Formulation Optimization and In Vitro and In Vivo Preclinical Evaluation of Valsartan IR Tablets
| Main Authors: | N. Tirumalesh, K. P. R. Chowdary |
|---|---|
| Format: | Article |
| Terbitan: |
, 2019
|
| Online Access: |
https://zenodo.org/record/2597327 |
Daftar Isi:
- The objective of the present study is optimization of Valsartan tablet formulation employing βCD, Starch 1500, and Soluplus by 23 factorial design to achieve NLT 85% dissolution in 10 min and to evaluate the optimized formulations by In Vitro and In Vivo (Preclinical) methods. Eight Valsartan tablet formulations were prepared using selected combinations of the three factors as per 23 factorial design. Valsartan tablets were prepared by direct compression method and were evaluated. The individual and combined effects of the three factors βCD, Starch 1500 and Soluplus are highly significant (P < 0.01) in influencing the dissolution rate of Valsartan tablets.Valsartan tablet formulations Fb,Fab, Fbc and Fabc disintegrated rapidly and gave very rapid dissolution of Valsartan, 92.4%, 99.4% ,96.2% and 99.2% in 10 min respectively. The increasing order of dissolution rate (K1) observed with various formulations was F1< Fc< Fa< Fac< Fb< Fbc< Fab <Fabc. The polynomial equation describing the relationship between the response, percent drug dissolved in 10min (Y) and the levels of βCD (X1) , Starch 1500 (X2) and Soluplus (X3) based on the observed results was found to be Y = 68.625 + 4.375(X1) + 27.375(X2) - 2.375(X1 X2)+ 3.375(X3) + 0.125(X1 X3) - 1.875(X2 X3) - 0.625(X1 X2 X3) Based on the above equation, the formulation of optimized Valsartan tablets with NLT 85% dissolution in 10 min require βCD at 1:3.5 ratio of drug: βCD, Starch 1500 at 24.37% of drug and βCD content , and Soluplus at 1% of drug and βCD content. The optimized Valsartan tablet formulation gave 85.75% dissolution in 10min fulfilling the target dissolution requirement. The optimized Valsartan IR tablet formulation developed exhibited rapid absorption, higher plasma concentrations and higher bioavailability (123.5%) when compared to Valsartan market product. Hence formulation of Valsartan IR tablets with NLT 85% dissolution in 10 min could be optimized by 23 factorial design.