lubrication and some miscellaneous applications.
Types of jellies:
Medicated jellies
(i) Water soluble drugs like local anaesthetics, spermicides and antiseptics are suitable for
incorporation in the jellies.
(ii) They are easy to apply and evaporation of the water content produces a pleasant cooling
effect. The medicinal film usually adheres well and gives protection but is easily removed by
washing when the treatment is complete.
e.g. ephedrine sulfate jelly - used to arrest bleeding from nose.
pramoxine HCl , a local anaesthetic - relieves discomfort of pruritis and haemorrhoids.
phenylmercuric nitrate - as spermicidal contraceptive.
Lubricant jelly
Catheters, items of eletrodiagnostic equipment, such as cystoscopes, and rubber gloves or finger
stalls used for rectal and other examinations require lubrication before use.
The lubricants must be sterile for articles inserted into sterile regions of the body, such as urinary
bladder.
For painful investigations a local anaesthetic may be included as in Lignocaine Gel B.P.C.
Miscellaneous uses
The following are more specialized jellies -
(a) Patch testing
Here the jelly is the vehicle for allergens applied to the skin to detect sensitivity. Several allergens
may be applied on one person. The viscosity of the jelly and it leaves on drying help to keep the
particles separate.
(b) Electrocardiography
to reduce electrical resistance between the patients skin and electrodes of the cardiograph, an
electrode jelly may be applied. This contains NaCl to provide good conductivity and often pumice
powder which, when applied onto the skin, removes part of the horny layer of the epidermis, the
main layer of electrical resistance.
FORMULATION
Pharmaceutical jellies are usually prepared by adding a thickening agent such as tragacanth or
carboxy methylcellulose (CMC) to an aqueous solution in which drug has been dissolved.
The mass is triturated in a mortar until a uniform product is obtained.
For the preparation of jellies whole gum is preferred rather than powdered gum because the
former gives a clear preparation of uniform consistency.
The following gelling agents are used for the preparation of jellies.
(i) Tragacanth
the main hydrophilic component of tragacanth that gels in water has been named bassorin -
hence, tragacanth jellies are sometimes called bassorin paste.
The amount of gum required for a preparation varies with its use:
(a) For lubricating jelly 2 to 3%.
(b) Fro dermatological vehicles about 5%.
(c) For incorporation of ichthamol, resorcinol, salicylic acid and other medicaments, about 5% is
generally used. All formulations contain alcohol and/or glycerol and/or a volatile oil to disperse
the gum and prevent lumpiness when water is added.
(d) They vary in viscosity, due to the natural origin of the gum and variations in milling and
storage.
(e) The film left on the skin tends to flake.
(f) Viscosity is rapidly lost outside the pH range of 4.5 to 7.0; for example if benzoic acid is used as
the preservative.
(g) They are susceptible to microbial growth.
Example:
Formula Ichthamol 1.0 g
Tragacanth 2.5 g
Alcohol 90% 5.0 g
Glycerin 1.0 g
Purified water q.s. 50.0g
Procedure:
(i) Alcohol is taken in a 100 ml, wide mouthed jar; and then tragacanth is added to it. (The
reverse order may lead to lump formation). Mixed well.
(ii) Water is added as quickly as possible and mixed.
(iii) Separately ichthamol, glycerin and 10 ml water is mixed. Final weight is adjusted by adding
more of water.
2. Sodium alginate
Uses:- As lubricant - 1.5 to 2 % is used.
As dermatological vehicle - 5 to 10 % is used.
A trace of Ca - salt (CaCl2) may be added to increase the viscosity and most formulations contain
glycerol as a dispersing agent.
Advantage: Sodium alginate has an advantage over tragacanth that is available in several grade
or standardized viscosity.
3. Pectin
Pectin is a very good gelling agent and is used in the preparation of many types of jellies
including edible jellies.
Glycerin is used as a dispersing agent and humectant in dermatological jellies.
Jellies must be packed in well-closed containers because they lose water rapidly by evaporation
and this lose water rapidly by evaporation and this is increased by the susceptibility of pectin gels
to syneresis (i.e. exudation of the aqueous phase as a result of contraction of the gel).
4. Starch
Starch in combination with gelatin and glycerin is commonly used for preparations of jellies.
Glycerin in 50% may act as preservative.
Medicaments are incorporated in the cold jelly by trituration.
5. Gelatin
Insoluble in cold water but swell and softens in it. It is soluble in hot water.
Hot solution contain 2% gelatin forms a jelly on cooling.
Very stiff (15%) jellies are melted before used and after cooling to desired temperature are applied
with a brush to the affected area. The area is covered with bandage and the dressing may be left
in place for several weeks.
Zinc-gelatin jelly (Unnas paste) is such an example.
Formula: Zinc oxide 15g
Gelatin 15g
Glycerin 35g
Water 35g
Procedure:
(i) Gelatin soaked in water until softened.
(ii) Glycerin is added and heated over bath until the glycerin is dissolved.
(iii) Adjust the weight to 85 g if necessary by adding more amount of water.
(iv) ZnO is passed through sieve (#120). Required amount is added in small amounts to the
molten base with gentle stirring. Stirring is continued until a viscous product is obtained.
(v) The product so obtained is poured in a tray to a depth of about 1 cm with continuous
trituration throughout the operation. When the mass is set, carefully the mass is cut into pieces of
about 1.5cm2 with a blade or sharp knife.
6. Cellulose derivative
Methyl cellulose and sodium carboxy methyl cellulose
1. produce neutral jellies of stable viscosity.
2. Have good resistance against microbial growth.
3. Clear due to freedom from insoluble impurities.
4. Produce strong film after drying on the skin.
Use: Sodium carboxy methyl cellulose can be used to prepare lubricating jellies and sterile jellies.
e.g. lignocine gel - because it can withstand autoclaving temperature.
N.B. Other cellulose derivatives are
Hydroxy propyl methyl cellulose (Hypermellose)
Carbomer
Polyvinyl alcohols.
7. Clays
Gels containing 7 to 20 % of bentonite can be used as dermatological bases.
Disadvantages:
1. They are opalescent and lack attractiveness.
2. Their pH is about 9.0 i.e. not suitable for application on the skin.
3. Residue on the skin is powdery and rather silky.
Preservation of jellies:
Although some bases like clays and cellulose derivative(s) resist microbial contamination but
since all the jellies contain large amount of water, therefore must be suitably preserved.
e.g. Methyl paraben 0.1 to 0.2 % is commonly used.
Loss of water can quickly lead to skin formation on jellies and to prevent the hygroscopic
substances, e.g. glycerol, propylene glycol or sorbitol solution may be added.
Bases and medicaments sensitive to heavy metals are sometimes protected by a chelating agent
e.g. ethylene diamine tetra acetic acid (EDTA)
POULTICE
Definition: Poultice are paste-like preparations used externally to reduce inflammation because
they retain heat well. After heating, the preparation is spread thickly on a dressing and applied, as
hot as the patient can bear it, to the affected area.
Uses;
(i) Glycerol, because of its hygroscopic nature, is believed to draw infected materials from the
tissues when the poultice is used for boils and similar infections.
(ii) Methyl salicylate (an antirheumatic drug),
thymol (a powerful bactericide),
boric acid (a weak antimicrobial agent),
and peppermint oil (which contributes to the smell) are used for different purposes.
Method of applying the poultice:
(i) Fro use, the poultice is heated, with occasional stirring, until it can only be tolerated on the
back of the hand.
(ii) Then it is spread thickly on lint or other dressing and applied to the affected area which is
sometimes first covered with muslin to facilitate removal after use.
(iii) A thick layer of cotton wool is applied to retain the heat and a covering of oiled silk may be
added to protect clothing.
Example:
The only example given in the pharmacopoeia is Kaolin Poultice B.P.C.
Formula: Heavy kaolin, finely sifted and dried at 1000C 52.7 g
Boric acid, finely sifted 4.5 g
Methyl salicylate 0.2 ml
Thymol 50 mg
Peppermint oil 0.05 ml
Glycerin 42.5 g
Procedure:
(a) Kaolin is spread in a suitable quantity of kaolin in a thin layer, e.g. on a tray of aluminium
foil, and dried at 1000C until the weight is constant. Allowed to cool down and then passed
through No. 180 sieve.
(b) Boric acid and kaolin are mixed in a mortar. Gradually the mixed powder is triturated with
glycerol to form a smooth paste.
(c) The paste is transferred to a heat-resistant glass-jar, protected either wit a paper or aluminium
foil and heated at 1200C for 1 hour in a hot-air oven, with occasional stirring. The antimicrobial
effects of the heat and glycerol destroy the sporing pathogens that may be in the kaolin. (Above
1200C glycerin may degrade).
(d) After cooling a mixture of thymol, methyl salicylate and peppermint oil are mixed. (Eutectic
mixture).
(e) Kaolin poultice is stored in well closed containers to prevent loss of volatile ingredients and
absorption of moisture from the atmosphere by glycerin.
SUPPOSITORIES AND PESSARIES
Syllabus:
Their relative merits and demerits
Types of suppositories, Suppository bases, classification, properties, preparation and packaging of
suppositories.
Use of suppositories for drug absorption.
Definition:
Suppositories are specially shaped solid dosage form of medicament for insertion into body
cavities other than mouth.
They may be inserted into rectum, vagina or the urethra.
This products are so formulated that after insertion, they will either melt or dissolve in the cavity
fluids to release the medicament.
Advantages of rectal suppositories:
(i) Mechanical action: The rectal suppositories are extensively used as a mechanical aid to bowel
evacuation which produce its action by either irritating the mucous membrane of the rectum
(e.g. glycerol and bisacodyl) or by lubricating action or by mechanical lubrication.
(ii) Local action: The rectal suppositories may be used for soothing, antiseptic, local anaesthetic
action or for astringent effect. Therefore, they may contain
soothing e.g. zinc oxide
local anaesthetic- e.g. cinchocaine, benzocaine
astringents e.g. bismuth subgallate, hamamelis extract and tannic acid
antiinflammatory e.g. hydrocortisone and its acetate.
(iii) To provide systemic action: Suppositories are convenient mode of administration of drugs
which irritate the gastrointestinal tract, cause vomiting, are destroyed by the hepatic circulation,
or are destroyed in the stomach by pH changes, enzymes etc.
Partial bypass: The lower portion of the rectum affords a large absorption surface area from
which the soluble substances can absorb and reach the systemic circulation.
e.g. aminophylline used in asthmatic and chronic bronchitis.
morphine a powerful analgesic
ergotamine tartarate used to treat migraine
indomethacin and phenyl butazone analgesic and anti-inflammatory actions.
Systemic treatment by the rectal route is of particular value for
(a) treating patients who are unconscious, mentally disturbed or unable to tolerate oral
medication because of vomiting or pathological conditions of the alimentary tract.
(b) administering drugs, such as aminophylline, that cause gastric irritation, and
(c) treating infants.
PESSARIES
Pessaries are solid medicated preparations for introducing into the vagina, where they melt or
dissolve and exert a local action.
They are used mainly for vaginitis (inflammation of the vagina) and leucorrhoea (unpleasant
vaginal discharge). Vaginitis may be caused by a variety of micro-organisms or key old age. The
medicaments in official pessaries are:
acetarsol an antiprotozoal agent
di-iodohydroxyquinoline for yeast and protoplast infections.
lactic acid often useful in leucorrhoea
nystatin for yeast infections
crystal violet for various microbial infections.
TYPES OF SUPPOSITORIES:
1. Rectal suppositories
These are meant for introduction into the rectum for their systemic effect. They are tapered at
one or both ends and usually weigh about 2 gm. The rectal suppositories meant for children are
smaller in size and weight is 1 gm.
2. Vaginal suppositories:
They are meant for introduction into vagina.
They are larger than rectal suppositories and vary in weight from 3 to 6 gm or more.
They may be conical, rod-shaped or wedge shaped.
They a re exclusively used for their local action on vagina.
3. Urethral Suppositories (or Urethral bougies)
They are meant for introduction into the urethra.
Their weight varies from 2 to 4 gm and length from 2 to 5 inch. Urethral suppositories are very
rarely used.
4. Nasal suppositories (Nasal bougies)
They are meant for introduction into nasal cavity.
They are similar in shape to urethral bougies.
Their weight is about 1 gm and length 9-10 cm.
They are always prepared with glycero-gelatin base.
5. Ear cones (aurinaria)
They are meant for information into the ear.
Generally theobroma oil is used as a base.
They are prepared in an urethral bougies mould and cut according to the required size.
Properties of an Ideal Suppositories Base
1. It should melt at body temperature or dissolve or disperse in body fluids.
2. It should release any medicament readily.
3. It should keep its shape when being handled.
4. It should be non-toxic and non-irritant to the mucous membrane.
5. It should be stable on storage.
6. It should be compatible with any added medicament.
7. It should be stable if heated above its melting point.
8. It should be easily moulded and should not adhere to the mould.
9. It should be easily mouldable by pouring or cold compression.
[Since it is not possible to get all the above mentioned qualities in a single base, so a combination
of bases is used to get a product of required qualities. A number of patent improved suppository
bases are available. Most of these are mixtures of fats, waxes and/or esters in specific proportions
according to the desired qualities of the product to be obtained. Glycerogelatin and polyethylene
glycols are being widely used as suppository bases, though theobroma oil is extensively used in
extemporaneous preparations but it is losing its importance because it is unstable to heat and has
undesirable physical properties.]
Types of Suppository Bases
Suppository bases fall into two classes -
1. Fatty bases - these melt at body temperature.
2. Water-soluble or water miscible bases - these dissolve or disperse in rectal secretions.
3. Emulsifying bases
FATTY BASES
Theobroma oil (Cocoa butter)
It is a yellowish-white solid with a chocolate-like odour. It is a mixture of glyceryl esters of
stearic, palmitic, oleic and other fatty acids. Its valuable characteristics include -
Advantages:
(a) A melting point range of 30 to 36 0C; hence it is solid at normal room temperatures but melts
in the body.
(b) Ready liquefaction on warming and rapid setting on cooling.
(c) Miscibility with many ingredients.
(d) Blandness i.e. does not produce irritation.
Disadvantages:
(a) Polymorphism
When melted and cooled it solidifies in different crystalline forms, depending on the temperature
of melting, rate of cooling and size of the mass. If melted at not more than 360C and slowly
cooled it forms stable beta crystals with normal melting point, but if over-heated it may produce,
on cooling, unstable gamma crystals, which melt at about 150C, or a-crystals, melting at about
200C. These unstable forms eventually return to the stable condition but this may take several
days and meanwhile, the suppositories may not set at room temperature or, if set by cooling, may
remelt in the warmth of the patients home.
This lowering of the solidification point can also lead to sedimentation of suspended solids and
delay in issuing the product to the patient. Consequently, great care must be taken to avoid over-
heating the base when making theobroma oil suppositories.
(b) Adherence to mould
Because theobroma oil doesnt contract enough on cooling to loosen the suppositories in the
mould, sticking may occur, particularly if the mould is worn. This is prevented by lubricating the
mould before use.
(c) Softening point too low for hot climates
To raise the softening point, whit beeswax may be added to theobroma oil suppositories intended
for use in tropical and subtropical countries.
(d) Melting point reduced by soluble ingredients
Substances, such as chloral hydrate, that dissolve in theobroma oil, may lower its melting point to
such an extent that the suppositories are too soft for use. To restore the melting point, a controlled
amount of white beeswax may be added.
(e) Slow deterioration during storage
This is due to oxidation of the unsaturated glycerides.
(f) Poor water absorbing capacity
This fault can be improved by the addition of emulsifying agents.
(g) Leakage from the body
Sometimes melted base escapes from the rectum or vagina. This is most troublesome with
pessaries because of their larger size, and therefore, these are rarely made with theobroma oil.
(h) Relatively high cost
Synthetic fats
As a substitute of theobroma oil a number of hydrogenated oils, e.g. hydrogenated edible oil,
arachis oil, coconut oil, palm kernel oil, stearic and a mixture of oleic and stearic acids are
recommended.
N.B. Synthetic suppositories bases are by hydrogenation and subsequent heat treatment of
vegetable oils such as palm oil and arachis oil. The oils are generally esters of unsaturated fatty
acids. Hydrogenation saturates the unsaturated fatty acids and heat treatment splits some of the
triglycerides into fatty acids and partial esters (mono- and di-glycerides).
Advantages of these synthetic fats over theobroma oil:
1. Their solidifying points are unaffected by overheating.
2. They have good resistance to oxidation because their unsaturated fatty acids have been
reduced.
3. Their emulsifying and water absorbing capacities are good. [They usually contain a proportion
of partial glycerides some of which, e.g. glyceryl monostearate, are w/o emulsifying agents and,
therefore, their emulsifying and water absorbing capacity are good.
4. No mould lubricant is required because they contract significantly on cooling.
5. They produce colorless, odourless and elegant suppositories.
Disadvantages:
1. They should not be cooled in refrigerator because they become brittle if cooled quickly. Certain
additives e.g. 0.05 % polysorbate80, help to correct this fault.
2. They are more fluid than theobroma oil when melted and at this stage sedimentation rate is
greater. Thickeners such as magnesium stearate , bentonite and colloidal silicon dioxide, may be
added to reduce this.
WATER SOLUBLE AND WATER MISCIBLE BASES
Glycero-Gelatin base
This is a mixture of glycerol and water made into a stiff jelly by adding gelatin.
It is used for the preparation of jellies, suppositories and pessaries. The stiffness of the mass
depends upon the proportion of gelatin used which is adjusted according to its use.
The base being hydrophilic in nature, slowly dissolves in the aqueous secretions and provide a
slow continuous release of medicament. Glycerogelatin base is well suited for suppositories
containing belladonna extract, boric acid, chloral hydrate, bromides, iodides, iodoform, opium,
etc.
Depending upon the compatibility of the drugs used a suitable type of gelatin is selected for the
purpose. Two types of gelatins are used as suppository base
(i) Type-A or Pharmagel-A which is made by acid hydrolysis (has isoelectric point between 7 to 9
and on the acid side of the range behaves as a cationic agent, being most effective at pH 7 to 8. )
is used for acidic drugs.
(ii) Type-B or Pharmagel-B which is prepared by alkaline hydrolysis (having an isoelectric point
between 4.7 to 5 and on the alkaline side of the range behaves as an anionic agent, being most
effective at pH 7 to 8 ) is used for alkaline drugs
Disadvantages:
Glycerogelain base suppositories are less commonly used than the fatty base suppositories
because:
(i) Glycerol has laxative action.
(ii) They are more difficult to prepare and handle.
(iii) Their solution time depends on the content and quality of the gelatin and the age of the base.
(iv) They are hygroscope, hence must be carefully stored.
(v) Gelatin is incompatible with drugs those precipitate with the protein e.g. tannic acid, ferric
chloride, gallic acid, etc.
Soap-Glycerin Suppositories
In this case gelatin and curd soap or sodium stearate which makes the glycerin sufficiently hard
for suppositories and a large quantity of glycerin upto 95% of the mass can be incorporated.
Further the soap helps in the evacuation of glycerin.
The soap glycerin suppositories have the disadvantage that they are very hygroscopic, therefore
they must be protected from atmosphere and wrapped in waxed paper or tin foil.
Polyethylene glycol bases / Macrogol bases (Carbowaxes)
Depending on their molecular weight they are available in different physical forms.
Examples of Macrogol bases:
I
II
III
IV
Macrogol 400
Macrogol 1000
Macrogol 1540
Macrogol 4000
Macrogol 6000
Water
-
-
-
33
47
20
-
-
33
-
47
20
20
-
33
-
47
-
-
75
-
25
-
-
By choosing a suitable combination a suppository base with the desired characteristics can be
prepared.
Advantages:
1. The mixtures generally have a melting point above 420C, hence, does not require cool storage
and they are satisfactory for use in hot climate.
2. Because of the high melting point they do not melt in the body cavity, rather they gradually
dissolve and disperse, releasing the drug slowly.
3. They do not stick to the wall of the mould since they contract significantly on cooling.
EMULSIFYING BASES
These are synthetic bases and a number of proprietary bases of very good quality are available,
few of which are described below:
Witepsol
They consist of triglycerides of saturated vegetable acids (chain length C12 to C18) with varying
proportions of partial esters.
Massa Esterium
This is another range of bases, consisting of a mixture of di-, tri- and mono- glycerides of
saturated fatty acids with chain lengths of C11 to C17.
Massuppol
It consists of glyceryl esters mainly of lauric acid, to which a small amount of glyceryl
monostearate has been added to improve its water absorbing capacity.
Advantages of these bases over cocoa butter:
1. Over heating does not alter the physical characteristics.
2. They do not stick to the mould. They do not require previous lubrication of the mould
3. They solidify rapidly.
4. They are less liable to get rancid.
5. They can absorb fairly large amount of aqueous liquids.
PREPARATION OF SUPPOSITORIES
Suppositories are prepared by two processes: moulding (hot process or fusion process) and cold
compression.
Mould
Various types and sizes of suppository moulds are available. In the dispensary suppository moulds
with six or twelve cavities with desired shape and size may be used. For large scale production
moulds up to 500 cavities may be used.
Moulds are made up of stainless steel, nickel-copper alloy, brass, aluminium or plastic.
For cleaning, lubrication and removal of suppositories the mould can be opened longitudinally by
removing the screw in the centre of the plates.
The nominal capacities of the common moulds are 1g, 2g, 4g and 8g.
Calibration of the mould
The nominal capacity of a mould is not always correct. It will vary for different bases. Each
mould should be calibrated before use by preparing a set of suppositories or pessaries using the
base alone, weighing the products and taking the mean weight as the true capacity. This is
repeated for each base and the value is recorded for future use.
Displacement value
The volume of a suppository from a particular mould is uniform but its weight will vary because
the densities of medicaments usually differ from the density of the base with which the mould
was calibrated.
To prepare products accurately, allowance must be made for the change in density of the mass
due to added medicaments. For this purpose the displacement value of a medicament is taken
into consideration.
Definition: The number of parts of medicament (drug) that displaces one part by weight of the
base is known as the displacement value of that drug.
The following table lists the displacement values, with reference to theobroma oil, for substances
prescribed in suppositories and pessaries.
Table
Aminophylline
Bismuth subgallate
Castor oil
Chloral hydrate
Cinchocaine Hydrochloride
Cocaine hydrochloride
Hydrocortisone
1.5
3.0
1.0
1.5
1.5
1.5
1.5
Hydrocortisone acetate
Ichthammol
Morphine Hydrochloride
Phenobarbitone
Resorcinol
Tannic acid
Zinc oxide
1.5
1.0
1.5
1.0
1.0
1.0
5.0
Example:-
To prepare ten suppositories each containing 300 mg bismuth subgallate.
Mould size is 1 g.
Displacement value of bismuth subgallate is 3.
300 mg bismuth subgallate = 0.3 g bismuth subgallate
Displacement value of bismuth subgallate means 3 g bismuth subgallate displaces 1 g theobroma
oil.
Therefore, 0.3 g bismuthsubgallate will displace
(1 3) 0.3 = 0.1 g suppository base (i.e. theobroma oil)
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So the working formula for each suppository will be
Bismuth subgallate 0.3g
Theobroma oil 0.9g
Total 1.2g
Determination of Displacement value of a Medicament
The displacement value of a given medicament can be determined as follows:
Six suppositories are prepared with theobroma oil only (or other base) and their total weight =a
mg
Six suppositories are prepared containing 40% of the medicament and their total weight = b mg.
Amount of theobroma oil = c mg = 60% of b mg = 0.6 b mg
Amount of medicament = d mg = 40% of b mg = 0.4 b mg
The weight of theobroma oil displaced by d mg of medicament = (a - c) mg
Displacement value of the medicament = d / (a - c) mg
For example:
Weight of six unmedicated suppositories = 6g
Weight of six suppositories containing 40% of zinc oxide = 8.8 g
60Theobroma oil in this = --- 8.8 = 5.28 mg 100
40Zinc oxide in this = --- 8.8 = 3.52 mg 100
Theobroma oil displaced by 3.52 g of zinc oxide = 6 - 5.28 = 0.72 g
Therefore, the displacement value of zinc oxide = 3.52 / 0.72 = 5 (approximately)
Lubrication of Moulds
If the cavities of the mould are imperfect, i.e. poorly polished or scratched, it may be difficult to
remove the cocoa butter suppositories without damaging their surfaces unless a lubricant is used.
In this case an aqueous lubricant is used.
Glecero-gelatin base is sticky in nature hence they are lubricated with an oily lubricant e.g.
liquid paraffin or arachis oil.
It is unnecessary to lubricate the mould when synthetic fat or macrogol bases are used. The
products have better surface if the mould is dry.
For theobroma oil the following lubricating preparation is found to be useful:
Soft Soap 10 g
Glycerol 10 ml
Alcohol (90 %) 50 ml
The lubricant should be applied on a pad of gauze or muslin, or with a small fairly stiff brush.
To avoid excess lubrication the moulds are closed and kept inverted on a clean tile to drain out
excess lubricant.
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