头孢喹肟在猪体内的药动学及生物利用度  

Pharmacokinetics and bioavailability of cefquinome in pigs

作　　者：杨大伟[1,2] 陈杖榴[2] 丁焕中[2] 沈祥广[2] 徐夙素[1] 古小燕[2] 

机构地区：[1]中国兽医药品监察所,北京100081 [2]华南农业大学兽医学院广东省兽药研制与安全评价重点实验室,广东广州510642

出　　处：《中国兽医学报》2009年第9期1182-1185,共4页Chinese Journal of Veterinary Science

基　　金：国家"十一五"科技支撑计划重点课题"新型抗菌原料药的研制与应用"资助项目(2006BAD31B01)

摘　　要：10头健康杂种猪,随机交叉设计试验,头孢喹肟按1 mg/kg的剂量分别进行耳缘静脉和颈部肌肉单点注射给药,给药间隔时间为1周。采用反相高效液相色谱法测定血清中头孢喹肟的药物浓度,用药代动力学程序软件3P97处理血清中药物浓度-时间数据。结果表明,静脉注射给药后,猪血清中头孢喹肟的药时数据符合二室开放模型,其主要药动学参数为:t1/2α为0.16 h,t1/2β为1.34 h,V(c)为0.24 L.kg-1,Cl(s)为0.26 L.kg-1.h-1,AUC为3.97 mg.L-1.h;颈部肌肉单点注射给药后,猪血清中头孢喹肟的药时数据符合一级吸收二室模型,其主要药动学参数为:t1/2ka为0.08 h,t1/2α为0.84 h,t1/2β为2.76 h,t(max)为0.32 h,C(max)为1.80 mg.L-1,Cl(s)为0.25 L.kg-1.h-1,AUC为4.12 mg.L-1.h,F为102.37%。The pharmacokinetics of cefquinome and the bioavailability were investigated by a cross over design following single intravenous （1 mg/kg） and intramuscular （1 mg/kg） administration of the drug in 10 healthy pigs. A 7-day washout period was allowed between different treatments. The concentrations of cefquinome in serum were determined by HPLC and the concentration-time data were analyzed with 3P97 program. It ＇s best to fit the cefquinome concentration-time data to two-compartment open model after single i. v. dosing. The main pharmacokinetic parameters were as follows：t1/2α 0.16 h,t1/2β 1.34 h ,V（c） 0.24 L · kg^- 1 ,Cl（s） 0.26 L · kg^-1 · h^- 1 ,AUC 3.97 mg· L^- 1 · h. A two-compartment model with first order absorption best described the drug concentration-time data after single i. m. administration in healthy pigs. The main pharmacokinetic parameters were as follows： t1/2ka 0.08 h, t1/2α 0.84 h,t1/2β 2.76 h ,t（peak） 0.32 h,C（max） 1.80mg· L^-1,Cl（s） 0.25 L· kg^-1 · h^-1,AUC4.12 mg· L^-1 · h,F 102.37%.

关 键 词：头孢喹肟 猪 药动学 生物利用度 高效液相色谱法 

分 类 号：S859.796[农业科学—临床兽医学]