5 - Suppository Products Flashcards
Comminution
vs
Trituration
Particle Size Reduction ONLY
Grinding & Mixing in mortar & pestle to reduce particle size
Electric grinder + Sieve
Type of Solvent that has
HIGH Dielectric Constant
HIGH Polarity
POLAR
Water
Type of Solvent that has
Medium Dielectric Constant
Medium Polarity
Semi-Polar
Alcohol or Glycol
Type of Solvent that has
Low Dielectric Constant
Low Polarity
Non-Polar SOlvent
Mineral oil / Benzene
Types of Ointment bases used in
Suppositories
Oleaginous Base
Absorption (W/O Base)
Water Soluble (PEG)
Aqueous (hydrophilic Gel, methylcellulose)
How to make a STICK?
Ointment Base + WAX
More WAX –> INCREASED MELTING POINT
(harder)
2 Types of Gels
dispersions in AQ vehicle rendered jellylike by addition of a gelling agent
consist of carbomers + cellulosics
Single Phase
Two-Phase = Magma
ex. Milk of Magnesia
Local Actions of Suppositories
Topical Effects
Emollient / Laxative
Anesthetic
Steroid
Systemic Action of Suppositories
Analgesic / Antipyretic
Epileptic
Anti-emetic/nausea
Asthma
Advantages of Suppositories
AVOID:
Stomach pH / enzyme degradation / FIRST PASS metabolism
good for irritating drugs / vomiting patients
Children / uncooperative patients
Physiologic Factors that affect Absorption
for suppositories
Colonic Content
Circulation
hemorrhoidal veins / lymphatic circulation
PHYSICOchemical Factors that affect absorption
for suppositories
neutral pH
no buffer capacity
partition coefficient
particle SIZE
composition of suppository base
3 main Requirements for suppository BASES
Melt / Dissolve @ body temp ~37*C
Inert
Relationship to ointment bases
Types of Suppository Bases
Oleaginous (fatty) = Cocoa Butter
MELT @ body temp
Water-Soluble / miscible = Glycerinated Gelatin
slowly dissolve –> slower release
W/O Emulsions / polyoxyl 40 stearate / witepson
Suppositories have the MOST RAPID RELEASE
when the drug is in base
Solubility + Hydrogen bonds are what affect Drug release of suppositories
INSOLUBLE
Phenobarb in PEG base (hydrophilic)
Sodium Phenobarb in hydroPHOBIC base
What is best in terms of Polarity & Solubility
of the Drug vs the Base?
Drug INSOLUBLE in base = RAPID RELEASE
Drug has OPPOSITE POLARITY vs the base = Rapid release
Solubility + Hydrogen bonds are what affect
Drug release of suppositories
Ways to Prepare Suppositories in Compounding
Molding
Melt + Mix + Pour –> cast iron molds / disposable molds
Compression
COLD compression on mass
Hand-Rolling + Shaping
OTC Suppository products generally have a
effect
LOCAL EFFECT
Ex. Hydrocortisone / Biscodyl
Mesalamine / Preparation H
Vasoconstrictor / Anesthetic / Protectants
What type of lubricant do you use for a suppository with a
(hydrophobic base) Oleaginous Base?
Suppository Compounding
GLYCERIN lubricant
(hydroPhilic)
Use lubricant of OPPOSITE polarity vs suppository base
What type of lubricant do you use for a suppository with a
PEG / Glycerinated Gelatin (HydroPhilic Bases)?
Suppository Compounding
MINERAL OIL lubricant
hydroPHOBIC
Use lubricant of OPPOSITE polarity vs the suppository base
What type of preperation do you use for a
low-dose drug?
Suppository Compounding
WEIGHT CALCULATION
based on density
What type of preperation do you use for a
HIGH DOSE drug?
Suppository Compounding
DOUBLE POUR preperation
-
Pour #1 -
-
Drug + 1/2 base, QS with remaining base
- COOL -> SCRAPE -> REMOVE
-
Drug + 1/2 base, QS with remaining base
- Pour #2 -
-
RE-MELT
- pour -> remove –> Dispense
-
RE-MELT
Vaginal Inserts/Tablets/Capsules
(Pessaries)
primarally LOCAL application
OBLONG SHAPE
typically use PEG (water-soluble) BASE
Applicator for insertion
Antibiotics / Antifungals / Spermatocides
Hormones / Contraceptive
WET VAGINAL TABLETS FIRST
Stability Considerations for Suppositories
Chemical / Physical
COOL STORAGE & AVOID HUMIDITY
Cocoa butter -> fridge / Glycerinated Gelatin –> cool place
PEG –> room temp
MICROBiological
Therapeutic / Toxicological
OTC Rectal Suppositories
LOCAL EFFECT =
Vasoconstrict / Anesthetic / Protectants
Anusol
Tucks
Preparation H
Prescription Rectal Suppositories
w/ LOCAL EFFECT
Bisacodyl
Hydrocortisone
Mesalamine
Prescription Rectal Suppositories
w/ Systemic Effect
Chlorpromazine / Prochlorperazine
HydroMORPHONE / OxyMorphone
Indomethacin
Promethazine
Type of OLEAGINOUS Base used in Suppositories
FATTY BLEND
Cocoa Butter
Type of Absorption Bases (hydroPhilic) used in Suppositories
Witepsol
Type of Water-Soluble Base / Water-Miscible Base use in suppositories?
(HydroPHOBIC)
PEG / Glycerinated Gelatin
Water-Miscible = Aqueous Base = Hydrophilic Base use GELATIN
