探针药物法测定大黄对大鼠肝细胞色素CYP2E1酶的影响  

Evaluation of activity of hepatic CYP2E1 following administration of Radix et Rhizoma Rhei by probe drug in rats

作　　者：陈荣[1] 谢陶吟[1] 邹素兰[1] 徐星凯[1] 

机构地区：[1]常州市第一人民医院药剂科,常州213003

出　　处：《中国临床药学杂志》2009年第2期109-111,共3页Chinese Journal of Clinical Pharmacy

基　　金：常州市科技局项目(WZ200701);常州四药临床药学会科研基金

摘　　要：目的用探针药物法测定大黄对大鼠肝细胞色素CYP2E1酶的影响。方法将SD♂大鼠随机分组,给药组予大黄灌胃,以生理盐水组为空白对照,尾静脉给予CYP2E1探针药物氯唑沙宗,HPLC法检测体内药动学参数来评价各组的CYP2E1酶活性。结果氯唑沙宗代谢符合二室模型,给药组t12β(1.18±0.28)h、AUC(20.09±12.11)mg.h.L-1、V(c)(0.30±0.21)L、CL(s)(0.94±0.59)L.h-1,对照组t12β(1.49±0.14)h、AUC(38.87±8.35)mg.h.L-1、V(c)(0.21±0.06)L、CL(s)(0.12±0.02)L.h-1。结论大黄对大鼠肝细胞色素CYP2E1有诱导作用。AIM To determine the effect of the hepatic CYP2E1 activity following administration of Radix et Rhizoma Rhei by probe drug in rats. METHODS The rats were randomly divided into two groups. One group of rats were given orally Radix et Rhizoma Rhei once daily for seven days. The other group of rats were given orally normal saline once daily as the blank control group. Chlorzoxazone as the probe drug was administrated by vena caudalis. Concentrations of probe drug were determined by HPLC. CYP2E1 activity was evaluated by comparing the pharmaeokineties of chlorsoxazone in rats. RESULTS The chlorzoxazone metabolism corresponded to two-compartment model. The parameters after received RadixetRhizomaRhei were t1/2β（1.18 ± 0.28） h, AUC （20.09± 12.11）mg·h·L^-1, V（c）（0.30±0.21） L and CL（s） （0.94 ± 0.59） L·h^-1. The parameters of control group were t1/2β（ 1.49 ± 0.14） h, AUC （38.87 ± 8.35）mg·h·L^-1, V（c）（ 0.21 ±0.06） L,CL（s） （0.12±0.02） L·h^-1. CONCLUSION It suggests that Radix et RhizomaRhei tended to be the induction of the CYP2E1.

关 键 词：探针药物 CYP2E1 大黄 氯唑沙宗 

分 类 号：R285[医药卫生—中药学]