Impact of multiple H/D replacements on the physicochemical properties of flurbiprofen.

ABSTRACT: Although deuterium incorporation into pharmaceutical drugs is an attractive way to expand drug modalities, their physicochemical properties have not been sufficiently examined. This study focuses on examining the changes in physicochemical properties between flurbiprofen (FP) and flurbiprofen-d₈ (FP-d₈), which was successfully prepared by direct and multiple H/D exchange reactions at the eight aromatic C-H bonds of FP. Although the effect of deuterium incorporation was not observed between the crystal structures of FP and FP-d₈, the melting point and heat of fusion of FP-d₈ were lower than those of FP. Additionally, the solubility of FP-d₈ increased by 2-fold compared to that of FP. Calculation of the

SUBMITTER: Uchiyama H 

PROVIDER: S-EPMC10718516 | biostudies-literature | 2023 Dec

REPOSITORIES: biostudies-literature