@article{APS7452,
author = {Xue-Qing Li and Da-Fang Zhong and Hai-Hua Huang and Shuo-Dong Wu},
title = {Demethylation metabolism of roxithromycin in humans and rats},
journal = {Acta Pharmacologica Sinica},
volume = {22},
number = {5},
year = {2016},
keywords = {},
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 chromatography-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.
Conclusion: The O-demethyl-RXM was an active metabolite in humans, and there were some species differences in RXM demethylation metabolism between humans and rats.},
issn = {1745-7254}, url = {http://www.chinaphar.com/article/view/7452}
}