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36.6μmol·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。
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.
出处
《中国现代应用药学》
CAS
CSCD
2015年第11期1363-1366,共4页
Chinese Journal of Modern Applied Pharmacy
基金
常州四药临床药学科研基金(CZSYJJ11002)
