摘要
目的:研究黄芩提取物对大鼠细胞色素P450同工酶CYP1A2,CYP3A4,CYP2E1,CYP2C19活性的影响。方法:建立同时测定大鼠血浆中4种探针药物的高效液相色谱方法,用Cocktail探针药物法,将雄性SD大鼠随机分为2组,给药组灌胃给予黄芩提取物混悬液,对照组灌胃给予相同剂量的生理盐水。给药10 d后尾静脉注射4种探针药物,眼眶取血,通过测定4种探针药物的代谢以评价CYP1A2,CYP3A4,CYP2E1,CYP2C19的活性,采用Kinetica5.0计算药代动力学参数。结果:4种探针药物的T1/2较对照组均有增加,其中氨苯砜、氯唑沙宗和奥美拉唑的T1/2增加显著;氨苯砜、氯唑沙宗和奥美拉唑的MRT0→∞均有增加,其中氯唑沙宗和奥美拉唑的MRT0→∞增加显著。结论:黄芩提取物对CYP1A2,CYP3A4,CYP2E1,CYP2C19均有抑制作用,其中对CYP3A4,CYP2E1,CYP2C19抑制作用显著。
Objective：To study the effect of Scutellaria extract to cytochrome P450 enzymes CYP1A2 CYP3A4,CYP2E1 and CYP2C19.Method： To establish an RP-HPLC method for the study of 4 probe drugs in rats plasma.The rats are divided in 2 groups randomly.One group were given Scutellaria extract once daily,another received normal saline once daily as the blank control.After 10 days of treatment,the rats were given 4 probe drugs by tail intravenous injection and the plasma were obtained at 0,5,10,15,30,15,60,180,360,540,720 min.The plasma concentration of 4 probe drugs was determined by RP-HPLC.The pharmacokinetic parameters were calculated by Kinetica 5.0.Result： The metabolism of dapsone,chlorzoxazone and omeprazole are slowed down significantly while the T1/2of all 4 probe drugs were increased.The MRT0→∞of chlorzoxazone and omeprazole were increased significantly.Conclusion：Scutellaria extract tended to be the inhibitor of CYP1A2,CYP3A4,CYP2E1 and CYP2C19.But CYP3A4 and CYP2E1 were affected significantly.
出处
《中国实验方剂学杂志》
CAS
北大核心
2012年第2期202-205,共4页
Chinese Journal of Experimental Traditional Medical Formulae
