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大鼠中CYP2C9活性的评估:单独使用甲苯磺丁脲以及与安非他酮联合使用的情况

Evaluation of CYP2C9 Activity in Rats: Use of Tolbutamide Alone and in Combined with Bupropion.

作者信息

Qiu Xiangjun, Song Jijun, Yuan Hongchang, Hou Yi, Pan Xiaofeng, Xu Ren-Ai

机构信息

Medical College of Henan University of Science and Technology, Luoyang 471003,China .

Children ' s Hospital of Zhengzhou, Zhengzhou 450053, China .

出版信息

Iran J Pharm Res. 2014 Spring;13(2):635-9.

PMID:25237359
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC4157039/
Abstract

A "cocktail"of several probe drugs is often used to evaluate metabolic activity of multiple cytochrome P450 enzymes in one session. Some interactions among probe drugs can appear and may impact the rate of biotransformation of other ones. Our presented work was aimed on the influence of bupropion on cytochrome P450-mediated metabolism of tolbutamide. The biotransformation rates of tolbutamide administered either separately or in combined with bupropion were compared in this study. The results revealed that bupropion had no significant effect on tolbutamide hydroxylation. Thus, due to stability in cytochrome P450 enzyme metabolic activity in the case of combining of two model probe drugs the procedure can show to no extent differential results comparing to the single-marker use.

摘要

几种探针药物的“鸡尾酒”通常用于在一次实验中评估多种细胞色素P450酶的代谢活性。探针药物之间可能会出现一些相互作用,这可能会影响其他药物的生物转化速率。我们目前的工作旨在研究安非他酮对细胞色素P450介导的甲苯磺丁脲代谢的影响。本研究比较了单独给予或与安非他酮联合给予甲苯磺丁脲时的生物转化速率。结果显示,安非他酮对甲苯磺丁脲的羟基化没有显著影响。因此,由于两种模型探针药物联合使用时细胞色素P450酶代谢活性的稳定性,与使用单一标记物相比,该方法在很大程度上不会显示出差异结果。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/dca6/4157039/f36b8a54217f/ijpr-13-635-g001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/dca6/4157039/f36b8a54217f/ijpr-13-635-g001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/dca6/4157039/f36b8a54217f/ijpr-13-635-g001.jpg

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本文引用的文献

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Drug Metab Lett. 2011 Jan;5(1):17-24. doi: 10.2174/187231211794455235.
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Profiling induction of cytochrome p450 enzyme activity by statins using a new liquid chromatography-tandem mass spectrometry cocktail assay in human hepatocytes.
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J Chromatogr B Analyt Technol Biomed Life Sci. 2010 May 1;878(15-16):1169-77. doi: 10.1016/j.jchromb.2010.03.026. Epub 2010 Mar 23.
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