Improving the solubility and bioavailability of anti-hepatitis B drug PEC via PEC-fumaric acid cocrystal.

ABSTRACT: PEC is a new generation of phosphamide ester anti-hepatitis B virus drug. It is a prodrug of tenofovir and can be rapidly metabolized to tenofovir. However, its poor solubility in water (0.219 mg mL^-1 at 25 °C) has limited its oral bioavailability. In this study, we aimed to improve the solubility and consequently the oral bioavailability of PEC via a cocrystal. A cocrystal of PEC with fumaric acid (FUA) (PEC-FUA, 1 : 1) was successfully obtained and characterized. The crystal structure of this cocrystal was tested using a single crystal X-ray diffraction method. The intrinsic dissolution rate (IDR) characterization was performed in a pH 6.8 buffer. The solubility of this cocrystal in 0.1 M HCl (pH 1.0) and pH 6.8 phosphate buffers was investigated, and the results showed

SUBMITTER: Li L 

PROVIDER: S-EPMC9056957 | biostudies-literature | 2020 Sep

REPOSITORIES: biostudies-literature