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.Suppository A single dosage form. they should release medication very quickly. get local or systemic effect melt or dissolve inside the body. inserted into body cavities.
. Contract on cooling to allow easy withdrawal of suppository from mould. Not deteriorated or contaminating drug during storage. Easily manufactured by compression or molding. 8. Stable on storage. 10. Inert. Solidify rapidly to minimize sedimentation of dispersed solids.The ideal suppository base 1. 9. 4. 7. 3. Non-toxic. odor and drug release pattern. Has wetting and emulsifying properties. 5. Remain molten sufficient period to allow pouring into moulds. 2. Dissolve in mucous or melt quickly at body temp . 6. keep its shape during storage or handle does not change color.
miscible with other drug. melts 30-36ºC &solidify at 27 ºC or at room temperature depending on purity & type of oil its melt quickly &solidify quickly.Type of suppository bases: 1. Fatty base: melts at body temperature . its naturally occurring . chocolate like odor.example: Theobroma oil or( cacao butter) . .
. m. if melted suddenly &quickly at high temperature it will form unstable that melt at 15 ºC. it may form melt at 20 ºC. Low m. Stability problem. Adherence to the mould. Low water absorbance.The disadvantages of theobroma oil: Polymorphism: when melt &solidify form different crystal form depending on temp if its melt at low temp will form -polymorph (stable form). solved by surfactant.p can be raised by adding white bees wax or a synthetic fatty base Witepsol. Not suitable for warm countries. solved by white bees wax. solved by lubricant.p.
Mixture: ater & glycerin 70%. gelatin14% Gelatin can be increased up to 18% for warm countries .water soluble base: Dissolve in body fluid ex: Glycerogelatin base: dissolves in mucous secretions.
.Disadvantages of this base: laxative effect due to presence of glycerin Difficult to prepare Hygroscopic.
slowly dissolves in mucous secretions. low no. waxy solid. water miscible. its identified by a no. M. sterilized by heating.p & other properties. a different M. .irritant. non.WT. This base is non-toxic.Synthetic water soluble base: Macrogol= PEG Are poly condensation product of ethylene oxide & water. .WT can produce different bases of different m.After melting its miscible with body fluid & it's excellent solvent for many drugs. middle is semisolid & high no. M.WT viscous liq.
then rolled into a uniform cylinder with large spatula.METHODS OF PREPARATION 1. Cylinder cut into number of pieces rolled on one end to produce a conical. Hand Rolling It has the advantage of avoiding the necessity of heating the cocoa butter. . A plastic-like mass is prepared by triturating cocoa butter and active ingredients in mortar. The mass is formed into a ball in palm of hands.
On a small scale. The friction of the process causing the base to soften into paste.2. Compression Molding Compression molding mixed base and drug forced into special compression mold using suppository making machines. a mortar and pestle may be used (preheated mortar facilitate softening of the base) . The suppository base and other ingredients are combined by mixing.
4.Removing suppositories from mold.Dispersing or dissolving the drug in melted base. .Melting the base 2. 3.3.Allowing to congeal 5.The mixture is removed from heat and poured into a suppository mold. Fusion Molding Fusion Molding involves: 1.
. of a medicament that will displace one part of suppository base (normally theobroma oil).Displacement values The displacement value of a medicament is the number of parts or by weight gram.
PRACTICAL PHARMACEUTICAL CALCULATIONS Example Calculate the quantities required to make 10 theobroma oil suppositories (2 g mould) each containing 400 mg of zinc oxide (Displacement value= 4.7) .
85 g Therefore.7 g of theobroma oil= 0. So.7 g of zinc oxide would displace 1 g of theobromaoil1 g of zinc oxide would displace 1 ÷ 4.7 g of theobroma oil.Solution steps weight of zinc oxide = 400 mg × 10 = 4 g Weight of base for unmedicated suppositories = 2 g × 10= 20 g Displacement value of zinc oxide = 4.7 means that 4. the weight of base required to make medicated suppositories = 20 ± 0.15g grams . 4 g of zinc oxide will displace (4 × 1) ÷ 4.85 g =19.
Glycero-gelatin base has a density 1.2 times greater than theobroma oil.3) . each containing100 mg aminophylline (Displacement value = 1. Example Calculate the quantities required to make six glycero gelatin suppositories (4 g mould).
6) ÷ 1.55 g Therefore.6 g of aminophylline displace (1 × 0.25 g grams .8 g displacement value of aminophylline = 1.55 g = 28. the weight of base required to make medicated suppositories= 28.3 g of theobroma oil= 0.2 = 28.Solution steps weight of aminophylline = 100 mg × 6 = 600 mg or 0.2 of the glycero-gelatin base = 0.46 g of theobroma oil This means that the aminophylline would displace 0.8 g ± 0.46 g × 1.3 0.6 g Weight of base required for unmedicated suppositories = 4 g × 6 × 1.
. then its displacement value is not required when calculating the respective amounts of medicament and base required preparing the suppository.Medicaments included as a percentage w/w If a medicament is present in a suppository as a percentage w/w.
Content uniformity Melting range test Drug release test Fragility test Disintegration test.Testing of suppositories: Finished suppositories are routinely inspected for: Appearance. .
Lipid-water solubility of the drug 2.Degree of drug ionization 4. Factors influencing absorption of drug from suppository: Physiologic factors Physicochemical factors of the drug and the base: 1.Nature of the base .Particle size of the drug 3.