Preparation, Optimization And Evaluation Of Anti-Inflammatory, Analgesic And Inflammatory Bowel Disease Of Indomethacin Raft Forming Tablets

Abstract

This research focuses on developing a gastro-retentive floating tablet of Indomethacin, a non-steroidal anti-inflammatory drug (NSAID), using the raft-forming approach. The formulation incorporates Indomethacin as the active ingredient, with quercetin (a polyphenolic compound) and raft-forming polymers serving as adjuncts. Quercetin contributes additional anti-inflammatory and antioxidant properties, helping to protect against gastric damage. To optimize the raft-forming tablet, we employed a central composite design and response surface methodology using Design Expert® software (version 11.1.2.0). The experimental design incorporated three levels, two factors, and one process parameter. The experimental design utilized three levels, two factors, and one process parameter. Pectin (X1), Quercetin (X2), and wet granule thickness (X3) were selected as critical independent variables. Tablets were prepared using the wet granulation method and evaluated for weight variation, hardness, thickness, friability, drug content, floating lag time, and raft strength—all of which met standard specifications. The optimized formulation (F11) achieved a cumulative drug release of 89%. This formulation was further evaluated in vivo for anti-inflammatory activity using the carrageenan-induced rat paw edema model, analgesic efficacy via the tail-immersion test, and effectiveness in inflammatory bowel disease (IBD). Results demonstrated that the optimized raft-forming tablet significantly reduced paw edema compared to the inducer group. Analgesic testing showed that the formulation containing Quercetin produced a significant increase in reaction time (p < 0.0001) compared to the inducer group, with percentage inhibition comparable to standard Diclofenac sodium.