Investigation of Picroside II's Impacts on the P450 Activities Using a Cocktail Method

ABSTRACTAIMTo evaluate the effects of picroside II on P450 activities in rats.METHODSFive probe drugs (diclofenac, midazolam, dextromethorphan, chlorzoxazone and omeprazole) were simultaneously given to rats after single and multiple dosing of picroside II. The plasma concentrations of the five probes were measured by LC-MS and their corresponding pharmacokinetic parameters were calculated.RESULTSThere were no differences among the five probes in their plasma concentrations and the corresponding pharmacokinetic parameters in rats after single dosing of picroside II (10 mg·kg−1). The AUC0-t and the drug concentration of omeprazole increased significantly (P< 0.05) in rats after multiple dosing of picroside II (10 mg·kg−1, orally, twice daily for 12 consecutive days).CONCLUSIONSingle administration of picroside II had very little impact on the activities of P450 while multiple administration of picroside II tended to inhibit CYP2C19 activity.