Formulation design and optimization of sustained release tablet dosage form of Diacerein

Abstract

Diacerein is both an anti-inflammatory drug and an anti-arthritic agent. At present, no sustained release dosage form of Diacerein is commercially available. The aim of the study was to develop an optimized formulation of sustained release tablet dosage form of Diacerein that will be highly patient compliant. A three-level full factorial design was employed to develop nine different formulations of matrix tablets using a combination of Methocel K100M CR and Methocel K4M CR polymer at different ratios. The physical evaluation of both the drug-excipient powder mixtures and tablets of the nine formulations were performed and results were found to be within acceptable ranges for all tests. Dissolution profiles of tablets were obtained and the kinetics of drug release from the matrix tablets were determined by employing various mathematical models. The release data were simulated in Design Expert Software to carry out statistical analysis and the effect of both polymers on release patterns were observed after 1, 4 and 8 h in terms of contour plots and 3D surface plots, which were found to be statistically significant (p < 0.05). Finally, the overlay plot was obtained from which the optimized formulation of Diacerein was determined.