Abstract

FORMULATION DEVELOPMENT OF EFAVIRENZ TABLETS EMPLOYING β--CYCLODEXTRIN, HYDROXY PROPYL β-CYCLODEXTRIN AND SOLUTOL HS15

*R.Yogananda¹, K. P. R. Chowdary²

¹Research Scholar, Dept. of Biotechnology, Acharya Nagarjuna University, Nagarjunanagar- 522510, Guntur, A.P., India.
²A.U. College of Pharmaceutical Sciences, Andhra University, Visakhapatnam – 530003.

ABSTRACT

Efavirenz, exhibits low and variable oral bioavailability due to its poor aqueous solubility. Its oral absorption is dissolution rate limited and it requires enhancement in the solubility and dissolution rate for increasing its oral bioavailability. The objective of the present investigation was to determine the individual main and combined (interaction) effects of CDs and Solutol HS15 on the dissolution rate of efavirenz from tablet formulations in a series of 22 – factorial experiments. Efavirenz (100mg) formulated in to compressed tablets by wet granulation method employing selected combinations of CDs ( βCD and HPβCD ) and Solutol HS15. All the tablets prepared were of good quality fulfilling the official (I.P) standards with regard to hardness, friability, disintegration time and drug content. Drug dissolution from the tablets formulated followed first order kinetics and gave relatively higher rates of dissolution (K1) and dissolution efficiency (DE30) values when compared to those of efavirenz plain tablets. Formulations E4 and E8, which are formulated employing βCD-Solutol HS15 and HPβCD-Solutol HS15 respectively, gave much higher dissolution rates when compared to plain tablets, E1. A 42.5 and 34.2 fold increase in K1 was observed respectively with formulations E4 and E8 when compared to formulation E1 ( plain tablets ). The dissolution efficiency ( DE30 ) was also increased from 4.56% for formulation E1 to 41.54 % and 36.59 % respectively for formulations E4 and E8.

Keywords: Efavirenz Tablets, β-Cyclodextrin, HPβ-Cyclodextrin Solutol HS15, Dissolution Rate, Factorial Study.