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Abstract

FORMULATION AND EVALUATION OF COLON TARGETED DRUG DELIVERY SYSTEM OF SULFASALAZINE

Shinde Vidya Sudhakar*, Shinkar Dattatraya Manohar, Saudagar Ravindranath Bhanudas

ABSTRACT

The nonsteroidal anti-inflammatory drugs (NSAIDs) are found to be potential chemopreventive agents of ulcerative colitis. Sulfasalazine, an NSAID with containing salicylate and Sulfapyridine was proved to be effective for pain and inflammation. In the light of this information, the present study was carried out to develop oral colon-targeting drug delivery system for sulfasalazine using xanthan gum as a carrier. Matrix tablets containing various proportions of xanthan gum were prepared by wet granulation technique using starch paste as a binder. The tablets were evaluated for hardness, drug content and were subjected to in vitro drug release studies. The amount of sulfasalazine released from the matrix tablets at different time intervals was estimated by a UV method. Xanthan gum matrix tablets released only 1-5% of sulfasalazine in the physiological environment of stomach and small intestine depending on the proportion of xanthan gum used in the formulation. When the dissolution study was continued in simulated colonic fluids (with rat caecal content medium), the matrix tablets containing higher amount of xanthan gum release rate gradually decreases of sulfasalazine after degradation by the colonic bacterial action. The matrix tablets containing 40 mg of xanthan gum released about 98.46% of sulfasalazine in simulated colonic fluids up to 24 hr containing rat caecal contents. The xanthan gum matrix tablets of sulfasalazine showed no change either in physical appearance, drug content or in dissolution pattern after storage at 40º C/RH 75% for 3 months. Differential scanning calorimetry (DSC) studies indicated no possibility of interaction between sulfasalazine and xanthan gum/other formulation excipients.

Keywords: Colon targeted, enteric coating, sulfasalazine, xanthan gum, rat caecal content.


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