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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。
OBJECTIVE: To study the demethylation pathway of roxithromycin in human and rat and to study the antibacterial activity of demethyl roxithromycin in vitro.METHODS: The determination of roxithromycin in human and The metabolites of demethylated products in rats were determined. Three kinds of bioassay test strains were selected by double dilution method. The antibacterial activities of roxithromycin, demethylated metabolites and several other major metabolites were determined in vitro. Results: Roxithromycin mainly undergoes O-demethylation metabolism in the human body, whereas N-demethylated metabolism mainly undergoes in vivo in rats. The metabolite O-desmethyl roxithromycin has comparable in vitro antibacterial activity as the parent drug. Conclusion: O-desmethyl roxithromycin is the active metabolite of roxithromycin in humans. Roxithromycin has species divergence in human and rat demethylation products.