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临床上广泛使用的 (E) -罗红霉素在人体内有多种代谢途径。在鉴别和制备其代谢产物的基础上 ,采用二倍稀释法 ,选用 3种生物检测实验标准菌株 ,测定了母体药物和 6种主要代谢产物的体外抗菌活性(MIC,MBC)。结果表明 ,(E) -罗红霉素经代谢转化后 ,生成的 (Z) -罗红霉素异构体的活性略下降 ,(E) -红霉素肟的活性无明显改变 ,(E) - O-单去甲罗红霉素的 MIC未改变 ,而对芽孢杆菌的 MBC有所降低 ,(E) - N-单去甲罗红霉素的活性显著降低 ,(E) -脱红霉糖罗红霉素则基本失活。被测药物及代谢物在不同菌株之间的MIC和 MBC变化趋势基本相同 ,MBC较相应的 MIC大 10 0～ 10 0 0倍左右。
Clinically widely used (E) - roxithromycin in the human body has a variety of metabolic pathways. On the basis of identification and preparation of its metabolites, three kinds of bioassay test strains were selected by double dilution method. The in vitro antibacterial activity (MIC, MBC) of the parent drug and six main metabolites were determined. The results showed that the activity of (Z) - roxithromycin isomers decreased slightly after the transformation of (E) - roxithromycin and the activity of (E) - erythromycin oxime did not change significantly ) - The MIC of O-monovagrythromycin was unchanged, whereas the MBC of Bacillus was decreased, the activity of (E) -N-monascorubicin significantly decreased, (E) -reduced Roxithromycin is basically inactivated. The trends of MIC and MBC of tested drugs and metabolites in different strains are basically the same, MBC is about 10 0 ~ 100 times larger than the corresponding MIC.