Novel Formulations of the Antiviral Drug Favipiravir: Improving Permeability and Tabletability

作者：Xinyuan Wang, Lei Wang, Changlin Yao, Guanying Xie, Shuhong Song, Huimin Li, Yaqian Qu, Xutang Tao · 发表于：Crystal Growth & Design · 年份：2021 · DOI：10.1021/acs.cgd.1c00150 · 被引用次数：38 · 研究领域：Crystallography and molecular interactions、Crystallization and Solubility Studies、Enzyme Structure and Function

Recently, favipiravir, as a broad-spectrum antiviral drug, has gain more attention because it might be a candidate to remedy the coronavirus disease 2019 (COVID-19). To improve its poor permeability and tabletability, four multicomponent crystals of favipiravir (FPV) were prepared by a slow evaporation or liquid-assisted grinding method, including three cocrystals (FPV-theophylline, 1:1; FPV-saccharin, 1:1; FPV-5-fluorouracil, 1:1) and one salt (FPV-piperazine, 2:1). All of the crystal structures were solved by single-crystal X-ray diffraction. Interestingly, FPV-theophylline has a crystal structure similar to that of FPV, leading to similar properties, such as solubility, permeability, and tabletability. Except for FPV-theophylline, all of the other multicomponent crystals exhibit an enhanced permeability and tabletability. Our studies provide a new insight in overcoming the shortcomings of the important antiviral drug FPV.