Demethylation metabolism of roxithromycin in humans and rats  

人与大鼠体内罗红霉素去甲基化代谢(英文)

作　　者：李雪庆[1] 钟大放[1] 黄海华[2] 吴硕东 

机构地区：[1]沈阳药科大学药物代谢与药物动力学实验室,沈阳中国110016 [2]沈阳药科大学微生物教研室,沈阳中国110016 [3]中国医科大学第二临床学院,沈阳中国110003

出　　处：《Acta Pharmacologica Sinica》2001年第5期89-94,共6页中国药理学报（英文版）

基　　金：Project supported by the National Natural Science Foundation of China, No 39625025 and 39930180

摘　　要：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.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。

关 键 词：ROXITHROMYCIN METABOLISM macrolide antibiotics liquid chromatography mass spectrum analy-sis 

分 类 号：R96[医药卫生—药理学]