CRYSTAL ENGINEERING OF ANTIVIRAL AGENT EFAVIRENZ FOR SOLUBILITY ENHANCEMENT

摘要

In the current study, we attempted to improve the physicochemical properties of antiviral drug efavirenz through the cocrystal synthesis. The neat grinding performed to study the effect of coformer-fumaric acid (FA) on solubility and dissolution of efavirenz, which can serve as the green cocrystal synthesis approach. The prepared cocrystals were characterized for characteristics like powder flow properties, aqueous saturation solubility, in vitro powder dissolution study. The synthesized cocrystals were characterized by Fourier transform infrared spectroscopy, differential scanning calorimetry, powder X-ray diffraction. The formation of a cocrystal of efavirenz and caffeine was confirmed by the characterization techniques which suggests the interactions between efavirenz and coformer-fumaric acid leads to cocrystal formation. The powder flow properties, solubility, and dissolution profile of efavirenz are significantly improved by its cocrystallization.