Formulation Development of Extended Release Tablet Containing Anti-Muscaranic Agent

Abstract

ASFTFT2016 is muscarinic receptor antagonist used for the treatment of urinary incontinence which leads to increase into urination frequency. ASFTFT2016 is widely used as a muscarinic receptor antagonist. The aim of the present work was to develop extended release tablets of ASFTFT2016 using different grades of hydrophilic polymers such as hypromellose (HPMC). The purpose of developing extended release dosage form was to reduce dosing frequency and eliminate the side effects such as dry mouth, constipation, dizziness, blurred vision which are observed with immediate release tablets. The tablets were prepared by direct compression using different grades of HPMC and other moisture protective excipients such as microcrystalline cellulose (MCC) PH 112, lactose anhydrous DCL 21, syloid 63 FP, syloid 244 FP in different ratio. Effect of hardness, diluent ratio, blending time on the drug release were studied. Drug release at different pH and in presence of alcohol were checked for optimized batch containing alone Anycoat CN10T 10000. As a back-up, formulation with 7:3 ratio of Anycoat CN10T 10000 and Anycoat CN10T 4000 grades of HPMC was also prepared which can be selected if bioequivalence test fails. The optimized batch showed similar drug release to innovator in different dissolution media. Alcohol didn’t increase drug release significantly due to insolubility of polymer in it. The developed formulation was robust and will be studied for bio equivalence with innovator.