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Suppositories

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  #6 GLYCERIN SUPPOSITORIES Suppository - solid dosage form intended for insertion into the body orifices where they melt, soften, dissolvem and exert localizied or systemic effect. 5 TYPES OF SUPPOSITORIES 1. rectal - cylindrical or bullet shape - 32 mm (1 ½ inch) - 2g adult; 1g children Use: glyercin  –  laxative effect Sodium stearate  –  (Soap); solidifying agent    Cathartic  –  acts directly on colonic mucosa to produce normal peristalsis. Not appreciably affects the motility of small intestine    Relieve  pruritus ani  –  pain associated w/ hemorrhoids    constipation 2. urethral (bougies or inserts)  –   slender, pencil shaped. Male:  4g; 140 mm long, 3-6 mm diameter Female:  2g; 60-70 mm long Uses:   o   dilatation of uterus o   Anti-infective agent o   Erectile dysfunction o   Tx of local infection 3. vaginal (pessaries) - globular, oviform, cone-shaped; 5 grams. Caused by : Trichomonas vaginalis, Candida (Monilia) albicans, Haemophilus vaginalis    Estrogenic substances (dienestrol)  –  used to restore the vaginal mucosa to its normal state. Vaginal tablets (vaginal inserts) - easier to manufacture, more stable, and less messy.    Anti-infective    w/ homonal substances Tablet lubricant    –  Magnesium stearate Disintegrating agent  - startch    Use: anti-fungal    Anti-infective    Contraceptive (w/ spermicide) 4. otic (aural)  –   pencil-shaped 5. nasal (burginarium)  –   pencil-shaped CRITERIA FOR SUPPOSITORIES 1. melts at body temperature 2. firm at room temperature 3. yields at clear melt 4. inert and compatible with other agent 5. wetting and emulsifying 6. acid value (<0-2) 7. saponification value (200-245)  –  if it forms ester 8. non- irritating 9. iodine value (<7)  –  determines the unsaturation of double bonds (C=C) TYPES OF SUPPOSITORY BASES 1. tend to melt -    cocoa butter (theobroma oil)  –  polymorphic -   very good suppository base for rectal, seldom used in vagina and urethral -   tendency to lower melting point -   inability to absorb aqueous solution    witepool  –  C 12    –  C 18 (no polymorphism)    wecobee  –  only suppository base that came from coconut oil 2. tend to dissolve  –   polyethylene gylcol (PEG) - ↓ PEG –  liquid (300, 400, 600) - ↑ PEG –  semi-solid - ↑↑ PEG –  solid- wax ( > 1000)- clear colorless liquid METHODS OF PREPARATION 1. hand rolling  –   mixing and rolling in a pile tile. 2. compression - more elegant in appearnce -   very simple’ avoid sedimentation    -  not for large manufacturing -  mix -> supp. Compression device -> apply pressure -> cool 3. fusion method -   melting of all ingredients -   pour directly to mold -   freeze -   wrap in Aluminum foil

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Jul 23, 2017
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