Abstract:

Osthol is a natural drug component of coumarins. It is insoluble in water and has a short half-life，resulting in poor bioavailability. It is absorbed through the intestine and distributed rapidly in other tissues. This paper reviews the in vivo process，pharmacokinetics，targeting and metabolites of Osthol. The substances metabolized by Osthol in vivo are not the same as those simulating liver metabolism in vitro. After phase Ⅰ metabolism，Osthol produces demethylated osthol，dehydrogenated Osthol and hydroxylated Osthol. Some studies have proved that there are no dehydrogenated products in urine and feces through in vivo metabolism detection. However other studies have shown that they can be detected in blood and urine，with lower the content of dehydrogenated products in urine，and there are dehydrogenated products in liver metabolism after incubation in vitro. It is possible that dehydrogenated Osthol is an active metabolite in vivo. Clarifying the metabolic characteristics and products of Osthol in vivo and in vitro is helpful to find active metabolites.

Key words: osthol, pharmacokinetics, metabolites