Abstract

FORMULATION AND EVALUATION OF SELF MICROEMULSIFYING DRUG DELIVERY SYSTEM OF TELMISARTAN

Dr. Yogesh Thorat*, Dr. Avinash H. Hosmani, Pallavi Gulave, Onkar Wale, Nitin Mane, Prachet Bagewadikar

ABSTRACT

Telmisartan is Angiotensin II Receptor Antagonist, which is used in the prevention and treatment of hypertension. Major drawback of Telmisartan is its low water solubility and high permeability. Nearly 40% of new drug candidates exhibit low solubility in water, which leads to poor oral bioavailability, high intra- and inter subject variability and lack of dose proportionality. Hence, various approaches are used to improve the dissolution rate of drugs for bioavailability enhancement. Amongst them, Self micro emulsifying drug delivery systems (SMEDDS) have shown great promise for enhancing bioavailability of low solubility compounds. Therefore, through this work, an attempt was made to improve the dissolution rate and thus oral bioavailabillity of Telmisartan by formulating SMEDDS. The system consisting of Labrafac PG, Tween 80 and PEG 400 with a drug load 20 mg/ml was formulated and evaluated for various parameters like stability, in vitro drug release, drug content. Stability studies reveal that F1, F2, F3, F4, F5 and F7 were stable at 4°c and 45°c temperatures which indicate its thermodynamic stability. The drug content was varied from 97.89% to 99.16%. The optimized SMEDDS formulation F4 showed a significant increase in the dissolution rate and oral absorption compared to the plain drug. Therefore we may conclude that the SMEDDS can become a reliable technique for the solubilization of poorly water soluble drug, specially to overcome the problem associated with solubility.

Keywords: Telmisartan, solubility enhancement, self microemulsifying drug delivery system.