Design, synthesis, and bioavailability evaluation of coumarin-based prodrug of meptazinol.


Based on the known coumarin-based prodrug system, a new meptazinol (Z)-3-[2-(propionyloxy) phenyl]-2-propenoic ester (3) was designed and synthesized as prodrug to minimize the first-pass effect of meptazinol (1) and improve the oral bioavailability. The prodrug (3) showed a 4-fold increase in oral bioavailability over the parent drug meptazinol in rats. 


Figures and Tables

Sorry, we couldn't extract any figures or tables for this paper.