FORMULATION, DEVELOPMENT AND IN-VITRO EVALUATION OF TELMISARTAN USINGPOLYMERS IN FLOATING DRUG DELIVERY SYSTEM

Abstract

The therapeutic effectiveness of Telmisartan an (ARB) angiotensin II receptor blocker that is often used to treatment of hypertension is limited by its low bioavailability (42–58%) and water solubility is poor. Patient compliance is decreased by the frequent dosage required by conventional formulations. To overcome these obstacles a floating drug delivery system (FDDS) that used natural polymers was created to improve telmisartan's solubility, prolonged release and stomach retention. Natural polymers with gel-forming, biodegradable and biocompatible qualities such as xanthan gum, HPMC and PEO were used. Direct compression was used to create the formulations (F1–F9) which were then assessed for buoyancy, in vitro drug release and physicochemical characteristics. The compatibility of telmisartan with excipients were evaluated by FTIR and DSC analyses. The tablets' hardness, friability and flow characteristics were all satisfactory. According to buoyancy studies total floating periods ranged from 9.5 to 11.5 hrs with floating lag times ranging from 38 to 55 seconds. Studies on drug release in vitro showed sustained release for 12 hrs with the best release patterns being shown by F3 and F9. The study comes to the conclusion that Floating Drug Delivery System (FDDS) of telmisartan utilizing polymers can increase patient compliance, decrease the frequency of dose and improve bioavailability providing a viable strategy for managing hypertension.