抗菌药物药代动力学/药效学分析用于帕珠沙星临床试验中给药方案的指导

Dosing regimen selection for pazufloxacin tablet in clinical trial based on its pharmacokinetic/pharmacodynamic analysis

目的预测帕珠沙星的临床试验中可能的给药方案。方法通过已经获得的药代动力学数据、蛋白结合率数据以及细菌敏感性数据,用蒙特卡洛模拟的方法,计算不同给药方案在不同的药代动力学/药效学(PK/PD)靶值下的达标概率(PTA),并与对照药左氧氟沙星进行比较。结果帕珠沙星日剂量1000 mg与左氧氟沙星750 mg的达标概率相近。结论根据模拟的结果,推荐了帕珠沙星500 mg bid的给药方案用于临床研究。

Objective To predict the possible closing regimen for the clinical study of pazufloxacin.Methods Based on the pharmacokinetic parameters of pazufloxacin,its protein binding rates and bacterium susceptible data,the probability of target attainment（PTA） was calculated at different pharmacokinetic/pharmacodynamic（PK/PD） target values through Monte Carol simulation and was compared with the values of reference drug levofoxacin.Results The results showed the PTAs of daily dose of 1000 mg pazufloxacin to similar pathogens was comparable with that of daily dose of 750 mg of levofloxacin.Conclusion Based on the simulated data,500 mg bid of pazufloxacin was recommended for the further clinical studies.