suppositories

G.ANILKUMAR M.PHARMACY(PHARMAC EUTICS)

contents
 Introduction  Classification

of suppositories  Advantages & disadvantages  Ideal properties of suppositories  Formulation of suppositories  Preparation of suppositories  Evaluation & packing of suppositories

Introduction
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Suppositories are the solid dosage forms meant to be inserted into the body cavities like rectum , urethra and vagina ,where they melt or soften to release the drugs and exert local or systemic effects.

Classification Of Suppositories
Rectal suppositories y Vaginal suppositories ( PESSARIES ) y Urethral suppositories ( BOUGIES ) y Nasal suppositories y Ear suppositories
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VAGINAL SUPPOSITORY
y y y y

They are also called as PESSARIES. SHAPE : globular, oviform or cone-shaped. Used occasionally. Intended for local effects like contraceptives, antiseptics in feminine hygiene

URETHRAL SUPPOSITORY
y y y y

Also called as BOUGIES . SHAPE slender, pencil-shaped. Intended for anti-bacterial or as a local anesthetic preparative for urethral examination. Occasionally used.

RECTAL SUPPOSITORY
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Intended for local action to relieve constipation, irritation, itching and inflammatory associated to hemorrhoids

Classification Of Suppositories Via Position Of Action

LOCAL EFFECT : y In case of pain, itching and hemorrhoid. y Locally active drugs include astringents, antiseptics, local anesthetics, vasoconstrictors, anti-inflammatory, soothing and protective agents and some laxatives. SYSTEMIC EFFECT : y Anti-asthmatics, anti rheumatics, anti-pyretic and analgesics
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ADVANTAGES
EASILY ADMINSTERED to children, old persons, to unconscious or sometimes to mentally unstable persons who cannot swallow the drug. y Convenient mode of administration for drugs which irritate the GIT, causing vomiting and destroyed in acidic ph of stomach and enzymes of GIT. y FASTER ONSET OF ACTION as compared to oral administration because absorption of drug through rectal mucosa directly reaches blood
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DISADVANTAGES
They are not acceptable by the patients. y The manufacturing process is difficult. y The drugs which cause irritation to the mucous membrane cannot be administered as suppositories. y Most of the suppositories should be stored at low temperature10-20c in a refrigerator , other wise the base gets liquified.
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IDEAL PROPERTIES OF SUPPOSITORY BASES

It should melt at body temperature or dissolve or disperse in body fluids. y It should release any medicament easily. y It should keep its shape when being handled. y It should be non-toxic and non-irritant to the mucous membrane. y It should be stable on storage and also stable if heated above its M.P.
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IDEAL PROPERTIES OF SUPPOSITORY BASES

It should be easily molded and should not adhere to the mold. y It should possess good wetting and emulsifying properties. y It should be able to incorporate a high percentage of water. y It should be chemically and physically stable
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Formulation of suppositories
1. 2. 3. 4. 5. 6. 7.

Bases Anti- oxidants Emulsifying agents Hardening agents Preservatives Thickening agents Plasticizers

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1. a. i. 

 

Bases :They are of two types Hydrophilic bases water-dispersible bases: properties: These are mixtures of non-ionic surfactants which are chemically related to polyethylene glycols. These are used alone or in combination with other types of bases Cellulose derivatives like methylcellulose sodium carboxy methylcellulose also come under this class. Eg; polyoxyethylene sorbitan fatty acid (tween)

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ii)Water soluble bases:

1.   

Glycero-gelatin This occurs as a gel .It is a mixture of gelatin, glycerol and water. According to B.P the composition of the base is gelatin-14%w/w ,glycerol-70%w/w To get a stiff mass, the quantity of gelatin should be increased to32%w/w and that of glycerol reduced to 40%w/w.

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b) Lipophilic bases
1.   

Coca butter: Properties: It is a natural triglyceride It can exist in more than one crystalline form i.e., it exhibits polymorphism It consists of mixture of oleic acid , palmitic acid , stearic acid .

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2.Anti2.Anti-oxidants
They protect the drug and the base from getting degraded due to oxidation. y Examples : i. Ethyl or propyl gallate ii. Ascorbic acid and its esters iii. Hydroquinone iv. Tocopherols
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3.Emulsifying agents:


  4. 

They increase the water-absorbing capacity of fatty bases. This makes it possible to include aqueous solutions in the formulation. Examples : polysorbates (tween 61) Wool alcohol ,wool fat Hardening agents: These are included in those formulations where the melting point of the base is decreased by the drug.

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These agents bring the melting point to normal. Examples : macrogols with high molecular weight. 5.Preservatives : They should be included in suppositories which contain water soluble bases to prevent microbial growth. Examples :methyl paraben , propyl paraben 6.Thickening Agents: They increase the viscosity of molten base and prevent sedimentation of suspended insoluble solids. Examples: Aluminium monostearate ,collodial silica ,magnesium stearate.

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7.Plasticizers :
They impart plasticity to the fatty base and makes it less brittle. y Examples : i. Castor oil ii. Glycerine or propylene glycol iii. Glycol iv. Tween 80 v. Tween 85
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