| 金雀异黄酮在体内对CYP3A活性的影响 |
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| 引用本文： | 肖昌琼,周宏灏.金雀异黄酮在体内对CYP3A活性的影响[J].中国临床药理学与治疗学,2011,16(6):643-646. |
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| 作者姓名： | 肖昌琼 周宏灏 |
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| 作者单位： | 1. 湖南省郴州市第一人民医院北院,郴州423000,湖南
2. 中南大学临床药理研究所,长沙410078,湖南 |
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| 基金项目： | 国家自然科学基金(30528026,30300428,30672497,30500623); 纽约中华医学会基金(01-755) |
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| 摘 要： | 目的:阐明金雀异黄酮在体内对细胞色素氧化酶P-4503A(CYP3A)活性的影响。方法:本试验采用双周期交叉临床试验。临床试验按照两阶段交叉方案进行。第一阶段随机分成的2组受试者随机给予金雀异黄酮片或安慰剂处理14 d,第15天给所有受试者米哒唑仑探针药,经过14 d洗脱期后交叉重复试验,分别以0~36 h血浆中米哒唑仑的血浆曲线下面积、半衰期作为CYP3A的活性指标。HPLC测定其活性。服药后0~36 h血中咪达唑仑以及1’-羟基咪达唑仑用HPLC-MS/MS方法测定。结果:经金雀异黄酮处理后,咪达唑仑AUC0-36 h明显降低(144±55)ng.mL-1.hvs(126±40)ng.mL-1.h,P<0.05],AUC0-∞显著降低(209±57)vs(181±43)ng.mL-1.h,P<0.05],Cmax显著降低(49±20)vs(36±14),P<0.05]。结论:金雀异黄酮对体内CYP3A酶活性具有显著的诱导作用,应当关注经CYP3A代谢的药物与金雀异黄酮合用时可能发生的潜在的药物相互作用。
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| 关 键 词： | 金雀异黄酮 CYP3A酶活性 药代动力学 |
Effects of genistein on cytochrome P450 3A activity in healthy volunteers |
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| XIAO Chang-qiong,ZHOU Hong-hao.Effects of genistein on cytochrome P450 3A activity in healthy volunteers[J].Chinese Journal of Clinical Pharmacology and Therapeutics,2011,16(6):643-646. |
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| Authors: | XIAO Chang-qiong ZHOU Hong-hao |
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| Institution: | XIAO Chang-qiong1,ZHOU Hong-hao21North Hospital,First People's Hospital of Chenzhou City,Chenzhou 423000,Hunan,China,2Pharmacogenetics Research Institute,Institute of Clinical Pharmacology,Central South University,Hunan 410078,Changsha |
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| Abstract: | AIM:To examine the potential effects of genistein on CYP3A activity. METHODS: The experiment was conducted in an open,randomized,2-period crossover study.The probe drug midazolam was used as an indicator of CYP3A function.Every volunteer was administered orally,once a day for 14 days,genistein 1000 mg or placebo(control).On 15th day,a 7.5 mg midazolam was administrated orally.The plasma concentration of midazolam,1-OH midazolam was determined over 36 h.RESULTS:Coadministration of genistein obviously decreas... |
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| Keywords: | Genistein CYP3A activity Pharmacokinetics |
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