【摘要】 目的检测氟喹诺酮类药物对肺炎链球菌临床分离株的防突变浓度(MPC),并探讨其与药动学参数的关系,为临床合理用药提供依据。方法采用琼脂二倍稀释法检测4种抗菌药物对25株肺炎链球菌临床分离株的MIC值,计算MIC50和MIC90值;采用新鲜制备的1010CFU/mL菌液测定MPC值,计算MPC50、MPC90和MPC/MIC比值,并探讨MPC值与药动学参数的关系。结果2种氟喹诺酮类药物中,莫西沙星的MPC值较低,MPC范围在0.5～2mg/L,MPC50和MPC90值分别为1mg/L和2mg/L,以400mg每日1次的药动学参数计算莫西沙星的Cmax/MPC90、AUC/MPC90分别为2.2和19.7;左氧氟沙星的MPC范围在2～4mg/L,MPC50和MPC90值分别为2mg/L和4mg/L,在左氧氟沙星3个剂量组中500mg组Cmax/MPC90、AUC/MPC90明显高于200mg与300mg组,分别为1.9和9.6。结论莫西沙星400mg每日1次、左氧氟沙星500mg每日1次的给药方案有望防止肺炎链球菌突变的发生。更多还原

【Abstract】 Objective To determine the mutant prevention concentration(MPC) of fluoroquinolones to S.pneumoniae and explore its relationship with clinical pharmacokinetics.Methods The MICs to S.pneumoniae were determined with the standard two-fold agar dilution method.MPCs were measured with the bacterial inoculated >1010CFU/mL.Its relationship with pharmacokinetic parameters was discussed.Results Moxifloxacin had lower MPC values ranging from 0.5 mg/L to 2 mg/L.The MPC50 and MPC90 were 1 mg/L and 2 mg/L,respectively.The Cmax/MPC90 and AUC/MPC90 values were 2.2 and 19.7,respectively.The MPC50 and MPC90 of levofloxacin were 2 mg/L and 4 mg/L.Its MPC ranged from 2 mg/L to 4 mg/L.The Cmax/MPC90 and AUC/MPC90 values of levofloxacin 500 mg once daily were 2.2 and 19.7,which were the highest among the three dosing regimens.Conclusions The regimens like moxifloxacin 400 mg or levofloxacin 500 mg once daily has advantage in resistance mutation prevention.更多还原