SUPPOSITORY BASE, CLASSIFICATION, IDEAL PROPERTIES OF SUPPOSITORY BASE, THEOBROMA OIL, COCOA BUTTER,

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  • เผยแพร่เมื่อ 14 ต.ค. 2024
  • SUPPOSITORIES,
    Suppositories are semi-solid dosage forms intended for insertion into body orifices
    Like rectum, vagina, urethra where they melt, soften, or dissolve at body temperature and provide a local or systemic effect to treat various diseases.
    WHAT IS SUPPOSITORIES BASE?
    Suppository base excipients are used in the manufacture of suppositories.
    They can be hydrophobic or hydrophilic.
    Suppositories should melt at just below body temperature 37°C
    which allows for erosion of the dosage form and release of the API.
    Hard fat suppository bases melt at approximately body temperature.
    PROPERTIES OF IDEAL SUPPOSITORY BASE
    1. Melts at body temperature or dissolves in body fluids.
    2. Non-toxic and non-irritant.
    3. Compatible with any medicament.
    4. Releases any medicament readily.
    5. Easily mouldedand removed from mould.
    6. Stable to heating above the melting point.
    7. Easy to handle.
    8. Stable on storage.
    PROPERTIES OF IDEAL SUPPOSITORY BASE
    For fatty bases the following additional specifications are required:
    1. “Acid value” is below 0.2
    2. “Saponification value” ranges from 200 to 245
    3. “Iodine value” is less than 7
    4. The interval point and solidification point is small.
    5. They does not produce irritation.
    SUPPOSITORY BASE CLASSIFICATION
    Classification of suppository bases
    1. Fatty bases (Oleaginous Base)
    they melt at body temperature.
    Cocoa Butter (Theobroma oil)
    Synthetic Fats
    Hydrogenated oil
    2. Aqueous base (Water-soluble or water miscible base)
    Glycero-gelatin
    Soap glycerin
    Macrogol (PEG)
    they dissolve or disperse in rectal secretions.
    3. Emulsifying bases - they emulsifies small amount of aqueous solution of drug.
    Massa esterinum
    Witepsol
    Massupol
    THEOBROMA OIL (COCOA BUTTER)
    Obtain from the seed of Theobroma cocoa.
    It is a yellowish-white solid with an odour of chocolate and is a mixture of glyceryl esters of different unsaturated fatty acids.
    It is a mixture of
    Glyceryl esters of stearic,
    Palmitic, oleic like fatty acid
    Dissolve at body temperature
    Theobroma oil (cocoa butter) Advantages
    A melting range of 30 - 36°C
    Solid at room temperature but melts at the body temperature
    Very stable & chemically inert.
    Miscible with many ingredients.
    Non-irritating.
    Ready liquefaction on warming
    Rapid setting on cooling.
    Theobroma oil (cocoa butter) Disadvantages
    1. Polymorphism
    2. Adherence to the mould
    3. Melting point reduced by soluble ingredients
    4. Rancidity on storage
    5. Poor water-absorbing ability:
    6. Leakage from the body:
    7. Expensive
    1. Polymorphism (more than one crystalline forms)
    Cocoa butter has three polymorphs
    1. α-crystals (unstable, Melting point 20°C),
    2. β-crystals (stable, Melting point 36°C)
    3. γ-crystals (unstable, Melting point 15°C).
    When melted and cooled it solidifies in different crystalline forms, depending on the temperature of melting, rate of cooling and size of the mass.
    1. Polymorphism (more than one crystalline forms)
    If melted at not more than 36°C and slowly cooled, it forms stable beta crystals with normal melting point.
    If over-heated & then cooled, it produces
    Unstable gamma crystals which melt at about 15°C OR Alpha crystals melting at 20°C so care must be taken during melting
    Unstable forms return to stable condition after several days.
    Cocoa butter must be slowly melted over a warm water bath to avoid the formation of the unstable crystalline form
    This lowering of the solidification point can also lead to sedimentation of suspended solids.
    Consequently, great care must be taken to avoid over-heating the base when making theobroma oil suppositories.
    2. Adherence to the mould:
    Cocoa butter does not contract sufficiently on cooling to loosen the suppositories in the mould.
    Sticking may be overcome by adequate lubrication.
    3. Melting point reduced by soluble ingredients:
    Phenol and chloral hydrate have a tendency to lower the melting point of cocoa butter.
    So, solidifying agents like beeswax (4%) may be incorporated to compensate for the softening effect of the added substance.
    4. Rancidity on storage:
    Due to the oxidation of unsaturated glycerides.
    5. Poor water-absorbing ability:
    Improved by the addition of emulsifying agents.
    6. Leakage from the body:
    Sometimes the melted base escapes from the rectum or vagina, so it is rarely used as a pessary base.
    7. Expensive and Relatively high cost (150 g MRP:Rs 400-500)
    #base_use_in_suppository
    #ideal_properties_suppository_base
    #pharmaceutics
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