Preparation and Evaluation of Gastroretentive Systems of Telmisartan

Abstract

Telmisartan (TEL) is a selective angiotensin II receptor blocker used in the management of cardiovascular disorders. It is a class II drug according to biopharmaceutics classification system; with poor solubility and high permeability. Owing to its hydrophobicity, TEL demonstrates low dissolution behavior in gastro-intestinal (GIT) media ensuing deprived absorption, and later poor bioavailability. The subject of the research is to prepare a floating tablet of TEL for oral use, which related to various benefits which can be summarized by improvement in the solubility and increment in the absorption and hence better bioavailability will be obtained in addition to reduction in its side effects. The Gastroretentive Floating Tablets (GFT) were formulated by means of hydroxy propyl methyl cellulose (HPMC). Six batches were formulated by Direct Compression (DC) and Wet Granulation (WG) method by using different HPMC concentrations. In addition to that, changing the diluent type (avecil 101 and 102) to reach optimal floating and dissolution performance.These prepared formulas were examined for angle of repose, Carr's Index (CI), hardness, Floating Lag Time (FLT), Floating Duration (FD) and dissolution profile. F5 (the favored formula) comprised 120mg HPMC plus 20mg sodium bi carbonate (NaHCO 3 ) which formulated by DC displays a reasonable characteristics in release profile with FLT of 8±2 second and buoyancy of 6.5±0.5 hours. It was concluded that F5 (the favored formula) represent a hopeful one as a floating of gastroretentive drug delivery systems of Telmisartan. KEYWORDS:In addition to that, changing the diluent type (avecil 101 and 102) to reach optimal floating and dissolution performance.