Wednesday , 2 December 2020

Novel Approaches in Co-Crystal Formation of Asunaprevir for Improved Physicochemical Properties

Pratyusha Tatipamula1*, Dr. M. Sunitha2
1Department of Pharmaceutics, MNR College of Pharmacy, Sangareddy, Telangana, India.
2Principal, Shadan Women’s College of Pharmacy, Khairatabad, Hyderabad, Telangana, India.

In the current study, we attempted to improve the physicochemical properties of antiviral drug asunaprevir through the cocrystal synthesis. The neat cooling crystallization method to study the effect of coformer-hydroxybenzoic acid (FA) on solubility and dissolution of asunaprevir, 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 asunaprevir and 2,5-dihydroxybenzoic acid was confirmed by the characterization techniques which suggests the interactions between drug and coformer acid leads to cocrystal formation. The powder flow properties, solubility, and dissolution profile of drug are significantly improved by its cocrystallization.

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