FORMULATION AND EVALUATION OF PH-DEPENDENT EUDRAGIT S-100 COATED MATRIX TABLETS OF TOFACITINIB CITRATE FOR COLON TARGETED DRUG DELIVERY i

The goal of the current study was to create and assess pH-dependent Eudragit S-100 coated matrix tablets containing tofacitinib citrate for colon-targeted medication delivery. Using chitosan and Carbopol 940 P as release-retarding polymers and citric acid and sodium bicarbonate as gas-generating agents, matrix tablets were made by direct compression. Bulk density, tapped density, compressibility index, Hausner ratio, hardness, thickness, friability, weight variation, drug content, floating lag time, and total floating duration were among the pre-compression and post-compression parameters that were assessed for a total of nine formulations (F1–F9). Every formulation showed adequate buoyancy behavior and acceptable physicochemical properties. All formulations displayed sustained release characteristics in in vitro drug release experiments, with formulation F8 exhibiting optimal drug release with a floating lag time of 28 ± 2 seconds and a cumulative drug release of 98.95 ± 1.40% at 12 hours. The optimized formulation followed Higuchi diffusion kinetics with a non-Fickian diffusion mechanism, according to drug release kinetic experiments. The optimized formulation's good stability was confirmed by stability testing conducted under accelerated settings, which showed no appreciable changes in physical appearance, drug content, hardness, and drug release profile.

According to the study's findings, Eudragit S-100 coated matrix tablets of tofacitinib citrate may be a viable method for efficient colon-targeted medication delivery with extended drug release and enhanced therapeutic efficacy.

Keywords: Tofacitinib citrate, Colon targeted drug delivery, Eudragit S-100, Matrix tablets, Chitosan, Carbopol 940 P, Floating tablets, Sustained release, pH-dependent coating, Drug release kinetics.