液相色谱-电喷雾离子阱质谱法研究人尿中阿奇霉素的主要代谢产物  

Study on essential metabolites of azithromycin in human urine by liquid chromatography-mass spectrometry

作　　者：孙璐[1] 胡艳玲[1] 杨亚楠[1] 包凯[1] 

机构地区：[1]沈阳药科大学

出　　处：《中国临床药理学与治疗学》2009年第9期984-989,共6页Chinese Journal of Clinical Pharmacology and Therapeutics

摘　　要：目的:研究阿奇霉素在人尿中的主要代谢产物。方法:受试者口服阿奇霉素后收集0～144 h尿样,经Strata C18-E固相萃取小柱分离纯化后,采用液相色谱-电喷雾离子阱质谱法(LC/ESI-MSn)对样品进行分析,通过比较空白尿样和给药后尿样的总离子流色谱图和选择离子监测色谱图,分析可能的代谢产物。结果:在人尿中共发现了8种代谢产物,通过与得到的代谢产物对照品比较,鉴定出2种代谢产物的结构,并推测出其他6种代谢产物的化学结构。阿奇霉素在人体内的主要代谢途径包括O-去甲基、N-去甲基、N-去甲基后去红霉糖和羟基化。结论:本研究为深入了解阿奇霉素在人体内的代谢情况提供了可靠的方法和参考依据。AIM：To investigate the essential metabolites of azithromycin in human urine.METHODS： The urine samples of the volunteers after an oral administration of 500 mg azithromycin tablets were collected for 0-144 h,the samples were purified and separated through Strata C18-E solid-phase extraction column and analyzed with liquid chromatography-mass spectrometry.The potential metabolites were analyzed through comparing the TIC and SIM chromatograms of the blank urine and sample urine,and the structure of the metabolites were identified through the correlation of the full scan MSn spectra of azithromycin and the metabolites.RESULTS： Eight metabolites were found in human urine,4 metabolites were identified,the major metabolic pathways of azithromycin in human were O-demethylation,N-demethylation,N-desmethyl descladinose and hydroxylation.CONCLUSION： The research is possible to supply a reliable reference for further study on the metabolites of azithromycin.

关 键 词：液相色谱-电喷雾离子阱质谱法 阿奇霉素 代谢产物 

分 类 号：R969.1[医药卫生—药理学]