Formulation development, optimization and study on drug release kinetics of Eudragit® L100-HPMC E15 LV mixed film-coated colon- targeted Mesalamine tablets
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Abstract
the drug with microcrystalline cellulose and other ingredients.The fabricated Mesalamine tablets were coated with Eudragit L100 polymer and HPMC E 15 LV. The fluctuation in colonic pH conditions during inflammatory bowel disease and the nature of less fluid content in the colon may limit the expected drug release in the colon. Addition of HPMC E 15 LV may control this problem by hydrophilic nature and excellent film-forming characteristics like ductility and elasticity.
The different batches of Mesalamine tablets (FM1-FM5) were coated with increasing concentration of Eudragit L100 and HPMC E 15 LV. The coating was given up to 8% TWG(Total weight gain) of the uncoated tablet. Drug release studies were conducted in different pH conditions in the presence of rat ceaecal contents. The different buffer conditions were chosen to mimic the pH changes in the terminal part of the ileum as well as in the colon. The drug release profile was analyzed for colon-targeting performance in vitro. The release profile of the tablets indicates that the drug release was retarded in the tablet by film coating. The addition of HPMC E 15 LV ensures the channels for allowing colonic fluids to penetrate into the core and subsequent drug release at the target site. The kinetics of the drug release also evaluated the release pattern that was best fitted with Higuchian release. The results of the mechanism of release revealed that drug release was found to be a complex one with diffusion, erosion and swelling.
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