Abstract

FORMULATION, OPTIMIZATION AND EVALUATION OF MESALAMINE TIMED RELEASE DOSAGE FORM

Karthik Rajkumar*, Rajagopal Kumaravelrajan and Gokul Kanmani

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Abstract

Mesalamine, a medication commonly used to treat inflammatory bowel illnesses, poses difficulties in oral administration due to its pHdependent release profile and restricted absorption in the gastrointestinal tract. Pelletization is a viable strategy to addressing these concerns because it allows for controlled release and increased bioavailability. Mesalamine pellets were manufactured via extrusionspheronization and tested for a variety of physicochemical qualities. Different formulations were created using varying amounts of mesalamine, microcrystalline cellulose, and hydroxypropyl methylcellulose. The pellets were evaluated for micrometric characteristics and in vitro drug release profiles under simulated gastrointestinal circumstances. The effect of formulation characteristics on drug release kinetics was investigated using mathematical models. This mesalamine pellets, which were rigorously tuned using a 32-factorial design, were assessed for various responses, including drug release. The improved formulation demonstrated drug release over 8 hours, resulting in a delayed therapeutic impact when compared to immediate-release formulations. Finally, the manufactured mesalamine pellets revealed promising properties for delayed release, which could improve patient compliance and therapeutic outcomes in the treatment of inflammatory bowel illnesses.

Keywords: Mesalamine, Pellets, Extrusion-Spherization, Inflammatory Bowel Disease.