Editor-in-Chief Hatice Kübra Elçioğlu Vice Editors Levent Kabasakal Esra Tatar Online ISSN 2630-6344 Publisher Marmara University Frequency Bimonthly (Six issues / year) Abbreviation J.Res.Pharm. Former Name Marmara Pharmaceutical Journal
Journal of Research in Pharmacy 2021 , Vol 25 , Issue 6
In vitro studies for BCS classification of an antiviral agent, favipiravir
Selin Seda TİMUR1,Meltem ATAŞOĞLU2,Yalçın ÖNER2,Tutku Ceren KARABULUT2,Hakan EROĞLU1
1Department of Pharmaceutical Technology, Faculty of Pharmacy, Hacettepe University, Sıhhiye 06100 Ankara, Turkey
2Tobio Novelfarma Drug Industry and Trade Limited Company, Ümraniye 34768 İstanbul, Turkey
DOI : 10.29228/jrp.91 Favipiravir (6-fluoro-3-hydroxy-2-pyrazinecarboxamide) is a purine nucleic acid analog, which is an antiviral agent used in the treatment of influenza. Since the recent outbreak caused by 2019-novel coronavirus (nCoV), there has been a seek for effective antiviral agents to be used in the treatment of coronavirus disease 2019 (COVID-19), and favipiravir has been one of the options which provides a broad-spectrum therapy. Herein, we studied the aqueous solubility and in vitro permeability characteristics of favipiravir in order to shed light on the BCS classification of this antiviral agent used in COVID-19 therapy. The in vitro solubility was assessed using saturated solution of favipiravir in four different aqueous media and the solubility values were evaluated during 72 h at 37 oC. The solubility of favipiravir was between 4.48 to 8.5 mg/ml, which is 5.85 to 10.63 times of calculated solubility limit. Caco-2 cell monolayers were utilized for the permeability assessment, and the drug solutions in three different concentrations including the highest dose required for bioequivalence exemption of the immediate release dosage form were applied. The effect of efflux transporters on the permeability of favipiravir was also determined using a P-gp inhibitor, Verapamil HCl. According to the data obtained from the in vitro studies, favipiravir can be considered as a representative of class I compound. Keywords : Favipiravir; antiviral therapy; BCS classification; solubility; permeability; Caco-2 cell monolayer
Marmara University