Zhang Shu-qiu, Zhang Li-feng, Xing Jie, Zhong Da-fang
Laboratory of Drug Metabolism and Pharmacokinetics, Shenyang Pharmaceutical University, Shenyang 110016, China.
Yao Xue Xue Bao. 2003 May;38(5):374-9.
To investigate the metabolic profile of roxithromycin in dogs and the effects of oral and intravenous administrations on the metabolism of roxithromycin.
Liquid chromatography-tandem mass spectrometry (LC-MSn) was used for separation and analysis of roxithromycin and its metabolites in dog bile after an oral dose or intravenous dose of roxithromycin. The metabolites were identified by comparisons of their mass spectra and LC behaviors with the references.
Totally 13 metabolites were detected in dog bile, including N-demethylated derivatives, N, N-didemethylated derivatives, O-dealkylether derivatives, decladinose derivatives, and the geometric isomers of parent drug and its metabolites.
Roxithromycin underwent 4 metabolic pathways in which geometric isomerization and decladinose metabolism were found to be markedly different between the two administration routes.
研究罗红霉素在犬体内的代谢概况以及口服和静脉给药对罗红霉素代谢的影响。
采用液相色谱-串联质谱法(LC-MSn)对口服或静脉给予罗红霉素后犬胆汁中的罗红霉素及其代谢产物进行分离和分析。通过将其质谱和液相色谱行为与对照品进行比较来鉴定代谢产物。
在犬胆汁中总共检测到13种代谢产物,包括N-去甲基化衍生物、N,N-双去甲基化衍生物、O-去烷基醚衍生物、去克拉定糖衍生物以及母体药物及其代谢产物的几何异构体。
罗红霉素经历了4条代谢途径,其中几何异构化和去克拉定糖代谢在两种给药途径之间存在明显差异。