Effect of Breviscapinun Powder for Injection on the Activity of CYP2D6 in Rats

OBJECTIVE: To study the effect of breviscapinun powder for injection on the activity of cytochrome P4502D6 (CYP2D6) in rats. METHODS: The rats were randomly divided into three groups, i.e. control group (normal saline), breviscapinun low-dose and high-dose groups (0.54,0.18 mg·100 g-1). Each group was given medicine once a day via intravenous injection for 14 days. On the 15th day, all rats were injected with metoprolol solution, then blood samples of inner canthus 0.8 mL were collected at a set of time-points. The plasma concentration of metoprolol was determined by HPLC. RESULTS: In high-dose group, AUC and t1/2 of metoprolol were significantly higher than those in control group (P0.05), and CL were significantly lower than that of control group (P0.05) 14 days after administration of breviscapinun powder for injection. Compared with control group, AUC and t1/2 of metoprolol were higher and CL was lower in low-dose group, but there were no significant differences between low-dose group and control group. CONCLUSION: High-dose of breviscapinun powder for injection can significantly inhibit the activity of CYP2D6 in rats.