| should remain solid at Room Temp but soften, melt or dissolve readily at body temp so that drug is fully available once inserted | Suppository bases |
| Superior base for treatment of anorectal disorders because of its emollient or soothing, spreading action. | Cocoa Butter |
| Nature of Suppository Bases | The base must be capable of melting, softening, or dissolving to release its drug for absorption.
The base should not irritate the mucous membranes of the rectum
Avoiding colonic response and prompt a bowel movement, eliminating the prospect of complete drug release and absorption.
No chemical and/or physical interactions between the medicinal agent and the suppository base, which may affect the stability and/or bioavailability of the drug.
Long-acting or slow-release suppositories are also prepared. Morphine sulfate in slow-release suppositories is prepared by compounding pharmacists. The base includes a material such as alginic acid, which will prolong the release of the drug over several hours . |
| CLASSIFICATION OF SUPPOSITORY BASES | 1 fatty or oleaginous bases.
2 water-soluble or water-miscible bases.
3 miscellaneous bases, generally combinations of Lipophilic and hydrophilic substances.
MNEMONICS: FAWAMIS |
| Ideal suppository bases: | 1 physically and chemically stable
2 nonirritating
3 non-toxic
4 nonsensitizing
5 compatible with variety of drugs
6 stable during storage
7 esthetically acceptable
8 It should contract slightly on cooling or release itself from 9 the mold with requiring mold lubricants
10 has wetting and emulsifying properties
11 high water number
12 can be manufactured by molding by hand, machine, 13 compression or extrusion
14 It should melt or dissolve in rectal fluids and should not bind |
| Most frequently employed, Cocoa butter
Hydrogenated fatty acids of vegetable oils ,i.e. such as palm kernel oil and cottonseed oil
Fat based compounds containing compounds of glycerin with the higher–molecular-weight fatty acids, palmitic and stearic acid, such as glyceryl monostearate and glyceryl monopalmitate | Fatty or oleaginous bases |
| Fat obtained from the roasted seed of
Theobroma cacao.
is an IDEAL BASE, melting just below body temperature and yet maintaining its solidity at usual room temperatures.
melts at 30˚C to 36˚C (86°F to 97°F),
Yellowish-white solid having a faint, agreeable
chocolate-like odor.
Chemically, it is a triglyceride (combination of
glycerin and one or different fatty acids). | (Fatty or Oleaginous Bases)
Cocoa Butter, NF |
| 1 Cocoa butter exhibits __, because of its triglyceride content | 1 polymorphism |
| Polymorphic Forms of Cocoa Butter | 1 Alpha crystals (metastable crystalline form)
2 Beta crystals (greater stability and higher melting point) |
| 1 Cocoa Butter solidifying agents
2 Substances such as __ have a tendency to lower the melting point of cocoa butter. | 1 Cetyl Ester Wax (20%) or Beeswax (4%)
2 phenol and chloral hydrate |
| 1 (triglycerides from palm, palm kernel, coconut oils with self-emulsifying glyceryl monostearate and polyoxyl stearate)
2 ( from coconut oil)
3 ( sat. FA C12-C-18 with partial glycerides) | 1 Fattibase
2 Weecobee bases
3 Witepsol bases |
| Water-Soluble and Water-Miscible Bases | 1 Glycerinated gelatin
2 Polyethylene glycols |
| It is for vaginal suppository - hydrophobic and causes irritation that's why it's seldom used as rectal supp
SLOWER TO SOFTEN and mix with the physiologic fluids than is cocoa butter and therefore provides a SLOWER RELEASE
have a tendency to absorb moisture as a result of the HYGROSCOPIC NATURE, they must be protected from atmospheric moisture
may have a DEHYDRATING EFFECT and irritate the tissues upon insertion.
most frequently used in preparation of vaginal suppositories, prolonged local action of the medicinal agent is usually desired. | Glycerinated gelatin |
| Glycerinated gelatin preparations | 1 dissolving granular gelatin (20%) in glycerin (70%) and adding water or a solution or suspension of the medication (10%). |
| __ in the formula for the suppositories minimizes this action; however, if necessary, the suppositories may be moistened with __ prior to insertion to reduce the initial tendency of the base to draw water from the mucous membranes and irritate the tissues. | Water
glycerol + water + gelatin = glycero-gelatin base |
| much more easily inserted than those with a cocoa butter base | Urethral suppository |
| Urethral suppositories Formula | the gelatin constitutes about 60%
the glycerin 20%
the medicated aqueous portion about 20% |
