药学与临床研究
藥學與臨床研究
약학여림상연구
PHARMACEUTICAL AND CLINICAL RESEARCH
2014年
4期
306-309
,共4页
汪辉%苏珊%陈向东%姜剑伟%王岩岩%靳悦
汪輝%囌珊%陳嚮東%薑劍偉%王巖巖%靳悅
왕휘%소산%진향동%강검위%왕암암%근열
泰比培南%大腿感染模型%PK/PD
泰比培南%大腿感染模型%PK/PD
태비배남%대퇴감염모형%PK/PD
Tebipenem%Thigh infection model%PK/PD
目的:通过泰比培南对小鼠大腿克雷伯菌感染模型PK/PD研究,预测最佳PK/PD参数。方法:选用临床肺炎克雷伯菌1株,采用琼脂二倍稀释法检测药物的最低抑菌浓度(MIC);构建小鼠的肺炎克雷伯菌大腿感染模型,分三种剂量(50、15、3 mg·kg-1)给予受试药物,观察给药24 h后大腿组织感染量变化,并采用HPLC法检测血药浓度。结果:体外测得MIC为0.03μg· mL-1;在小鼠的肺炎克雷伯菌大腿感染模型中,50、15、3 mg·kg-1三种剂量均对感染有治疗作用, PK/PD参数AUC/MIC、Cmax/MIC、T>MIC的相关系数r2分别为0.8、0.75、0.54。结论:体内PK/PD研究表明,AUC/MIC、Cmax/MIC参数是反映泰比培南对小鼠的肺炎克雷伯菌大腿感染治疗效果主要的PK/PD参数。
目的:通過泰比培南對小鼠大腿剋雷伯菌感染模型PK/PD研究,預測最佳PK/PD參數。方法:選用臨床肺炎剋雷伯菌1株,採用瓊脂二倍稀釋法檢測藥物的最低抑菌濃度(MIC);構建小鼠的肺炎剋雷伯菌大腿感染模型,分三種劑量(50、15、3 mg·kg-1)給予受試藥物,觀察給藥24 h後大腿組織感染量變化,併採用HPLC法檢測血藥濃度。結果:體外測得MIC為0.03μg· mL-1;在小鼠的肺炎剋雷伯菌大腿感染模型中,50、15、3 mg·kg-1三種劑量均對感染有治療作用, PK/PD參數AUC/MIC、Cmax/MIC、T>MIC的相關繫數r2分彆為0.8、0.75、0.54。結論:體內PK/PD研究錶明,AUC/MIC、Cmax/MIC參數是反映泰比培南對小鼠的肺炎剋雷伯菌大腿感染治療效果主要的PK/PD參數。
목적:통과태비배남대소서대퇴극뢰백균감염모형PK/PD연구,예측최가PK/PD삼수。방법:선용림상폐염극뢰백균1주,채용경지이배희석법검측약물적최저억균농도(MIC);구건소서적폐염극뢰백균대퇴감염모형,분삼충제량(50、15、3 mg·kg-1)급여수시약물,관찰급약24 h후대퇴조직감염량변화,병채용HPLC법검측혈약농도。결과:체외측득MIC위0.03μg· mL-1;재소서적폐염극뢰백균대퇴감염모형중,50、15、3 mg·kg-1삼충제량균대감염유치료작용, PK/PD삼수AUC/MIC、Cmax/MIC、T>MIC적상관계수r2분별위0.8、0.75、0.54。결론:체내PK/PD연구표명,AUC/MIC、Cmax/MIC삼수시반영태비배남대소서적폐염극뢰백균대퇴감염치료효과주요적PK/PD삼수。
To elucidate the pharmacokinetic/pharmacodynamic(PK/PD) parameters that predict tebipenem efficacy against Klebsiella pneumoniae in murine thigh infection model. Methods: The minimal inhibitory concentration (MIC) of tebipenem against Klebsiella pneumoniae was determined by standard two-fold agar dilution method; three doses of 50, 15 and 3 mg·kg-1 were administrated in thigh infection model mice, respectively. The bacterial burden in thigh was measured at 24 h after the initiation of treatment and the drug concentration in plasma was determined by HPLC. Results: The MIC was 0.03μg·mL-1. The drug at all three doses of 50, 15 and 3 mg·kg-1 was effective in murine thigh infection model. Three PK/PD pa-rameters that correlated with efficacy of tebipenem were AUC/MIC (R2=0.8), Cmax/MIC (R2=0.75) and T>MIC (R2=0.54). Conclusions: PK/PD study indicates that AUC/MIC and Cmax/MIC are PK/PD parameters that correlated better with efficacy of tebipenem against Klebsiella pneumoniae in murine thigh infection model.