Suppositories: A semisolid substance for introduction into the rectum, vagina, or urethra, where it dissolves. it may be used to stimulate a bowel movement, but often serves as a vehicle for medicines to be absorbed. It commonly shaped like a cylinder or cone and may be made of soap, glycerinated gelatin, or cocoa butter(oil of Theobroma).
Ideal properties of suppository bases:
- It should melt at body temperature or dissolve or disintegrate in body fluids.
- Higher melting point bases may be necessary for eutectic mixtures. Addition of balsams to suppositories is intended for use in tropical climates.
- It should be inert, no-irritating and non-sensitizing
- It should be release the medicament readily.
- It should be compatible with a broad variety of drugs.
- It should be stable on storage and transportation.
- It should have wetting and emulsifying properties.
- It should be able to incorporate a high percentage of water in it i.e., a high water number.
- It should shrink sufficiently on cooling to release itself from mold and should be moldable by pouring or by cold compression.
- Fatty bases should have acid value below 0.2, saponification value in between 200to 245, iodine value less than 7 and a small range between the melting the melting and solidification points.
Suppository bases can be classified into three categories:
- Fatty bases(oleagenious bases)
- Water soluble or miscible bases
- Emulsifying bases.
1. Fatty bases:
- Theobroma oil: It is yellowish white solid obtained from crushed and roasted seeds of Theobroma cocoa.
- It is also known as cocoa butter with melting point of 30-35 C
- It is a mixture of glyceryl esters of stearic acid, oleic acid. It melts at body temperature and release the medicament for rapid absorption
- It readily liquefies on warming and quickly settles on cooling.
Disadvantages
- It shows polymorphism.
- It become rancid and melts in warm weather.
- It has a tendency to stick to the sides of mould when solidified.
- Leakage from body cavities on melting takes place.
- Relatively costly.
- Immiscible with body fluids.
Emulsified Theobroma oil:
- Used as a base when large quantity of aqueous solutions are to be incorporated.
- 5% glyceryl monostearate, 10% lenette wax, 2-3% cetyl alcohol, 4% bees wax and 12% spermaceti is recommended in the preparation of emulsified theobroma oil suppositories.
Hydrogenated oils:
- They are obtained by hydrogenation of various vegetable oils such as arachis oil, cotton seed oil etc.
- It is used as a substitute for theobroma oil because it has many advantages as.
- Resistant to oxidation.
- Lubrication of mould.
- Overheating doesn't affect the solidifying point.
- Colorless, odorless and elegant suppositories are formed.
- Emulsifying and water absorbing capacities are good.
2. Water miscible and water soluble bases:
a)Glycerogelatin base:
- It is a mixture of glycerin and water which is made stiff by adding gelatin.
- The suppositories prepared by this are translucent, dissolve or disperse slowy in the body cavity and release the medicament.
- To avoid incompatible reactions Type A which is acidic in nature are used for acidic drugs having iso-electric point(7-9).
- Type-B which is alkaline in nature and used for alkaline drugs having iso-electric point(4.7-5)
Disadvantages:
- Gelatin is incompatible with many drugs.
- There are more chances of bacterial growth.
- Solution time depends on the content and quality of gelatin used.
- They are more difficult to prepare and handle.
b)Polyethylene glycol:
- They are called as carbowaxes or polyglycols or macrogals.
- They have molecular weight less than 1000 are liquids and more than 1000 are wax like solids.
Advantages:
- Chemically active .
- Non irritant.
- No bacterial growth.
- Inert substances.
- Have clean and smooth appearance.
Disadvantages:
- Hygroscopic.
- Incompatible with tannins, phenols etc.
- Supersaturation and forms crystals and fracture on storage.
3.Emulsifying bases:
a)Witepsol:
- Consist of triglycerides of saturated vegetable acid with various percentage of partial esters.
- Bees wax is added in hot climates.
- Suppositories should not be cooled rapidly to prevent from brittle and fractures.
b)Massa estarnium:
- Mixture of mono, di and triglycerides of saturated fatty acids.
- They are also called as a deps solidus.
c) Massuppol:
- It consist of glycerol esters of lauric acid to which small amount of glyceryl monostearate has been added to improve it water absorbing capacity.
Advantages:
- Solidify rapidly.
- Non irritant.
- Lubrication of mould is not required.
- Over heating has no effect on base.
- Absorb huge amount of water.
Disadvantages:
- Should not be could rapidly.
- Not very vicious on melting.
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