FORMULATION DEVELOPMENT OF EFAVIRENZ TABLETS EMPLOYING Β CYCLODEXTRIN, SOLUPLUS AND PVP K30: FACTORIAL STUDY

Abstract

Efavirenz, a widely prescribed HIV- 1 specific non – nucleoside reverse transcriptase inhibitor drug belongs to class IΙ
under BCS and exhibit low and variable oral bioavailability due to its poor aqueous solubility. It is practically insoluble in water
and aqueous fluids and as such it posses challenging problems in its formulation development. The objective of the present study
is to formulate efavirenz tablets employing β cyclodextrin (β CD), Soluplus and PVP K30 alone and in combinations and to
evaluate their effects on the dissolution rate of efavirenz tablets in a 23 factorial study. Efavirenz tablets were formulated
employing β CD, Soluplus and PVP K 30 as per 23 factorial design and the tablets were prepared by direct compression method.
The tablets prepared were evaluated for various physical properties, dissolution rate and dissolution efficiency. Dissolution data
were analyzed by Analysis of Variance (ANOVA) of 23 factorial studies. Efavirenz – βCD – Soluplus- PVP K 30 solid inclusion
complexes could be formulated into compressed tablets by direct compression method and the resulting tablets fulfilled the
official (IP 2010) specifications with regard to hardness, friability, drug content, disintegration time and dissolution rate .Efavirenz
dissolution was rapid and higher from the tablets formulated employing drug- βCD- Soluplus- PVP K 30 inclusion complexes
when compared to the tablets containing efavirenz alone and market product tested. The individual as well as combined effects of
the three factors involved i.e., βCD (factor A) ,Soluplus (factor B) and PVP K 30 ( factor C) except abc combination were highly
significant (P< 0.01) in enhancing the dissolution rate (K1) and dissolution efficiency (DE 30) of efavirenz. Combinations of β CD
– Soluplus, β CD – PVP K 30 and Soluplus – PVP K 30 gave higher enhancement in the dissolution rate of efavirenz tablets than
is possible with them alone. The tablets formulated employing drug- βCD- Soluplus- PVP K 30 inclusion complexes and market
product tested fulfilled the official (I.P 2010) dissolution rate test specification of NLT 70 % in 30 min prescribed for efavirenz
tablets. Hence combination of βCD with either Soluplus or PVP K 30 and combination of Soluplus with PVP K 30 is
recommended to enhance the dissolution rate and dissolution efficiency of efavirenz in its formulation development.