Formulation and Evaluation of Enteric Coated Matrix Tablets of Mesalamine for Inflammatory Bowel Disease

Abstract

Mesalamine is a gold standard anti-inflammatory drug used to treat inflammatory bowel illnesses. It's usually used to treat and keep Ulcerative Colitis in remission in mild to moderate cases. Mesalamine is rapidly cleared from circulation after being consumed orally, with an elimination half-life of only one hour. Oral intake of delayed or slow released matrix formulations can acquire therapeutic concentration in the intestines. The goal of this study was to use guar gum as a carrier to develop colon-specific delivery methods for mesalamine. The matrix tablets were made using the direct compression process, which is today regarded as a cost-effective and straightforward manufacturing method. Dip coating was used to coat the tablets with varied concentrations of Eudragit L100 polymer. Tablets were studied in vitro in a variety of dissolution solutions, including 0.1 N HCl (pH 1.2), phosphate buffers pH 6.8 and 7.4, and others. The optimized formulation was subjected to swelling tests. All of the formulations' physicochemical parameters were confirmed to be in line with pharmacopoeial norms. All formulations were subjected to stability tests in accordance with ICH recommendations. The tablets coated with Eudragit L100 (20 percent w/v) had a sustained release of 78.39 percent over 12 hours, while the uncoated tablets released the medication in 9 hours. Tablet stability tests revealed that under accelerated and room temperature storage settings for 6 months, there was reduced degradation. In the colon, the enteric-coated Eudragit L100 coated matrix tablets of mesalamine demonstrated promising site-specific drug delivery.
 Keywords: Mesalamine, Guar gum, Eudragit L100, Direct compression, Inflammatory bowel illnesses