Design, Development and Evaluation of Solubility Enhancement of Efavirenz by Solid Dispersion Technique

The new active ingredients are mostly poorly soluble in water; their oral bioavailability and solubility remain the most important criteria for pharmaceutical formulations. Solid dispersion techniques have attracted great interest to improve the dissolution rate of highly lipophilic drugs. They improve their bioavailability by reducing particle size, improving wettability, and forming amorphous particles. Use of one or more carriers for solid dispersion. Hydrophilic carriers are used in the formulation of a solid dispersion. The poorly water-soluble drug comes into contact with a solid carrier or its solution. In the formulation of tablets and capsules, these types of drugs are challenging. Various techniques are used for solid dispersion. Efavirenz is a (NNRTI) non-nucleoside reverse transcriptase inhibitor used for the treatment of HIV (human immunodeficiency virus) type I. Soluble in methanol, ethanol, and dichloromethane, practically insoluble in water. Efavirenz is classified as a BCS class II medication. The aim of the present work is to improve the solubility of Efavirenz by preparing its solid dispersion with polymers PVP and HPMC using solvent evaporation technique. The results show that the drug with PVP as polymer increases the dissolution rate compared to the drug with HPMC.