Chapter 12 Suppositories, Inserts, and Sticks

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Section 1

Question Answer
Three reasons to use suppositories1. promote defecation 2. introduce drugs into the body 3. treat anorectal diseases
supponereto place under
insertsolid dosage form that is inserted into a naturally occurring (nonsur- gical) body cavity other than the mouth or rectum, including the vagina and urethra.
suppositorysolid dosage form in which one or more APIs are dispersed in a suitable base and molded or otherwise formed into a suitable shape for insertion into the rectum to provide local or systemic effect.
Rectal suppositories32 mm (1.5 inch) long, are cylindrical, and have one or both ends tapered
Vaginal Inserts/pessariesare usually globular, oviform, or cone shaped and weigh about 5 g when cocoa butter is the base.
Urethral inserts/bougiesslender, pencil-shaped suppositories intended for insertion into the male or female urethra
Male urethral suppositories 3 to 6 mm in diameter and approximately 140 mm long, although this may vary.When cocoa butter is employed as the base, these suppositories weigh about 4 g.
Female urethral suppositories are about half the length and weight of the male urethral suppository, being about 70 mm long and weighing about 2 g when made of cocoa butter.
Medication sticks cylindrical in shape and generally range from 5 to 25 g. They are generally packaged in an applicator tube for topical administration, and the applicator can be adjusted to continually expose new, fresh stick from inside the tube.

Section 2

Question Answer
First-pass effect:Avoiding, at least par- tially, the first-pass effect that may result in higher blood levels for those drugs subject to extensive first-pass metabo- lism upon oral administration.
Drug stabilityAvoiding the breakdown of certain drugs that are susceptible to gastric degradation.
Large dose drugs:Ability to administer somewhat larger doses of drugs than using oral administration.
Irritating drugs:Ability to administer drugs that may have an irritating effect on the oral or gastrointestinal mucosa when administered orally.
Unpleasant tasting or smelling drugs:Ability to administer unpleasant tasting or smelling drugs whose oral adminis- tration is limited.

Section 3

Question Answer
Fatty or Oleaginous Basescocoa butter,Fattibase,Polybase
Cocoa Butter, NFthe fat obtained from the roasted seed of Theobroma cacao
Water-Soluble and Water-Miscible BasesThe main members of this group are glycerinated gelatin and polyethylene glycols.
Glycerinated gelatin suppositoriesmay be prepared by dissolving granular gelatin (20%) in glycerin (70%) and adding water or a solu- tion or suspension of the medication (10%)
Polyethylene glycol suppositoriesdo not melt at body temperature but rather dissolve slowly in the body’s fluids.
PREPARATION OF SUPPOSITORIES(a) molding from a melt and (b) hand rolling and shaping.
Molding(a) melting the base, (b) incorporating any required medicaments, (c) pouring the melt into molds, (d) allowing the melt to cool and congeal into suppositories, and (e) removing the formed suppositories from the mold.
amelting the base,
bincorporating any required medicaments,
c pouring the melt into molds
dallowing the melt to cool and congeal into suppositories
eremoving the formed suppositories from the mold
Hand Rolling and Shaping accommodating shapes and sizes, there is little requirement for today’s pharmacist to shape suppositories by hand.
CHARACTERISTICS DUE TO NATURAL AGING AND THE CAUSESOdor/color/shape/size/surface condition/weight
OdorFungal contamination
ColorDiscoloration due to oxidation
ShapeIncorrect temperature during storage
Surface conditionWhitening
WeightLoss of volatile substances