SUPPOSITORIES Flashcards
- Solid dosage form in which one or more API’s are** dispersed** in a suitable base and molded into a suitable shape
- Are solid dosage forms intended for insertion into the body orifices where they melt, soften, or dissolve and exert localized or systemic effects
SUPPOSITORIES
Suppositories used for nausea and vomiting
ONDANSETRON SUPPOSITORY
Suppositories used for nausea, vomiting tranquilizers
PROCHLORPERAZINE SUPP
CHLORPROMAZINE SUPP
Suppositories used for opioid analgesic
OXYMORPHONE SUPP
Suppositories used for Migraine
ERGOTAMINE TARTRATE SUPP
Suppositories used for NSAID
HYDROCORTISONE SUPP
MESALAMINE SUPP
Suppositories used for Analgesic-antipyretic
OPIGESIC SUPP
PARACETAMOL
Physiologic Factors affecting absorption of drugs from rectal suppositories
inside the body
circulation route
colonic contents
ph & lack of buffering capacity of the rectal fluids
Physicochemical Factors affecting absorption of drugs from rectal suppositories
product that you are preparing
lipid water solubility
particle size
nature of the base
- Drugs absorbed in the rectum bypass the first pass effect in the liver instead of being absorbed into the general circulation
- Lower hemorrhoidal veins surrounding the colon receive the absorbed drug and initiate its circulation throughout the body, bypassing the liver
CIRCULATION ROUTE
receive the absorbed drug and initiate its circulation throughout the body, bypassing the liver.
LOWER HEMORRHOIDAL VEINS
also assists in the absorption of rectally administered drugs
LYMPHATIC CIRCULATION
Rectal fluids are essentially neutral in pH (7.2-7.4) and have no effective buffer capacity, the form in which the drug is administered will not generally be chemically changed by the rectal environment
pH & lack of buffering capacity
Rectal fluids are essentially ____ in pH
NEUTRAL
pH of rectal fluids
7.2 - 7.4
- It is more effective for a drug to absorbed systematically in an empty rectum than from one that is distended with fecal
- Diarrhea, tissue dehydration can influence the rate and degree of absorption at the rectal site
COLONIC CONTENT
- a lipophilic drug that is distributed in a fatty suppository base in low concentration has less of a tendency to escape to the surrounding aqueous fluid than does a hydrophilic substances in a fatty base.
- the more drug a base contains, the more drug will be available for absorption
LIPID WATER SOLUBILITY
- Smaller particle size the more readily the dissolution of the particle and the greater chance for rapid absorption
- It is preferable to avoid a too fine particle size because of the high increase of the viscosity of the melted excipient that can result from the use of excessively small particles and possible difficulties in flow during production
PARTICLE SIZE
- Base must be capable of melting, softening or dissolving to release its absorption
- If the base interacts with the drug to inhibit its release , drug reaction will be impaired or prevented
- If the base irritates the mucous membranes of the rectum, it may initiate a colonic response and prompt a bowel movement, eliminating the prospect of complete drug release and absorption
NATURE OF THE BASE
Most frequently used for rectal suppositories
FATTY BASE
oleaginous
3 classification of bases
FATTY OR OLEAGINOUS BASE
WATER SOLUBLE OR WATER MISCIBLE BASE
MISCELLANEOUS BASE
Mixture of oleaginous and Water soluble and water miscible
MISCELLANEOUS BASE
- Theobroma cacao
- Melts at 30-36°C
- Ideal rectal suppository base
- Disadvantage: bec of triglyceruide exhibit polymorphism=> crystals
- Must be slowly and evenly melted in water bath to avoid crystallization
- Phenol and chloral hydrate-lowers melting pt
- Cetyl esters wax (20%) or beeswax (4%) (product will not solidify anymore)
COCOA BUTTER
most commonly used fatty or oleaginous base
COCOA BUTTER
- triglycerides of saturated fatty acids (lauric acid)
- triglycerites of saturated fatty acids C12-C18 with varied portion of corresponding partial glycerides)
WITEPSOL BASES
Triglycerides derived from coconut oil
WECOBES BASES