Design and In-Vitro Evaluation of Colon Targeted Delayed Release Tablets to Treat Ulcerative Colitis

Author(s): Gundati Sahithya*, K. Anie Vijetha, M. Sunitha Reddy And N. Vijaykumar3

Abstract: The aim of the present research investigation was to formulate and evaluate orally administered delayed release tablets of an anti-inflammatory drug for locally targeting the colon. Mesalamine is a BCS class IV drug intended for the treatment of Ulcerative Colitis. The developed product was designed to be pharmaceutically equivalent to Asacol HD - the Reference Listed Drug. The criticality of the formulation lies in hindering the API release in acidic environment and targeting to the colon. In the present study, the motto of delaying the drug release was achieved by incorporation of non-bio-degradable polymers with pH dependent solubility as enteric coating. Compatibility studies (40oC/75% RH) revealed that there were no physical as well as chemical interactions between drug and excipients. Trials of core tablets were carried out with varying proportions of binder (povidone), disintegrant (MCC) and lubricant (talc/Mg-stearate). The formulation with a similar release profile to that of coat removed innovator product was considered optimized (for core tablets). Coating trials were carried out with different proportions of enteric coating polymers, pore former, and plasticizer. A blend of equal proportions of Eudragit L 100 and Eudragit S 100 was found to be achieving the acid protection as that of innovator. The optimized coated formulation was charged to stability studies under accelerated storage conditions (40oC/75% RH) and the results were compared with initial results. It was concluded that the optimized formulation is pharmaceutically equivalent to innovator tablets and hence it shall be further evaluated for its bioequivalence.

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