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Pharmaceutics
Suppositories, Pessaries, Inserts
34
Biology
Graduate
02/26/2012

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Term
suppository
Definition
-solid dosage forms intended for a BODY ORIFICE where they melt, soften, or dissolved
-localized or systemic
Term
pessaries
Definition
-suppositories for vaginal use
Term
vaginal inserts usually prepared by
Definition
tablet compression
Term
rectal suppository characteristics
Definition
-usually 1.5 inches
-drug is 0.1% to 40%
Term
local effect
Definition
-pain and itching-hemorrhoids
Term
systemic effect
Definition
-many drugs
-analgesics, nausea/vomiting
Term
rectum anatomy and physiology
Definition
-15-20cm
-3ml mucous
-drug passes though rectum wall to vascular area of submucosal wall
-drug can be carried by 3 veins
Term
superior rectal vein empties into
Definition
portal vein
Term
middle/inferior rectal vein empty into
Definition
-general circulation
-most common
-AVOID first pass
Term
desired characteristics for suppository bases
Definition
-solid at room temp
-pourable when prepared
Term
types of supp bases
Definition
-oleaginous
-water soluble
-misc.
Term
fatty or oleaginous base
Definition
-cocoa butter
-polymorph
-beta is preferred
Term
cocoa butter substitues
Definition
from vegetable oils
Term
water soluble bases
Definition
-glycerol
-macrogels (PEG)
Term
glycerol
Definition
-gelatin or soap base
-used for laxative purpose and vaginal application
-slower to soften and mix than oil bases (dissolve)
-tendency to absorb moisture
-may moisten with water before insertion
Term
macrogels (PEG)
Definition
-have higher melting points
-dissolve rather than melt
-slower release of drug
-no refrigeration needed
Term
misc bases
Definition
-mixture of fatty and water bases
-must be emulsions
-Poloxyl 40 stearate (surfactant)
Term
fat soluble bases
Definition
-drug diffuses slowly
-base melts quickly
Term
water soluble bases
Definition
-drug diffuses quicker
-base dissolves slowly
Term
prep of supp
Definition
-compression
-hand rolling/shaping
-fusion/melt molding
Term
compression
Definition
-forces mass of base and drug into a mold
-friction in mixing causes base to form paste like consistency
-good for heat labile drugs, insoluble drugs
-no risk of drug settling
Term
hand rolling
Definition
-historic preparation, obsolete with readily available molds
-avoids head and molds
Term
fusion or melt molding
Definition
-most common
-5 steps
-melt the base
-incorporate drug
-pour into mold
-cool
-remove from mold
Term
types of molds
Definition
stainless steel, aluminum, brass, plastic
Term
molding
Definition
-lubrication of the mold
-mineral oil or equivalent
-needed for glycerated gelatin supp
-PEG,cocoa butter not needed?
-
Term
DF
Definition
weight of drug/weight of base displaced
Term
vaginal supp
Definition
-weight up to 5 g
-some systemic drug absorption for vaginal wall
-decreased first pass effect
-vaginal epithelium is significantly impermeable to drugs
-most LOCAL
Term
vag supp common base
Definition
-PEG
-may add surfactants and parabens
Term
most common vag supp
Definition
progesterone
Term
urethral supp
Definition
-cocoa butter is base
-female-50mm 2g
-male-125mm 4g
Term
MUSE
Definition
-medicated urethral system for erection
Term
micropellet
Definition
drug and PEG
Term
cocoa butter supp must be
Definition
refridgerated
Term
PEG refriderater?
Definition
no
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