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引用本文:张俊,朱振峰,张晓坚,孙雅,赵咏梅.3种抗菌药物对辛伐他汀在人肝微粒体中代谢的影响[J].中国现代应用药学,2015,32(11):1363-1366.
ZHANG Jun,ZHU Zhenfeng,ZHANG Xiaojian,SUN Ya,ZHAO Yongmei.Effects of 3 Kinds of Antibacterial Agents on Metabolism of Simvastatin in Human Liver Microsome[J].Chin J Mod Appl Pharm(中国现代应用药学),2015,32(11):1363-1366.
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3种抗菌药物对辛伐他汀在人肝微粒体中代谢的影响
张俊, 朱振峰, 张晓坚, 孙雅, 赵咏梅
郑州大学第一附属医院药学部,郑州 450000
摘要:
目的 体外研究人肝微粒体中罗红霉素、左氧氟沙星和氟康唑分别对辛伐他汀代谢的影响。方法 分别将罗红霉素、左氧氟沙星、氟康唑与辛伐他汀在人肝微粒体中共孵育,采用UPLC-MS/MS测定辛伐他汀的浓度。结果 罗红霉素和左氧氟沙星对辛伐他汀的代谢没有影响,氟康唑剂量依赖性抑制辛伐他汀的代谢,其IC50值为36.6 μmol·L-1。结论 氟康唑显著抑制辛伐他汀的代谢,罗红霉素与左氧氟沙星对辛伐他汀在人肝微粒体中代谢无明显药物相互作用。
关键词:  辛伐他汀  人肝微粒体  超高效液相串联质谱  相互作用
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基金项目:常州四药临床药学科研基金(CZSYJJ11002)
Effects of 3 Kinds of Antibacterial Agents on Metabolism of Simvastatin in Human Liver Microsome
ZHANG Jun, ZHU Zhenfeng, ZHANG Xiaojian, SUN Ya, ZHAO Yongmei
Department of Pharmacy, the First Affiliated Hospital of Zhengzhou University, Zhengzhou 450000, China
Abstract:
OBJECTIVE To study the effects of roxithromycin, levofloxacin and fluconazole on the metabolism of simvastatin in human liver microsome respectively. METHODS Simvastatin was incubated with roxithromycin, levofloxacin and fluconazole in human liver microsome. The residual concentration of simvastatin in human liver microsome incubates was determined by UPLC-MS/MS. RESULTS The roxithromycin and levofloxacin had no significant influence on the metabolism of simvastatin. The IC50 of fluconazole for the metabolism of simvastatin was 36.6 μmol·L-1 and the inhibit intension was dose dependent. CONCLUTION The fluconazole significantly inhibits the metabolism of simvastatin. The roxithromycin and levofloxacin have no significant drug interactions on the metabolism of simvastatin.
Key words:  simvastatin  human liver microsome  UPLC-MS/MS  interactions
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