中国临床药理学杂志2012，Vol.28Issue(6)：440-443,4.
Cocktail探针药物法评价灯盏花素对大鼠CYP450体内代谢活性的影响
Influence of breviscapinum on CYP450 isoforms by Cocktail probe drugs method
摘要
Abstract
Objective To study the influence of breviscapinum on the activities of CYP1A2, CYP2C9, CYP2E1 and CYP2D6 by cocktail probe drugs in rats. Methods The rats were randomly divided into three groups, control group, low dose group and high dose group. The rats in the low dose group and high dose group were treated with intravenous breviscapinum through caudal veins at the dose of 1. 8 , 5.4 mg · kg-1 once a day for 14 days respectively. The rats in the control group were injected with normal saline. On the 15th day, all rats in each group were injected with cocktail probes. The plasma concentrations of the different probe drugs were determined by HPLC and the main pharmacokinetic parameters were calculated. Results Compared with the control group, the AUC and t1/2 of metoprolol were significantly increased and the CL of metoprolol was significantly decreased in high dose group (P <0. 05). In low dose group, the pharmacokinetic parameters of metoprolol had the similar trend with high dose group, but it was not significantly different with those of the control group. There were no significant differences for the pharmacokinetic parameters of caffeine, chlorzoxazone and tolbuta-mide among these three groups. Conclusion High dose intravenous breviscapinum powder can inhibit the activity of CYP2D6, but has no influence on the activities of CYP1A2, CYP2C9 and CYP2E1.关键词
Cocktail探针药物法/CYPlA2/CYP2C9/CYP2E1/CYP2D6/灯盏花素Key words
Cocktail probe drugs/ CYP1A2/ CYP2C9/ CYP2E1/CYP2D6/ breviscapinum分类
医药卫生引用本文复制引用
龚文奇,梁晓光,李芹,刘洁,汪云..Cocktail探针药物法评价灯盏花素对大鼠CYP450体内代谢活性的影响[J].中国临床药理学杂志,2012,28(6):440-443,4.基金项目
天津市自然科学基金重点基金资助项目(09JCZDJC21500) （09JCZDJC21500）
高等学校博士学科点专项科研基金资助项目(新教师基金)资助课题(20091202120012) （新教师基金）
