| 大鼠肝细胞色素P4503A活性测定及其孵育条件的优化 |
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| 引用本文： | 任秀华,曹磊,斯陆勤,薛柯雯,裘军,李高.大鼠肝细胞色素P4503A活性测定及其孵育条件的优化[J].中国医院药学杂志,2010(10). |
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| 作者姓名： | 任秀华 曹磊 斯陆勤 薛柯雯 裘军 李高 |
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| 作者单位： | 华中科技大学同济医学院附属同济医院药学部;华中科技大学同济医学院药学院; |
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| 基金项目： | 国家自然科学基金资助项目(编号:30572265) |
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| 摘 要： | 目的:测定大鼠肝微粒体中细胞色素P4503A(CYP3A)的活性,并对其体外孵育条件进行优化。方法:采用1’-羟基咪哒唑仑的生成量表示肝中CYP3A的活性,高效液相色谱法测定肝微粒体中1’-羟基咪哒唑仑的浓度,用单因素试验法对其体外孵育条件进行优化,用线性Lineweaver-Burk双倒数作图法研究肝CYP3A酶促动力学。结果:1’-羟基咪哒唑仑在18.20~1 820.00μg.L-1范围内线性关系良好;体外优化的孵育条件为5μmol.L-1咪哒唑仑、0.102mg肝微粒体、孵育15min;肝CYP3A酶促动力学参数Km为1.67μmol.L-1,Vmax为95.15pmol.min-1.mg-1。结论:HPLC法操作简便、灵敏、快速,适用于肝微粒体中1’-羟基咪哒唑仑的浓度测定,肝CYP3A孵育条件及其酶促动力学研究为研究经CYP3A代谢的药物相互作用及其他物质对CYP3A酶的影响提供理论依据。
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| 关 键 词： | CYP3A活性 肝微粒体 高效液相色谱法 1’-羟基咪哒唑仑 优化 大鼠 |
Determination of the activity of cytochrome P450 3A in rat liver microsomes by HPLC and optimization of the incubated conditions in vitro |
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| REN Xiu-hua,CAO Lei,SI Lu-qin,XUE Ke-wen,QIU Jun,LI Gao.Determination of the activity of cytochrome P450 3A in rat liver microsomes by HPLC and optimization of the incubated conditions in vitro[J].Chinese Journal of Hospital Pharmacy,2010(10). |
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| Authors: | REN Xiu-hua CAO Lei SI Lu-qin XUE Ke-wen QIU Jun LI Gao |
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| Institution: | REN Xiu-hua1,2,CAO Lei2,SI Lu-qin2,XUE Ke-wen2,QIU Jun2,LI Gao2(1.Pharmacy of Tongji Hospital.Tongji Medical College,Huazhong University of Science and Technology,Hubei Wuhan 430030,China,2.Department of Pharmaceutics,School of Pharmacy,Tongji Medical College,China) |
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| Abstract: | OBJECTIVE To determine the activity of CYP3A and optimize the incubated conditions in the liver microsomes of rats.METHODS The formation of 1'-hydroxymidazolam determined by HPLC was used to indicate the activity of CYP3A.Single effect experimental design was used to optimize the incubated conditions and the enzyme kinetics was evaluated by graphical analysis with Lineweaver-Burk double reciprocal plots(1/velocity vs.1/ substrate]).RESULTS Calibration curves of 1'-hydroxymidazolam were linear in the range ... |
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| Keywords: | activity of CYP3A liver microsomes HPLC 1'-hydroxymidazolam optimization rat |
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