Formulation and Evaluation of Darifenacin Hydrobromide Extended Release Matrix Tablets

Author(s)

Sultana, S.M., Devi, S.A.

Author's Affiliation

Abstract

Darifenacin hydrobromide is a highly selective muscarinic (M3) receptor blocker that has been widely used for the treatment of overactive bladder syndrome. The bioavailability of darifenacin hydrobromide is 15–19% due to extensive first pass metabolism. Hence oral administration of darifenacin hydrobromide as extended tablets is a possible solution to overcome this problem. So the aim of the study was to formulate and evaluate Darifenacin hydrobromide extended release matrix tablets using extended release polymers like HPMC K4M, HPMC K15M and HPMC K100M, Metalose 60 SH-50 and Xanthum gum in different concentrations. Formulated tablets were characterized for different parameters like hardness, thickness, weight variation, friability, % Cumulative drug release etc. Nine formulations (F1 – F9) were formulated using direct compression technique. From the results obtained, it was concluded that the optimized formulation containing HPMC K15 M and K100M (1:2) showed better release up to 24hrs.The dissolution profiles and kinetic studies indicate that the release of Darifenacin Hydrobromide can be effectively controlled by the use of hydrophilic matrix systems. Different kinetic models were applied to the optimized formulation and observed that formulation (F9) followed first order kinetic model and Non-Fickian diffusion (or) Anomalous transport as mechanism of drug release.

Keywords

Darifenacin Hydrobromide, Extended Release Matrix Tablets, Bioavailability, HPMC K15M and HPMC K100M

Cite This Article

Sultana, S.M., Devi, S.A. (2016). Formulation and Evaluation of Darifenacin Hydrobromide Extended Release Matrix Tablets, International Journal for Pharmaceutical Research Scholars (IJPRS), 5(3), 82-90.