What is suppository
Solid or semi-solid dosage forms of various sizes and shapes intended for insertion into the body orifices where they melt or dissolved and exert localised or systemic effects
Sub- under
Ponere- to place
3 types of shape and sizes of suppositories
-rectal suppositories -long, cylindrical, have one or both ends tapered
-vaginal suppositories (pessaries) -globular, oviform, conical shaped
-urthral suppositories (bougies) -slender, pencil-shaped suppositories
Types of suppositories
-rectal
-urethral
-nasal insertion
-vaginal
-aural (ear cones)
Local actions of suppositories
-Rectal suppositories -constipation, haemorrhoids, other anorectal conditions
-vaginal suppositories -feminine hygiene, vaginitis
-urethral suppositories -antibacterial, local anesthetic preparatory to urethral examination
Systemic action of rectal suppositories
For systemic effects, the mucous membranes of the rectum and vagina permits absorption of many soluble drugs and exerts effect elsewhere in the body
Advantages of suppositories
-useful in patients with nausea and vomiting
-when a drug can’t be swallowed
-when a drug may be decomposed or inactivated by pH or enzymes in the GIT
Disadvantages of suppositories
-Inconvenient
-absorption is irregular and difficult to predict
-formulation melts easily
What are rectal suppositories ?
-suppository that is inserted into the rectum for their systemic effect
-consist drug incorporated into the base Theobroma Glycero-gelatin
-available in various sizes
-weight about 1-2 grams
-cone or torpedo shaped
Local and systemic effect of rectal suppositories
Local:
-pain
-itching
-inflammation
Systemic:
-anti-histamines
-anti-rheumatics
-anti-pyretic
-analgesics
What are vaginal suppositories ?
-pessaries
-larger than rectal suppositories
-conical, rod, wedge shaped
-2-4 grams
Eg: vaginal tablet, capsules
Local action:
-contraceptives
-antiseptics in feminine hygiene
What are nasal suppositories (Burginarium) ?
-insertion into nasal cavity
-thin, cylindrical shape
-always prepared with glycero-gelatin base
-1.0 gram, 9-10cm long
What are urethral suppositories
-insertion into the urethra
-size and shape same as nasal supp
-2-4 grams
-rarely used
-intended for anti-bacterial or as local anaesthetic reparative for urethral examination
What are aural supp ?
-inserted into ear aka aurinaria or ear cones
-rarely used
-thin, long, cylindrical
-prepared using theobroma oil
Characteristics of a suitable base
-non-irritant
-melts at body temperature
-dissolves in body fluids
-solidifies quickly
-easily moulded
There are 3 types of suppository bases
- Oleaginous bases
•butterlike constituency and chocolate like odor
-eg: Theobroma oil or cocoa butter
-synthetic oleaginous materials like hydrogenated fatty acids or vegetable oils
-doesn’t exhibit polymorphism
-Potential problems: viscosity lower than theobroma oil, affects drug distribution, localised irritation - Water soluble or miscible bases
-types: glycerol-gelatin base and water-miscinle bases
-glycerol-gelatin is commonly used
-usually used for vaginal pessaries
-disadvantages: possibility of microbial contamination, osmosis may occur upon dissolving mucous, hygroscopic behaviour - Miscellaneous bases
-polyethylene glycols
What is theobroma oil and its major problems
A very old base, readily melts in the body, qualifies all ideal characteristics of bases
Major problems:
-don’t heat above 35°C
-prone to oxidation
-shrinks upon cooling and may stick to mould
How to prepare suppositories
- Melting of base on water / steam bath
- Add the drug (emulsify / suspend) into the molten bas
- Pour the mixture into pre-cooled moulds
- Allow to cool and congeal under refrigeration or freezing
- Remove the formed suppositories from the mould
Calibration weight formula
Total weight/ number of supp = calibration weight
What is calibration of the moulds
Determine the volume of the mould, the suppositories are carefully melted in a calibrated beaker
Preparation by compression
Small scale:
-mixture is prepared using warn mortar and pestle
-fill mixture into cavities
-press down using flat headed plunger
-remove screw under cavities
-eject suppository
Big scale (power operated machines used):
-mixture or mass placed in cylindrical A
-forced through D using B piston
-fused mass formed in E
-remove retaining stop plate F
-further pressure ejects suppositories
Advantages and disadvantages of compression method
Advantages:
-simple
-result suppository is more elegant
-avoid possibilities of sedimentation of the insoluble solids in the suppository base
Disadvantages:
-too slow for large scale operation
-aur entrapment in moulding for fat-type suppositories
-not suitable for glycerogelatin based suppositories
Packaging and storage for suppositories
-glycerin: tightly closed glass container
-prepared with cocoa butter: wrapped individually
-contain light sensitive: individual wrapper, metallic foil
-comercially: individually wrapped
-continuous strips
-cocoa butter: 30°C
Administration instructions for rectal suppositories
- Empty bowels
- Wash hands with soap and warm water
- Remove any foil or plastic wrapping from suppository
- Lubricate tapered end of the suppository with a small amount of K-Y jelly
- Either stand with one leg on a chair or lay one side with one leg straight and the other leg bent toward your stomach
- Separate buttocks to expose rectal area
- Gently push suppository into the rectum until it passes the sphincter
- Close your legs and sit still for about 15 minutes
- Wash hands with soap and warm water immediately
Administration instructions of vaginal suppositories
- Wash your hands with soap and warm water
- Remove any foil or plastic wrapping from suppository
- Place suppository in applicator
- Hold applicator by the opposite end from where the suppository is
- Either lay on your back with your knees bent or stand with your feet spread a few inches apart and your knees bent
- Insert applicator into the vagina
- Remove applicator
- Wash your hands with soap and warm water
