FORMULATION AND EVALUATION OF MEFENAMIC ACID SUPPOSITORIES
Abstract
Mefenamic acid, 2-(2, 3-dimethylphenyl) amino benzoic acid a potent non-steroidal anti-inflammatory agent (NSAIDS), used to treat pain, including menstrual pain. It also decreases inflammation and uterine contractions. Like other NSAIDs, mefenamic acid causes irritation, vomiting, nausea, anorexia, hematemesis (vomiting blood), haematuria (blood in urine) and diarrhea when given orally. Consequently, an alternate route of administration to avoid or minimize the above side effects is preferred in the form of suppositories. Mefenamic acid suppositories were prepared by using oleaginous bases (oil soluble) and aqueous bases (water soluble). All the prepared suppositories were evaluated for various physical parameters like weight variation, drug content, hardness and melting point. The suppositories prepared with water soluble bases were within permissible range of all physical parameters. In-vitro release study was performed by USP type I apparatus using phosphate buffer pH 7.4 as dissolution media. The dissolution data obtained were fitted to zero order, first order, Higuchi, and korsmeyer’s plot to understand the order and mechanism of drug release from the suppositories. In vitro drug released from water soluble bases (PEG) were found to be greater than that from oil soluble bases.
Keywords: Suppositories; Mefenamic acid; Cocoa butter; PEG 4000; PEG 6000; Glycero-gelatin
References
Mehta RM. Dispensing pharmacy, Vallabh prakashan, New Delhi; 2004: 246
El-Majri MA, Sharma RK, Formulation and evaluation of suppositories of piroxicam, Int J Drug Del. 2010; 2: 108-112.
Singh H, Kumar R, Singh P, Development of UV spectrophotometric method for estimation of mefenamic acid in bulk and pharmaceutical dosage form, Int J Pharmacy Pharm Sci. 2011; 3(2): 237-238.
http://en.wikipedia.org/wiki/Mefenamic_acid
Nair L, Bhargava HN. Comparison of in vitro dissolution and permeation of fluconazole from different suppository bases, Drug Develop Ind Pharm. 1999; 25: 691
Akala EO, Adedoyn A, Ogunbona FA. Suppository formulations of amodiaquine: In vitro release characteristics, Drug Develop Ind Pharm. 1991; 17: 303-7
Borne RF. Nonsteroidal anti-inflammatory agents. In: Williams AD, Lemke LT, editors. Foye's principle of medicinal chemistry. 5th ed. Lippincott William and Wilkins; 2002. 751-93.
Guttadauria M. The clinical pharmacology of piroxicam. Acta Obstet. Gynecol. Scand. Suppl. 1986; 138:11-13.
Mycek MJ, Harvey RA, Champe PC. Lippincott’s Illustrated Reviews: Pharmacology, 2nd ed. Lippincott -Raven Publishers, Philadelphia, 1997, 410.
Suleiman MS, Najib NM. Release of indomethacin from suppository bases. Drug Develop Ind Pharm. 1990; 16:707-17.
The British pharmacopeia, The Pharm. Press. London. 1993; 350, 624.
Coben LJ, Lieberman HA. Theory and practice of Industrial Pharmacy, Varghese publishing house, Bombay, 585-87.
Gold M, Nepuri M, Lawrence H. Suppository development and production. In: Lieberman HA, Riger MM, Banker GS. Pharmaceutical dosage forms: Disperse system, Marcel Dekker Inc. New York, 1996; 2(2): 473.
Verheyen S, Mechanism of increased dissolution of diazepam and temazepam from polyethylene glycol 6000 solid dispersions, Int. J Pharm. 2002; 249: 45-58.
Riegelman S, Chiou WL, Increasing the Absorption Rate of Insoluble Drugs. United States Patent US 4151273. 1978.
Betageri GV, Makarla KR, Enhancement of dissolution of glyburide by solid dispersion and lyophilization techniques. Int. J Pharm. 1995; 126: 155-160.
