DEVELOPMENT AND EVALUATION OF MESALAMINE GASTRO-RESISTANT TABLETS

Abstract

Oral administration is the traditionally preferred route of drug administration providing a convenient method of effectively achieving both local and systemic effects. The colon is believed to be a suitable site where both local and systemic delivery of drugs could be achieved. Colonic drug delivery has gained increased importance not only for localized treatment of several colonic diseases, mainly inflammatory bowel disease (Crohn’s disease, ulcerative colitis) and colon cancer. The site specific delivery of drugs (Drug targeting) to lower parts of GIT improve the efficacy of drugs by concentrating the drug molecules at the site of action and minimize systemic side effects and drug instability issues. Consequently, various strategies have been developed for CTDDS (Colon targeted Drug Delivery System), which includes prodrugs, pH and time dependent systems, Bacterial enzyme dependent CDDS, pressure controlled colonic delivery and osmotic controlled drug delivery. Mesalamine is available in a number of oral and rectal (topical) formulations including tablets, micropellets (granules), suppositories and enemas. Several oral formulations have been developed, most of which have been designed with various mechanisms to postpone the release of the release of the active mesalamine compound until reaching the terminal ileum/colon in order to prevent proximal absorption in the small intestine. The present study involves development and in‐vitro evaluation of Mesalamine gastro resistant under colon drug delivery system for improving bioavailability by prolonging gastric retention time with the help of pH dependent polymer, which prevent the premature release of mesalamine in the small intestine.