Abstract

FORMULATION DEVELOPMENT AND OPTIMIZATION OF RITONAVIR TABLETS EMPLOYING STARCH 1500 AND SOLUPLUS

M. Priyadarsini, K. P. R. Chowdary* and S. V. U. M. Prasad

Abstract

The objective of the present study is to enhance the dissolution rate of Ritonavir by solid dispersion in Starch 1500 and Soluplus in its tablet formulation development and to optimse the Ritonavir tablet formulation employing Starch 1500(factor A) and Soluplus(factor B) by 22 factorial design to achieve NLT 85% dissolution in 10 min. Four Ritonavir tablet formulations were prepared using selected combinations of the two factors as per 22 factorial design. Ritonavir tablets were prepared by direct compression method and were evaluated. The individual and combined effects of the two factors, Starch 1500 and Soluplus are highly significant (P < 0.01) in influencing the dissolution rate of RITONAVIR tablets. Ritonavir tablet formulations Fab and Fa disintegrated rapidly within one min and gave very rapid dissolution of Ritonavir, 99.4% and 89.9% in 10 min respectively. The increasing order of dissolution rate (K1) observed with various formulations was F1< Fb< Fa< Fab. The polynomial equation describing the relationship between the response, percent drug dissolved in 10min (Y) and the levels of starch1500(X1) , soluplus (X2) based on the observed results was found to be Y = 77.74 + 16.92 (X1) + 9.42(X2) – 4.67(X1 X2). Based on the above equation, the formulation of optimized Ritonavir tablets with NLT 85% dissolution in 10 min require starch1500 at 1:3.84 ratio of drug: starch1500, and Soluplus at 1% of drug and starch1500 content. The optimized Ritonavir tablet formulation gave 85.5% dissolution in 10min fulfilling the target dissolution requirement. Formulation of Ritonavir tablets with NLT 85% dissolution in 10 min could be optimized by 22 factorial design.

Keywords: Formulation Development, Ritonavir tablets, Optimization, Factorial Design, Starch 1500, Soluplus.