注射用头孢拉宗在中国健康人体的药代动力学研究  

Study on pharmacokinetics of cefbuperazone in Chinese healthy volunteers

作　　者：梅和坤[1] 王瑾[1] 王睿[1] 白楠[1] 梁蓓蓓[1] 曹江[1] 唐铭婧[1] 汶柯[1] 江学维[1] 牛卉[1] 王凯[1] 

机构地区：[1]解放军总医院转化医学中心,北京100853

出　　处：《中国临床药理学杂志》2015年第24期2417-2419,共3页The Chinese Journal of Clinical Pharmacology

摘　　要：目的研究注射用头孢拉宗在中国健康人体的药代动力学。方法用开放、随机、自身三交叉对照试验设计。12名受试者分别接受单次静脉滴注头孢拉宗1.0,2.0,3.0 g,通过高效液相色谱法测定头孢拉宗浓度。用WinNonlin5.2.1计算药代动力学参数。结果头孢拉宗的线性范围为2~250μg·mL^(-1),头孢拉宗1.0,2.0,3.0 g的主要药代动学参数:C_(max)分别为(81.74±15.95),(145.47±42.22),(198.16±36.03)μg·mL^(-1),t_(max)分别为(1.01±0.03),(1.02±0.04),(1.01±0.03)h;t_(1/2)分别为(1.80±0.30),(1.88±0.31),(1.74±0.27)h;AUC_(0-t)分别为(136.37±43.31),(263.74±93.95),(335.76±68.47)μg·mL^(-1)·h。16 h后的尿药累积排泄率分别为(45.24±17.50)%,(48.27±15.18)%,(40.82±14.24)%。结论受试者单次静脉滴注头孢拉宗1.0,2.0,3.0 g后药物体内过程呈一级线性动力学特征。Objective To evaluate the pharmacokinetics of cefbuperazone in Chinese healthy volunteers.Methods The study was designed as an open,randomized,self- control study.12 subjects were received1.0,2.0,3.0 g of cefbuperazone,respectively.Cefbuperazone was determined by high performance liquid chromatography.WinNonlin5.2.1 software was used to calculate the pharmacokinetic parameters.Results Linear range of cefbuperazone was 2- 250 μg·mL ^-1.The main pharmacokinetic parameters of three doses（1.0,2.0,3.0 g） of cefbuperazone were as follows：C_（max） were（81.74±15.95）,（145.47±42.22）,（198.16 ± 36.03） μg·mL^-1,t_（max） were（1.01±0.03）,（1.02 ± 0.04）,（1.01±0.03）,t_（1/2） were（1.80±0.30）,（1.88±0.31）,（1-74±0.27）,AUC_（0-t） were（136.37±43.31）,（263.74±93.95）,（335.76±68.47）μg·mL^-1 · h,respectively.Urinary recovery rate with 16 h was（45.24±17.50）%,（48.27±15.18）%,（40.82±14.24）%.Conclusion The characteristic of cefbuperazone is linear.

关 键 词：头孢拉宗 药代动力学 高效液相色谱法 血药浓度 尿排泄率 

分 类 号：R978.1[医药卫生—药品] R969.1[医药卫生—药学]