RESUMEN
OBJECTIVE: To study the effect of Danshen injection and Xinkeshu tablets on the metabolism of CYP1A2, CYP2C9, CYP2C19, CYP2D6 and CYP3A4 in rabbits by cocktail probe substrates method. METHODS: Sixteen healthy fasted male rabbits were simultaneously given cocktail probe substrates including caffeine, tolbutamide, omeprazole, dextromethorphan and midazolam. The metabolic rates of cocktail probe substrates were determined by LC MS/MS methods at some specific time following the administration. Then the rabbits were randomly assigned to receive either Danshen injection or Xinkeshu tablets. The whole self-control trial was consisted of 3 cycles. The low, middle and high dosage (0.5, 1 and 2 mL · kg-1) of Danshen injection group would be administrated in 3 cycles in sequence. The low, middle and high dosage (90, 180 and 360 mg · kg-1) of Xinkeshu tablets group would be administrated in 3 cycles in sequence. Each cycle includes wall-out period of 7 d followed by administration of the 2 herbal medicines for consecutive 7 d. On the 15th day the cocktail probe substrates were administrated and the metabolic rates were determined. The differences of the metabolic rates between after and before admininstration of the 2 herbal medicines were assessed by one-way analysis of variance (ANOVA). RESULTS: After taking the agents of Danshen injection and Xinkeshu tablets, the metabolic rates of the five cocktail probe substrates had a tendency to decline compared with the before-administration. CONCLUSION: The outcome in vivo is in accordance with that in vitro. Danshen injection and Xinkeshu tablets can inhibit the metabolism of five CYPs (1A2, 2C9, 2C19, 2D6 and 3A4) activities in rabbits. At sometimes precautions are needed to co-administrate either Danshen injection or Xinkeshu tablets for-possible herb-drug interactions.
RESUMEN
Objective To establish a RP-HPLC method for determining the content of puerarin in Xinkeshu Tablets. Method The analysis was carried on a column of Zorbax Eclipse XDB-C_(18)(4.6 mm?150mm,5?m)at 25℃,with methanol-water-phosphoric acid(23:77:0.5)as mobile phase.The flow rate was 1.0 mL?min~(-1),and the detection wavelength was 250 nm.Result A good linearity was found in the range of 27.1～271.0 ng.The average recovery rate was 100.5 %,and RSD was 1.8%(n=5).Conclusion The method is simple,rapid,accurate,reproducible,and can be used to control the quality of Xinkeshu Tablets.