Abstract

This work aims at investigating the use of hydroxy propyl methyl cellulose (HPMC) polymer to formulate sustained release matrix tablets containing diacerein. The sustained release tablets of diacerein were prepared by wet granulation method using HPMC as a release retarding polymer. Various kinetic models were applied to interpret the release of drug from the matrix system. A complete cross over bioavailability study of the developed sustained and immediate release tablets was carried out in rabbits to prove the safety and efficacy of the formulation. The release of the drug from tablets showed non-fickian diffusion obeying first order kinetics. The pharmacokinetic parameters such as AUC_o-∞ value were 20.449±8.83 and 13.479 6.31 µg/h/ml, C_max values were 2.22±1.15 and 3.30±0.02 µg/ml, t_max values were 4±0.69 and 2±0.24 h and mean plasma elimination half life (t_½) were 0.145±0.03 and 0.294±0.07 h, respectively, for the developed sustained and immediate release tablets of diacerein. The extent of absorption of drug from the developed diacerein sustained release tablets was significantly higher than that for developed diacerein tablets due to lower elimination rate and longer half-life.

Key words: Diacerein, hydroxy propyl methyl cellulose (HPMC), hydrophilic matrix, bioavailability.