Solubility Enhancement of Efavirenz Hydrochloride by Hot Melt Technique

Abstract

The present investigation is aimed to formulate & characterize the immediate release tablet of Efavirenz by using Soluplus as a polymer. The proposed formulation of the immediate release tablet of Efavirenz are prepared by using solid dispersion by hot melt technique to improve solubility and dissolution rate of poorly water soluble Efavirenz . The drug to polymer ratio in optimized batch (TABSD13) was 1:3. The obtained batch was characterized for its percent drug contenet, thermal analysis (DSC), crystallinity (PXRD), FTIR and in vitro drug release. There were no compatibility issues and the crystallinity of drug was found to be reduced in prepared tablet which were confirmed by DSC and PXRD studies. The average dissolution rate of six Efavirenz tablet & marketed formulation in 0.5 % SLS in distilled water in 45 min were 72.77 % & 69.37 % respectively while in 120 min they were about 90.08 % & 88.24 % respectively & the standard deviations were also within the limits. It shows that the dissolution profiles of hot melt Efavirenz tablet & Marketed formulation were comparable in 0.5 % SLS in distilled water. This may be because of the SLS which act as good surfactant. Further investigations are required to reduce the amount of polymer in tablet that can provide maximum drug loading and acceptable dosage form