Formulation and Physicochemical Evaluation of Mesalazine Sustained-Release Gastro Resistant Tablets

Abstract

Introduction: Mesalazine (5-aminosalicylic acid) is often used as first-line treatment in patients with mild to moderate inflammatory bowel disease (IBD).Aims; Due to the low half-life of the drug, patients are forced to use the drug several times a day, so it seems necessary to prepare sustained-release forms of the drug for ease of use and to reduce the risks of forgetting to take the drug. Tablet pharmaceutical formulation, which is the most widely used pharmaceutical form, was selected in this study.Methods: Sustained-release mesalazine was prepared using water-soluble polymers and wet granulation method and was enterically coated using Eudragit S and L. Results: All kinds of formulations were made with different proportions of excipients, and finally, by examining the release process of the active ingredient mesalazine from the manufactured cores, the optimal core was selected as the final formulation in terms of the compliance of the release process of the active ingredient with the range approved by the pharmacopoeia, and control experiments physicochemistry was performed on them. After choosing the optimal core, the tablets were coated using Eudragit S and L and triethyl citrate in acetone and alcohol solvent, and the release process of the coated tablets in the acidic environment of 0.1 normal hydrochloric acid to ensure that the drug is not released in the acidic environment. The stability of the prepared tablets in terms of the amount of active ingredient mesalazine after 1 and 3 months was investigated by HPLC method and according to USP pharmacopoeia instructions and the results were reported. Discussion: The process of releasing the active ingredient from the sustained-release forms available in the pharmaceutical market of the country (Pentasa tablets and Mezantine capsules) was also investigated and compared with the final formulation in this treatise.