DEVELOPMENT AND EVALUATION OF FAST DISSOLVING TABLETS OF EFAVIRENZ BY SOLUBILITY ENHANCEMENT TECHNIQUE

Efavirenz (EFV) is an anti-retroviral agent with low aqueous solubility. To enhance the solubility of EFV by using the concept of mixed hydrotropy. Initially, solubility of EFV was determined individually in sodium acetate, sodium citrate, urea and sodium benzoate at concentration of 10% w/v solutions. Highest solubility was obtained in 10% sodium benzoate solution. Highest solubility was obtained in 1:6:1 ratio of Urea + Sodium benzoate + Sodium acetate. This optimized combination was utilized in the preparation of solid dispersions by using distilled water as a solvent. Fourier-transform infrared to show no drug-hydrotropes interaction has occurred. Formulation of FAST dissolving tablets of Efavirenz using mixed hydrotrophy technique with different concentrations of super disintegrants such as Crosspovidone and Sodium Starch Glycolate were prepared by using direct compression method. Dissolution studies of prepared tablets were done using USP Type II apparatus. The batch CF3 tablets show 98.3% cumulative drug release within 40 min. The miraculous enhancement in solubility and bioavailability of Efavirenz was clear indication of the potent mixed hydrotropy to be used in future for other poorly water-soluble drugs in which low bioavailability is a major concern.

KEYWORDS: Efavirenz, Mixed hydrotropy, Solid dispersions, fast dissolving tablets.