Abstract

“FORMULATION AND EVALUTION OF EXTENDED- RELEASE MINI TABLET OF DARIFENACIN BY USING NATURAL POLYMER”

Sohrab A.* and Shakeel M.

ABSTRACT

Darifenacin is a muscarinic M3 selective receptor antagonist, which by relaxing the detrusor muscles intended for symptomatic treatment of urge incontinence and increased urinary frequency and urgency as may occur in patients with overactive bladder syndrome. Darifenacin protein binding is 98%. The bioavailability of darifenacin is 15–19% due to extensive first pass metabolism (varying with type of metabolisers i.e. poor and extensive) with elimination t1/2 of 13-19 hours. Hence oral administration of darifenacin as extended release tablets is a possible solution to overcome this problem. So the aim of the study was to formulate and evaluate Darifenacin extended release mini tablets with less risk of dose dumping as well as inter and intra subject variability using extended release polymers like guar gum in different concentrations with increased ease of administration. The compatibility between drug and excipients were determined by using FTIR and DSC. Formulated tablets were characterized for different parameters like hardness, thickness, weight variation, friability, % drug release etc. Nine formulations (D1 – D9) were formulated using wet granulation technique. From the results obtained, it was concluded that the optimized formulation D5 showed better release up to 24hrs.

Keywords: Darifenacin, wet granulation, guar gum, mini tablet, extended release.