索西沙星在小鼠体内的药物代谢动力学研究  

Pharmacokinetic studies of chinfloxacin in mouse

作　　者：李国庆[1] 庞晶[1] 杨信怡[1] 李聪然[1] 游雪甫[1] 

机构地区：[1]中国医学科学院/北京协和医学院,医药生物技术研究所,北京100050

出　　处：《药学研究》2013年第6期311-313,共3页Journal of Pharmaceutical Research

基　　金：国家自然科学基金(81273427);国家十二五科技重大专项(2012ZX09301002)

摘　　要：目的研究索西沙星在小鼠体内的药物代谢动力学,分析索西沙星的药物代谢动力学/药物效应动力学(PK/PD)参数。方法使用HPLC-MS/MS法,以莫西沙星为内标,以梯度甲醇-水为流动相,测定灌胃5 mg.kg-1后小鼠血液中索西沙星的含量。以WinNonlin软件计算动力学参数。结果小鼠血液中索西沙星Cmax为1.085μg.mL-1,Tmax为10 min,T1/2为1.425 h,AUC0～24为1.101μg.mL-1.h,对金黄色葡萄球菌、肺炎链球菌、流感嗜血杆菌、副流感嗜血杆菌和化脓链球菌的Cmax/MIC50均大于8。结论索西沙星在小鼠体内的吸收、分布及代谢较快,对多种细菌具有较好的活性。Objective To determine the pharmacokinetics of chinfloxacin in mouse,and analyze the PK /PD parameters.Methods Chinfloxacin in mouse plasma after intragastric administration in 5 mg.kg-1 was determined by HPLC-MS / MS with moxifloxacin as internal standard.Methanol-water was used as the mobile phase.Then the parameters were calculated with WinNonlin.Results The Cmax was 1.085 μg.mL-1,Tmax was 10 min,T1 /2 was 1.425 h,AUC0 ～ 24 was 1.101 μg.mL-1.h in mouse plasma,and the Cmax/ MIC50 of S.aureus,S.pneumoniae,H.influenza,H.parainfluenzae and S.pyogenes were all above 8.Conclusion Chinfloxacin was absorbed,distributed and eliminated fast in mouse,and showed good activity against some kinds of bacteria.

关 键 词：索西沙星 小鼠药物代谢动力学 药物代谢动力学 药物效应动力学参数 

分 类 号：R969.1[医药卫生—药理学]