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
Commercially available triglycerides from palm, palm kernel, and coconut oils with self emulsifying glyceryl monostearate and polyoxyl stearate
FATTIBASE
- Most frequently used in the preparation of vaginal suppositories
- Gelatin (20%) glycerin (70%) Medication (10%)
- Tends to absorb moisture, has dehydrating effect and irritates tissue upon insertion (moist prior to insertion)
GLYCERINATED GELATIN BASE
components of glycerinated gelatin base
Gelatin (20%)
glycerin (70%)
Medication (10%)
Gelatin (60%)
glycerin (20%)
Medication (20%)
URETHRAL SUPPOSITORIES
- are polymers of ethylene oxide and water prepared to various chain lengths, molecular weighs and physical state.
- Having average molecular weights of 300, 400 and 600 clear, colorless liquids, while those with molecular weighs of 600-1000 are semisolids
- Do not melt at body temperature but rather dissolved slowly in the body’s fluid
- Do not leak from orifices
PEG SUPPOSITORIES
oldest and simplest method, by rolling the suppository into the desired shape. The mass is then rolled into a cylindrical rod of desire length and diameter
MOLDING FROM A MELT
cold mass of the base containing the drug is compressed into suppositories by using compression into the desired shape
COMPRESSION
If Glycerinated gelatin will be used as the base. The mold should be lubricated with ______
MINERAL OIL
If suppositories are stored in extreme dryness it may lose ____ and become
LOSE MOISTURE
BECOME BRITTLE
If suppositories are stored in high humidity it will absorb moisture and tends to become ____
SPONGY
Cocoa butter should be stored inside the ____
REFRIGIRATOR
Glycerinated gelatin should be placed in ____
CONTROLLED ROOM TEMPERATURE
PEG should be placed in ____
USUAL ROOM TEMPERATURE
A single-use medicated transurethral system for the delivery of alprostadil to the male urethra
* Treatment of Erectile dysfunction
MUSE
- Adv: easy to manufacture; more stable; less messy
- Usually ovoid packed with inserter
- Prepared by tablet compression
- Lactose - filler/diluent
- Starch - disintegrant
- Polyvinylpyrrolidone - Dispersing agent
- Magnesium Stearate - lubricant
VAGINAL INSERTS
more preferred than vaginal suppositories
VAGINAL INSERTS / VAGINAL TABLET
- Administering topical drugs
- Cylindrical in shape ranging from 5 to 25g
- Packed in an applicator tube for topical administration and the applicator can be adjusted to continually exposed new fresh sticks
How to prepare: - Same as preparing supp except that melt is poured into the administering device or tube
- Local anesthetics, sunscreens, oncology products, antiviral and antibiotics
MEDICATION STICKS
Opaque bases inclues
WAXES
OILS
PEGS
Clear bases included
SODIUM STEARATE
GLYCERIN
SIZE
Rectal (adult)
32mm (1.5 in)
SIZE
Rectal (infant and children)
16mm
SIZE
URETHRAL MALE
3 - 6 mm
other name for vaginal suppositories
PESSARIES
other name for urethral male supp
BOUGIES
WEIGHT
Rectal (adult)
2g
WEIGHT
Rectal (infant and children)
1g
WEIGHT
Vaginal
5g
WEIGHT
Urethral Male
4g
long, cylindrical, one or both ends tapered
RECTAL ADULT
pencil-like shape
RECTAL INFANT & CHILDREN
globular, oviform, or cone shape
VAGINAL
slender, pencil-shaped
URETHRAL MALE & FEMALE
SIZE
Urethral Female
70mm
WEIGHT
URETHRAL MALE
4g
WEIGHT
URETHRAL FEMALE
2g
Latin name for suppositories
SUPPONERE
supponere means
TO PLACE UNDER
avoiding the breakdown of certain drugs that are susceptible to
GASTRIC DEGRADATION
the ____ of the rectum and vagina permits the absorption of many soluble drugs
MUCOUS MEMBRANE