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| 雷公藤活性成分对大鼠体内P450酶活性的影响 | |
| 引用本文： | 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 |
| 作者姓名： | 刘史佳 刘子修 周玲 居文政 张军 谈恒山 |
| 作者单位： | 1. 南京中医药大学附属医院临床药理科,江苏,南京,210002 2. 南京中医药大学药学院,江苏,南京,210002 3. 南京军区总医院,江苏,南京,210002 |
| 基金项目： | 科技部重大新药创制科技重大专项项目,江苏省中医药领军人才项目 |
| 摘 要： | 目的用Cocktail探针药物法,研究雷公藤片对大鼠肝CYP450的影响。方法分别以奥美拉唑和咪达唑仑作为CYP2C19和CYP3A4的探针药,将大鼠随机分为低剂量和高剂量两组,每日早晚灌胃雷公藤片,采用液质联用法测定连续使用雷公藤片前后大鼠血浆中相应的探针药物的浓度及其药代动力学参数。结果连续灌胃10 d后,与用药前比较,奥美拉唑、咪达唑仑的血药浓度及其药代动力学参数有明显改变;低剂量组和高剂量组中咪达唑仑的AUC明显增加,CL/F明显降低,T12增大,Vd/F和Tmax变化不明显,高剂量组中Cmax有所增大;低剂量组中奥美拉唑的T21和Vd/F有所增大,高剂量组中AUC增加(P<0.05)。结论连续灌胃雷公藤片10 d后,雷公藤片对大鼠体内CYP3A4酶具有抑制作用;对CYP2C19酶具有一定的抑制作用。 |
| 关 键 词： | Cocktail 探针药物 雷公藤片 药代动力学 CYP450 CYP3A4 CYP2C19 |
Active ingredients of tripterygium wilfordii impact on P450 activities using a cocktail method |
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| LIU Shi-jia,LIU Zi-xiu,ZHOU Ling,JU Wen-zheng,ZHANG Jun,TAN Heng-shan. Active ingredients of tripterygium wilfordii impact on P450 activities using a cocktail method[J]. Chinese Pharmacological Bulletin, 2011, 27(2): 276-280 | |
| Authors: | LIU Shi-jia LIU Zi-xiu ZHOU Ling JU Wen-zheng ZHANG Jun TAN Heng-shan |
| Affiliation: | LIU Shi-jia1,LIU Zi-xiu2,ZHOU Ling2,JU Wen-zheng1,ZHANG Jun1,TAN Heng-shan3(1.Dept of Clinical Pharmacology,the Affiliated Hospital of Nanjing University of Traditional Chinese Medicine,Nanjing 210029,China,2.Nanjing University of Traditional Chinese Medicine,3.Nanjing General Hospital of Nanjing Military Command,Nanjing 210002,China) |
| 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 pharmacokin... |
| Keywords: | Cocktail CYP450 CYP3A4 CYP2C19 |
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