左氧氟沙星静滴液中年健康人体药动学研究  

Pharmacokinetics of single 500-milligram doses of intravenous levofloxacin in middle-age healthy volunteers

作　　者：李燕明[1] 孙铁英[1] 姚婉贞[2] 左明新[1] 付逸龙[1] 李可欣[1] 

机构地区：[1]卫生部北京医院,北京100730 [2]北京大学第三医院,北京100083

出　　处：《中国新药杂志》2004年第12期1144-1147,共4页Chinese Journal of New Drugs

摘　　要：目的:研究500mg左氧氟沙星静滴液在我国中年健康人群中的药动学特点并进行安全性评价。方法:10例中年健康志愿者接受单次静脉滴注500mg 左氧氟沙星后,固定时间采取血样及尿样,采用高效液相色谱法检测血及尿中的左氧氟沙星浓度。血样以高氯酸沉淀法进行预处理。结果:药动学符合静脉给药二室开放模型,C_(max)为(9.03±1.92)mg·L^(-1),t_(1/2)β为(7.99±1.69)h,V_d 为(1.24±0.31)L·kg^(-1),CL/F 为(11.64±2.51)L·h^(-1),用梯形法计算所得的AUC 为(44.79±9.05)mg·h·L^(-1)。24h 左氧氟沙星尿中的排泄率为(76.78±9.07)%。10例志愿者均顺利完成实验,仅1例出现失眠。结论:左氧氟沙星单次500mg 静脉滴注主要药动学参数与国外报道相仿,不良反应发生率低。高剂量左氧氟沙星应可作为严重或敏感性降低细菌感染的选择之一。Objective:To assess the safety and pharmacokinetic profile of levofloxacin.Method:4 male and 6 female healthy subjects at 48～56 years of age were i.v.given with a single dose of lev-ofloxacin (500mg).Blood and urine samples from the tested subjects were collected at fixed schedulesto assay levofloxacin concentrations in plasma and urine samples by a validated HPLC.Results:Thepharmacokinetic profile of levofloxacin was coincident with a two-compartment open model,and themain parameters were as follows:C_(max)=(9.03±1.92)mg·L^(-1),t_(1/2)β=(7.99±1.69)h,V_d=(1.24±0.31)L·kg^(-1),CL/F=(11.64±2.51)L·h^(-1),AUC=(44.79±9.05)mg·h·L^(-1),and therenal clearance rate was (76.78±9.07)% within 24 hours.Levofloxacin was well tolerated.Conclu-sion:No significant discrepancy between the Chinese population and Western population was found inthe pharmacokinetic parameters.Highly dosing of levofloxacin may offer an option in the treatment ofsevere infections and the infections that are unresponsive well to other antibiotics.

关 键 词：左氧氟沙星 药动学 高效液相色谱法 安全性 

分 类 号：R978.1[医药卫生—药品] R969.1[医药卫生—药学]