Formulation and Evaluation of Colon Targeted Drug Delivery of Mesalamine

Abstract

In this study, we report pectin–Chitosan compression coated core tablets of Mesalamine for colonic delivery. Each 150 mg core tablet contained Mesalamine and was compression coated using 100% pectin 1:1, 10 pectin:1 Chitosan, or 10 pectin :2 Chitosan, at coat weights as 400mg. Drug dissolution or system erosion or degradation studies were carried out in pH 1.2, 6.8,7.4 phosphate buffers using a pectinolytic enzyme. The system was designed based on the gastrointestinal transit time concept, under the assumption of colon arrival times of 6 h. It was found that pectin alone was not sufficient to protect the core tablets and Chitosan addition was required to control the solubility of pectin. The optimum Chitosan concentration was 1 and such system would protect the cores up to 6 h and after that under the influence of pectinase the system would degrade faster and delivering 5-ASA to the colon. The pectin– Chitosan (10:1) envelope was found to be a promising drug delivery system for those drugs to be delivered to the colon.