二氟沙星在猪体内的药物动力学及生物利用度研究  

Pharmacokinetics and Bioavailability of Difloxacin in Pigs

作　　者：曾振灵[1] 丁焕中[1] 黄显会[1] 陈杖榴[1] 

机构地区：[1]广东省兽药研制与安全评价重点实验室/华南农业大学兽医学院,广州510642

出　　处：《中国农业科学》2003年第7期846-850,共5页Scientia Agricultura Sinica

基　　金：广东省科技攻关资助项目 (2 0 0 2C2 0 2 10 )

摘　　要：7头健康杂种猪 ,按照随机拉丁方设计 ,进行静注、肌注及内服二氟沙星 (5mg·kg-1)的药物动力学研究。血浆样品经甲醇沉淀血浆蛋白 ,高速离心 ,用反相高效液相色谱法测定猪血浆中二氟沙星的浓度 ,MCPKP计算机程序处理血浆药物浓度 时间数据。健康猪静注给药的药时数据适合二室开放模型 ,主要药物动力学参数为 :t1/ 2α1.5 8± 0 .6 4h ;t1/ 2 β17.14± 4.14h ;V11.34± 0 .16L·kg-1;Vd(area) 4.91± 1.88L·kg-1;ClB0 .2 0± 0 .0 6L·kg-1·h-1;AUC2 7.2 4± 8.12mg·L-1·h。健康猪肌注、内服给药的药时数据均适合一级吸收二室模型 ,主要药物动力学参数为 :t1/ 2ka0 .47± 0 .2 2和 0 .5 4± 0 .44h ;t1/ 2 β2 5 .79± 8.10和 16 .6 7± 4.0 4h ;tmax1.2 9± 0 .2 6h和 1.41± 0 .88h ;Cmax1.77±0 .6 6和 2 .2 9± 0 .85mg·L-1;AUC 2 4.98± 9.2 9和 2 6 .5 9± 5 .30mg·L-1·h-1;F (95 .3± 2 8.9) %和 (10 5 .7± 37.1) %。二氟沙星在健康猪体内的主要药物动力学特征为 :吸收迅速 ,达峰时间短 ,表观分布容积大 ,消除半衰期长 ;肌注、内服给药吸收完全 ;生物利用度高。Pharmacokinetics of difloxacin was investigated in 7 healthy cross-bred pigs following single intravenous, intramuscular and oral administration of the drug at the dose of 5 mg·kg -1 BW. Blood samples were collected at different intervals after administration and concentrations of difloxacin were determined by HPLC method with a limit of detection of 0.05 μg·ml -1. The difloxacin concentration-time data were fitted to a two-compartment open model after single i.v. dosing in pigs. The main pharmacokinetic parameters were as follows: t 1/2α 1.58±0.64 h; t 1/2β 17.14±4.14 h; V 1 1.34± 0.16 L·kg -1; V d(area) 4.91±1.88 L·kg -1; Cl B 0.20±0.06 L·kg -1·h -1; AUC 27.24±8.12 mg·L -1·h -1. The drug concentration-time data were both fitted to a two-compartment model with first order absorption after single i.m. and p.o. administration in pigs. The main pharmacokinetic parameters were as follows: t 1/2ka 0.47±0.22 and 0.54±0.44 h; t 1/2β 25.79±8.10 and 16.67±4.04 h; t max 1.29±0.26 and 1.41±0.88 h; C max 1.77±0.66 and 2.29±0.85 mg·L -1; AUC 24.98±9.29 and 26.59±5.30 mg·L -1·h -1; F (95.3±28.9)% and (105.7±37.1)%. The results of present studies showed that difloxacin was rapidly absorbed, extensively distributed and slowly eliminated in pigs. The drug was completely absorbed after single i.m. and p.o. administration and had a good bioavailability in pigs.

关 键 词：二氟沙星 猪 药物动力学 生物利用度 浓度 浓度 MCPKP计算机 

分 类 号：S859.79[农业科学—临床兽医学]