二氟沙星在鸡体内的药物代谢动力学及生物利用度研究  

Study on pharmacokinetics and bioavailability of difloxacin in chickens

作　　者：丁焕中[1] 曾振灵[1] 杨桂香[1] 黄显会[1] 陈杖榴[1] 

机构地区：[1]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：《中国兽医科技》2004年第6期20-24,共5页Chinese Journal of Veterinary Science and Technology

基　　金：广东省科技攻关资助项目 (2 0 0 2C2 0 2 10 )

摘　　要：将 30只艾维茵肉鸡随机分为 3组 ,进行了静脉注射、肌肉注射及内服二氟沙星的药物代谢动力学研究。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鸡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。结果 ,健康鸡静脉注射给药的药时数据适合二室开放模型 ,主要药物代谢动力学参数为 :t1/ 2α=0 .6 9h± 0 .4 3h ;t1/ 2 β=6 .11h± 1.5 0h ;V1=1.70L/kg±0 .33L/kg ;Vd(area) =3.10L/kg± 0 .6 7L/kg ;ClB=0 .37L/ (kg·h)±0 .10L/ (kg·h) ;AUC =2 9.16 μg/ (mL·h)± 8.0 4 μg/ (mL·h)。健康鸡肌肉注射及内服给药的药时数据适合一级吸收一室模型 ,前者的主要药物代谢动力学参数为 :t1/ 2Ka=0 .17h± 0 .12h ,t1/ 2Ke=5 .6 4h± 0 .74h ,tmax =0 .86h± 0 .4 0h ,Cmax =2 .5 1μg/mL± 0 .36 μg/mL ,AUC =2 2 .6 2μg/ (mL·h) ± 3.2 8μg/ (mL·h) ,F =77.0 %± 11.8% ;后者的药物代谢动力学参数为 :t1/ 2Ka=1.4 6h± 1.0 0h ,t1/ 2Ke=8.2 0h± 3.12h ,tmax=4 .34h± 2 .4 0h ,Cmax=1.0 0 μg/mL± 0 .2 1μg/mL ,AUC =15 .82 μg/ (mL·h) ± 3.6 7μg/ (mL·h) ,F =5 4.2 %± 12 .6 %。二氟沙星在健康鸡体内的主要药物代谢动力学特征为Thirty healthy Avine broiler chickens were allotted to 3 groups at 10 chickens per group. Pharmacokinetics of difloxacin was investigated in the 30 healthy Avine broiler chickens following single intravenous,intramuscular and oral administration at the dose of 10 mg/ kg, respectively. Blood samples were collected at different intervals after administration and difloxacin concentrations were determined by the HPLC method with a limit of detection of 0.05 μg/mL. The difloxacin concentration-time data were fitted to a two-compartmental open model after single intravenous administration to the healthy chickens. The main pharmacokinetic parameters were as follows: t_(1/2α)=0.69 h±0.43 h,t_(1/2β)=6.11 h±1.50 h,V_(1)=1.70 L/kg±0.33 L/kg,V_(d(area))=3.10 L/kg±0.67 L/kg,Cl_(B)=0.37 L/(kg·h)±0.10 L/(kg·h),AUC=29.16 μg/(mL·h)±8.04 μg/(mL·h).The drug concentration-time data were both fitted to a one-(compartmental)model with first order absorption after single intramuscular and (oral) administration to the chickens.The main pharmacokinetic parameters after single intramuscular administration were as follows:t_(1/2Ka)=0.17 h±0.12 h, t_(1/2Ke)=5.64 h±0.74 h, t_(max)=0.86 h±0.40 h, C_(max)=2.51 μg/mL±0.36 μg/mL, AUC= 22.62 μg/(mL·h)±3.28 μg/(mL·h), F=77.00%±11.80%. The main pharmacokinetic parameters after single oral administration were as follows: t_(1/2Ka)=1.46 h±1.00 h,t_(1/2Ke)=8.20 h±3.12 h,t_(max)=4.34 h±2.40 h, C_(max)=1.00 μg/mL±0.21 μg/mL, AUC=15.82 μg/(mL·h)±3.67 μg/(mL·h), F=54.20%±(12.60%). The results of the present study showed that difloxacin was absorbed rapidly (after) intramuscular administration, distributed extensively and eliminated slowly in chickens. The drug was not absorbed completely (after) both single intramuscular and oral administration in chickens.

关 键 词：二氟沙星 高效液相色谱 药物代谢动力学 生物利用度 鸡 

分 类 号：S859.6[农业科学—临床兽医学]