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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 effects of Scutellaria baicalensis Georgi on cytochrome P450 isoenzyme CYP1A2, CYP3A4, CYP2E1 and CYP2C19 in rats. Methods: The simultaneous determination of 4 kinds of probe drugs in rat plasma by high performance liquid chromatography method, the use of Cocktail probe drug method, the male SD rats were randomly divided into two groups, the administration group given sotalin extract suspension The control group was given the same dose of normal saline. After 10 days of administration, 4 kinds of probe drugs were injected through the tail vein, and blood was collected from orbital orifice. The activities of CYP1A2, CYP3A4, CYP2E1 and CYP2C19 were evaluated by measuring the metabolism of 4 kinds of probe drugs. Kinetica5.0 was used to calculate the pharmacokinetic parameters. Results: The T1 / 2 of 4 kinds of probe drugs increased compared with the control group, of which, the increase of T1 / 2 of dapsone, chlorzoxazone and omeprazole was significant. Dapsone, chlorzoxazone and Ogilvy The MRT0 → ∞ increased with the addition of prazosin, and the MRT0 → ∞ increased significantly with the addition of chlorzoxazone and omeprazole. Conclusion: Scutellariae extract has inhibitory effect on CYP1A2, CYP3A4, CYP2E1 and CYP2C19, of which CYP3A4, CYP2E1 and CYP2C19 have significant inhibitory effects.