SUPPOSITORIES Text Book Ansels Pharmaceutical Dosage Forms and

SUPPOSITORIES

Text Book • Ansel’s Pharmaceutical Dosage Forms and Drug Delivery Systems Tenth Edition Loyd V. Allen, Jr, Ph. D Howard C. Ansel, Ph. D • Section V

Suppositories • Definition: • Suppositories are solid dosage forms intended for insertion into body orifices (rectum, vagina, urethra) where they melt, soften, or dissolve and exert a local or systemic effect. • The derivation of the word suppository is from the Latin supponere, meaning “to place under, ” as derived from sub (under) and ponere (to place)

• An insert is a solid dosage form that is inserted into a naturally occurring (nonsurgical) body cavity other than the mouth or rectum, including the vagina and urethra. • Medication sticks are a convenient form for administering topical drugs.

Suppositories • They are used either rectally , vaginally and occasionally urithrally. • They are with different size and shapes. • It should be easily inserted into intended orifice without undue distention.

Suppositories • Rectal suppositories. • Vaginal inserts • Urethral suppositories • Alprostadil urethral suppository • Special type of suppositories

Action of suppositories Local effect: Rectal: Antihemorrhoidal and laxative Vaginal: Contraception, antiseptic and to combat an invading pathogens. • Urethral : Antibacterial or local anesthetic. • •

Suppositories • Systemic effect • Advantages over oral therapy • Disadvantages • Examples on drugs administered orally

• Some factors of drug absorption from rectal suppositories • Colonic Content • Circulation Route • p. H and lack of buffering capacity of the rectal fluids

• Physicochemical factors of the drug and suppository base affecting rectal absorption: • Lipid –water solubility • Particle size • Nature of the base

Suppository Bases • The properties of an ideal suppository base • Classification of suppository bases: • According to bases physical characteristics the bases can be classified into: • Fatty or oleaginous bases • Water-soluble or water-miscible bases • Miscellaneous bases

1. Fatty or oleaginous bases: • Fatty bases are perhaps the most frequently employed suppository bases which contains: 1. Cocoa Butter 2. Hydroginated fatty acids of vegetables eg cotton seed oil

• 3. Compounds containing compound of glycerin with high m wt fatty acids such as palmitic acids. eg glyceryl monostearate to achieve the desired hardness and desired quality of submitting to the tempreture of the body.

Cocoa Butter

2. Water-soluble or water-miscible bases • Main members are glycerinated gelatin and polyethylen glycol. • Preparation • The glycerol-gelatin base U. S. P. consisted of 20% w/w gelatin, and 70% w/w glycerol & water Q. S. to 100%.

• Polyethylene glycols • Polymers of ethylen oxide and water prepared to various chin length , molecular weight s and physical states. • Poloxamers (Pluronics) 3. Miscellaneous Base • Mixture of olieogenous and water soluble materials • Some are emulsion w/o type or capable of dispersing in aq. Fluids.

• Formulation variables: • • Physical state Particle size Solubility Viscosity Brittleness Volume contraction SPECIAL PROBLEMS

Preparation of Suppositories • Suppositories are prepared by three methods: • preparation by mold • Preparation by compression • Hand rolling and shaping

Hand rolling and shaping • With the ready availability of suppository molds of accommodating shapes and sizes, there is little requirement for today's pharmacist to shape suppositories by hand.

preparation by mold

Suppository Molds:

• Lubrication of the mold • Calibration of the mold • Preparing and pouring the melt

Manufacturing Suppositories

• Packaging and storage • Stability of suppositories • Physical Stability • Chemical Stability • Microbiological Stability • Informing and Educating the Patient

• Informing and Educating the Patient