中国药理学通报2011，Vol.27Issue(2)：276-280,5.
雷公藤活性成分对大鼠体内P450酶活性的影响
Active ingredients of tripterygium wilfordii impact on P450 activities using a cocktail method
摘要
Abstract
Aim To evaluate the effects of Tripterygium wilfordii tablet on P450 activities by cocktail probe drugs in rats.Methods Two probe drugs ( omeprazole, midazolam )were simultaneously given to rats after low and high dosing of Tripterygium wilfordii tablets.The plasma concentrations of the two probes were measured by LC-MS and their corresponding pharmacokinetic parameters were calculated.Results There were some differences between omeprazole and midazolam in plasma concentrations and the corresponding pharmacokinetic parameters in rats after two dosing of Tripterygium wilfordii tablets administration.The AUC and T1/2 of midazolam increased significantly( P ＜0.05 ) and the CL/F decreased in rats after two dosing of Tripterygium wilfordii tablets for 10 consecutive days.No influences were observed on Tmax and Vd/F,but the Cmax of midazolam increased after high dosing of Tripterygium wilfordii tablets ; The T1/2 and Vd/F of omeprazole increased after low dosing of Tripterygium wilfordii tablets, and the AUC increased after high dosing of Tripterygium wilfordii tablets.Conclusion Tripterygium wilfordii tablets twice daily for 10 days can inhibit CYP3A4 activity significantly, and it may also have effect on CYP2C19.关键词
Cocktail/探针药物/雷公藤片/药代动力学/CYP450/CYP3A4/CYP2C19分类
医药卫生引用本文复制引用
刘史佳,刘子修,周玲,居文政,张军,谈恒山..雷公藤活性成分对大鼠体内P450酶活性的影响[J].中国药理学通报,2011,27(2):276-280,5.基金项目
科技部重大新药创制科技重大专项--中药新药临床评价研究技术平台(南京)建设(No 2008ZX09312-004) （南京）
江苏省中医药领军人才(No LJ200906) （No LJ200906）
