Objective: To evaluate effect of different doses of compound Danshen injection on rat liver microsomal cytochrome P450 metabolic activity by Cocktail probe drugs. Method: Male rats were randomly divided into four groups

including Danshen injection high

middle

low dosage groups and the control group.Reversed phase high performance liquid chromatography (RT-HPLC) is adopted to determine plasma concentration and 3P97 Pharmacokinetic software was employed to compare pharmacokinetic parameters of four specific probe drugs. Result: Compared with the control group

elimination half-time (t1/2β)of caffeine increased from 50.492 min to 54.456 min and the area under concentration-time curve (AUC) was significantly increased

clearance rate (CL) was significantly reduced in compound Danshen injection high-dose group;t1/2β of chlorzoxazone can be shortened

AUC was reduced and CL was significantly increased in high-dose group;t1/2β and AUC of tolbutamide were gradually increased and CL was gradually decreased as the dose.Pharmacokinetic parameters of midazolam were no significant differences of compound Danshen injection of three dose group. Conclusion: Compound Danshen injection on the overall level of rat liver micro-body CYP2C9 has a certain extent inhibition

and there is a dose-dependent.There are weak inhibitory effect on CYP1A2 and weak induction on CYP2E1 of high doses of compound Danshen injection

there is not effect on CYP1A2 and CYP2E1 of low and middle dosage of compound Danshen injection.There is not any effect on activity of CYP3A4.