| 人与大鼠体内罗红霉素去甲基化代谢(英文) |
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| 引用本文： | 李雪庆,钟大放,黄海华,吴硕东.人与大鼠体内罗红霉素去甲基化代谢(英文)[J].中国药理学报(英文版),2001,22(5):469-474. |
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| 作者姓名： | 李雪庆 钟大放 黄海华 吴硕东 |
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| 作者单位： | 沈阳药科大学药物代谢与药物动力学实验室，沈阳药科大学药物代谢与药物动力学实验室，沈阳药科大学微生物教研室，中国医科大学第二临床学院 沈阳，中国 110016，沈阳，中国 110016，沈阳，中国 110016，沈阳，中国 110003 |
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| 基金项目： | Project supported by the National Natural Science Foundation of China, No 39625025 and 39930180 |
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| 摘 要： | 目的:研究罗红霉素在人体和大鼠体内的去甲基化代谢途径,并研究去甲基罗红霉素的体外抗菌活性方法:采用LC-MS方法测定了罗红霉素在人体和大鼠体内的去甲基代谢产物;并用二倍稀释法,选择三种生物检测实验标准菌株,测定了罗红霉素、去甲基代谢产物以及其他几种主要代谢产物的体外抗菌活性。结果:罗红霉素在人体内主要经历O-去甲基化代谢,而在大鼠体内主要经历N-去甲基化代谢。代谢物O-去甲基罗红霉素具有与母体药相当的体外抗菌活性。结论:O-去甲基罗红霉素是罗红霉素在人体内的活性代谢产物,罗红霉素在人与大鼠体内的去甲基化产物具有种属差异。
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| 关 键 词： | 罗红霉素 代谢 大环内酯抗菌素 液相色谱法 质量光谱分析 |
Demethylation metabolism of roxithromycin in humans and rats |
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| LI Xue-Qing,ZHONG Da-Fang,HUANG Hai-Hua,WU Shuo-Dong.Demethylation metabolism of roxithromycin in humans and rats[J].Acta Pharmacologica Sinica,2001,22(5):469-474. |
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| Authors: | LI Xue-Qing ZHONG Da-Fang HUANG Hai-Hua WU Shuo-Dong |
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| Institution: | Laboratory of Drug Metabolism and Pharmacokinetics, Shenyang Pharmaceutical University, Shenyang 110016, China. |
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| Abstract: | AIM: To investigate the demethylated metabolites of roxithromycin (RXM) in humans and rats, and to study the antibiotic activity of these metabolites in vitro. METHODS: The demethylated metabolites of RXM in humans and in rats were identified by liquid chromatogra-phy-mass spectrometry (LC-MS), and the in vitro antibiotic activities of them against three standard strains were also studied compared with those of the parent drug and some other metabolites of RXM. RESULTS: O-Demethylation of RXM was one of the main metabolic routes of RXM in humans, whereas N-demethylation metabolism was more predominant in rats. O-Demethyl-RXM appeared to be equally effective with RXM. CONCLUTION: The O-demethyl-RXM was an active metabolite in humans, and there were some species differences in RXM demethylation metabolism between humans and rats. |
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| Keywords: | roxithromycin metabolism macrolide antibiotics liquid chromatography mass spectrum analy-sis |
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