Abstract

PHARMACOKINETIC EVALUATION OF OPTIMIZED VALSARTAN TABLETS FORMULATED EMPLOYING ? CD, CROSPOVIDONE AND SLS IN COMPARISON TO A MARKET PRODUCT

Ch . Tarakaramarao and K. P. R. Chowdary*

ABSTRACT

Valsartan, a widely prescribed anti hypertensive drug belongs to class II under BCS classification and exhibit low and variable oral bioavailability due to its poor aqueous solubility. It needs enhancement in the dissolution rate in its formulation development. Optimized valsartan tablet formulation with NLT 85% dissolution in 10 min could be developed employing βCD , Crospovidone and SLS by 23 factorial design. In the present study pharmacokinetic evaluation was done on optimized valsartan tablet formulation developed in comparison to a market product of valsartan tablets with an objective to evaluate their in vivo performance. Pharmacokinetic evaluation of the Optimized valsartan (40 mg) tablets in comparison to commercial valsartan (40 mg ) tablets (Valent-40) was done in healthy rabbits weighing 1.5 – 2.5 kg (n=6) of either sex in a cross over study at a dose of 40 mg of valsartan per tablet. The biological half – life (t ½) was found to be 5.06 h and 4.66 h respectively following the administration of optimized valsartan tablets formulated (Vopt) and Market product. With both the two products tested valsartan was found to be absorbed rapidly and peak concentration is achieved in 1 h. The absorption rate constant (Ka) was found to be 2.275 h-1 and 1.409 h-1 respectively with Vopt and Market product. The relative bioavailability (BA) of valsartan from the Vopt formulation was found to be 105.7 % when compared to Market product (100%). The optimized valsartan tablets formulated employing βCD, Crosspovidone and SLS are comparable to the market product with regard to in vivo performance.

Keywords: .