Litcius/Paper detail

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

Xinyuan Wang, Lei Wang, Changlin Yao, Guanying Xie, Shuhong Song, Huimin Li, Yaqian Qu, Xutang Tao

2021Crystal Growth & Design38 citationsDOI

Abstract

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.

Topics & Concepts

TheophyllineChemistryFavipiravirPharmacologyCoronavirus disease 2019 (COVID-19)Infectious disease (medical specialty)MedicineDiseasePathologyCrystallography and molecular interactionsCrystallization and Solubility StudiesEnzyme Structure and Function