Introduction to Suppositories
Objective
At the end of this lecture, student will be able to:
Discuss suppositories and its application
List advantages and disadvantages of suppositories
Explain suppositories types
List the ideal properties of suppositories bases
Introduction to Suppositories
q These are unit solid preparations which are intended for insertion into the body cavities like rectum, vagina, urethra, nose or ear cavity.
q They are normally used for local action or systemic absorption of the active ingredient.
q They usually melt, soften, or dissolve at body temperature and release the drug into body.
q They may contain one or more active medicaments
Applications of Suppositories
Mechanical action
Suppositories are extensively used as a mechanical aid to bowel evacuation which produce its action by either irritating the mucous membrane of the rectum (e.g. glycerol and bisacodyl) or by lubricating action or by mechanical lubrication.
q They have been used for a variety of conditions like hemorrhoids and local infections in vagina and rectum.
Local action
q The suppositories may be used for soothing e.g. zinc oxide, local anaesthetic- e.g. cinchocaine, benzocaine,astringents e.g. bismuth subgallate, hamamelis extract and tannic acid, anti-inflammatory e.g. hydrocortisone and its acetate.
q It is the alternated dosage form for drugs which have less bioavailability when it is taken orally
To provide systemic action
q Suppositories are convenient mode of administration of drugs which irritate the gastrointestinal tract, cause vomiting, destroyed by the hepatic circulation or destroyed in the stomach by pH changes, enzymes etc.
q Drugs having bad odour and taste can be used in suppository form.
q It is suitable for unconscious patients.
q It is suitable for drugs irritating effect in GIT.
q It is suitable for infants and old people who find difficulty in swallowing of drugs.
q It is suitable for the drugs which are destroyed by portal circulation.
Disadvantage of Suppositories
q The manufacturing process is more difficult as compared to other formulations.
q The drugs that irritate mucous membranes cannot be administrated by this form.
q Incomplete absorption may be obtained because the suppository usually promotes evacuation of the bowel.
q Suppositories are not suitable for patients suffering from diarrhea.
Types of Suppositories
1. Rectal suppositories
2. Vaginal suppositories (Pessaries)
3. Urethral Suppositories (Urethral bougies)
4. Nasal suppositories (Nasal bougies)
5. Ear cones (aurinaria)
Rectal suppositories
q These are meant for introduction into the rectum for their local or systemic effect.
q They are tapered at one or both ends and usually weigh about 2 g and for children are smaller in size with weight of 1 g.
q Rectal suppositories intended for localized action are most frequently used to relieve constipation or the pain, irritation, itching, and inflammation associated with hemorrhoids or other anorectal conditions.
Vaginal suppositories (Pessaries)
q They are meant for introduction into the vagina.
q They are larger than rectal suppositories and vary in weight from 3 to 6 g or more.
q They may be conical, rod-shaped, or wedge-shaped.
q They are exclusively used for their local action on the vagina.
q Localized effects are employed mainly as contraceptives, antiseptics in feminine hygiene, and as specific agents to combat invading pathogens.
Urethral Suppositories (Urethral bougies)
q They are meant for introduction into the urethra.
q Their weight varies from 2 to 4 g and length from 2 to 5 inch.
q Urethral suppositories are very rarely used.
Nasal suppositories (Nasal bougies)
q They are meant for introduction into the nasal cavity.
q They are similar in shape to urethral bougies.
q Their weight is about 1 g and their length 9-10 cm.
q They are always prepared with glycero-gelatin base.
Ear cones (aurinaria)
q They are meant for introduction into the ear.
q Generally theobroma oil is used as a base.
q They are prepared in a urethral bougies mold and cut according to the required size.
Properties of an ideal suppositories base
1. It should melt at body temperature or dissolve or disperse in body fluids.
2. It should release the medicament readily.
3. It should retain its shape during handling, transportation and storage.
4. It should be non-toxic and non-irritant to the mucous membrane.
5. It should be stable on storage.
6. It should be compatible with any added medicament or additives.
7. It should be stable if heated above its melting point.
8. It should be easily moulded and should not adhere to the mould.
9. It should not produce any pharmacological action.
Types of Suppository Bases
I. Fatty Bases (Oleaginous Bases)
Theobroma oil (Cocoa butter)
Synthetic fats
II. Water Soluble and Water Miscible Bases
Glycero-Gelatin base
Soap-Glycerin Suppositories
III. Emulsifying Bases
Witepsol
Massa Esterium
Massuppol
Ideal Suppository Base
• Melts at body temperature or dissolves in body fluids.
• Non-toxic and non-irritant.
• Compatible with any medicament.
• Releases any medicament readily.
• Easily moulded and removed from the mould.
• Stable to heating above the melting point.
• Easy to handle.
• Stable on storage.
Summary
q Suppositories are unit solid preparations which are intended for insertion into the body cavities like rectum, vagina, urethra, nose or ear cavity.
q Pessaries, Urethral bougies, Nasal bougies, aurinaria, Rectal suppositories are the types of suppositories.
Types of Suppository Bases
q Fatty Bases (Oleaginous Bases)
Theobroma oil (Cocoa butter)
Synthetic fats
q Water Soluble and Water Miscible Bases
Glycero-Gelatin base
Soap-Glycerin Suppositories
q Emulsifying Bases
Witepsol
Massa Esterium
Massuppol
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