GASTRO RETENTIVE TABLET OF FEBUXOSTAT: FORMULATION, DRUG RELEASE DYNAMICS AND FACTORIAL DESIGN

Present work highlights a strategy to develop a hydrophilic matrix based sustained release formulation for gastro-retentive drug delivery system (GRDDS) of Febuxostat. GRDDS is realized as a promising option for gout treatment, as the delivery system can control and prolong gastric residence time and supply high drug concentration in gastric region for better action. Swellable and floatable gastroretentive tablets were prepared by direct compression technique and evaluated for their swelling characteristics (Swelling index, water uptake), floating capacity (floating lag time and duration), Invitro drug release and stability studies. Factorial design was employed to optimize formulation components. Nine formulations were prepared using two independent variables, amount of Hydroxy Propyl Methyl Cellulose (HPMC) K4M (60, 90, & 120 mg) and amount of Sodium bicarbonate (20, 30, & 40 mg). The floating lag time and time required for 90% (t90%) of drug release were selected as dependent variables. Optimized formulation showed zero order Invitro drug release for more than 10 hours with excellent buoyancy properties. The prepared tablets floated within 3 min and maintain for more than 18 h. The decrease in the release rate was observed with an increase in the viscosity of the polymeric system. Polymer with lower viscosity (HPMC K4M) was shown to be beneficial than higher viscosity polymer (K15M and K100M) in improving the floating properties of GRDDS. These results suggest that prepared GRDDS has the improved release and retentive properties which will be translated into better treatment for gout and other disease.