恩诺沙星在健康及实验性感染乳房炎奶山羊间的比较药动学  

Study of Comparative Pharmacokinetics of Enrofloxacin in Healthy and Mastitis Lactating Goats Experimentally Infected with Staphylococcus aureus

作　　者：刘涤洁[1] 冯淇辉[1] 陈杖榴[1] 

机构地区：[1]华南农业大学兽医药理研究室,广州510642

出　　处：《中国农业科学》2003年第9期1100-1104,共5页Scientia Agricultura Sinica

摘　　要：每毫升 10 6菌落形成单位的金黄色葡萄球菌悬液 1ml单侧乳房内接种 ,人工诱发奶山羊乳房炎。 15只泌乳期健康奶山羊 ,按给药途径随机分为 3组 ,采用交叉试验设计 ,分别进行静注、肌注和乳房灌注恩诺沙星 (2 .5mg·kg-1)对健康和人工感染乳房炎的奶山羊进行比较药动学研究。采用HPLC法测定血中恩诺沙星及其代谢产物环丙沙星的浓度 ,用统计矩原理处理药物浓度 时间数据。结果表明 ,实验性乳房炎可以使静注给药后恩诺沙星在奶山羊的消除缓慢 (P <0 .0 5 ) ,消除半衰期 (t1/ 2 β)由 1.32± 0 .2 6h增至 1.77± 0 .12h ;使肌注给药恩诺沙星的吸收、生物转化和代谢均发生显著变化 (P <0 .0 1) ,药 时曲线下面积 (AUC)由 3.0 4mg·h-1·L-1增至 4 .36mg·h-1·L-1,代谢率 (f)由 4 4 .0 6 %降至 2 4 .0 2 % ,环丙沙星的AUC由 1.2 9降至 1.0 1mg·h-1·L-1;使乳房灌注给药恩诺沙星的平均滞留时间 (MRT)由 1.86h增至 2 .2 9h(P <0 .0 5 ) ,f由 4 5 .73%降至 30 .0 6 % (P <0 .0 1)。One ml 106 CFU (colony formation units) per ml suspension of Staphylococcus aureus was inoculated to one udder of the lactating goats to induce mastitis. Fifteen lactating goats were randomly divided into three groups according to different routes of administration. With cross-over design, comparative pharmacokinetic study was conducted in healthy and mastitis goats followed by single intravenous, intramuscular and intramammary administration of enrofloxacin at the dose of 2.5 mg·kg -1 body weight. Concentrations of enrofloxacin and its metabolite ciprofloxacin in plasma were determined by HPLC and the concentration-time data were analyzed by statistical moment principle. The results showed that, the elimination of enrofloxacin was slower in mastitis goats than in healthy goats when given enrofloxacin intravenously (P<0.05), the elimination half time (t 1/2β) increased from 1.32±0.26 h to 1.77±0.12 h; the absorption, biotransformation and the metabolism of enrofloxacin changed extremely significantly after infection when dosed intramuscularly (P<0.01), area under concentration-time curve (AUC) increased from 3.04 mg·h -1·L -1 to 4.36 mg·h -1·L -1; metabolic fraction (f) decreased from 44.06% to 24.02%, AUC of ciprofloxacin decreased from 1.29 mg·h -1·L -1 to 1.01 mg·h -1·L -1; the mean residual time (MRT) of enrofloxacin increased from 1.86 h to 2.29 h (P< 0.05), and the metabolic fraction of enrofloxacin decreased from 45.73% to 30.06% (P<0.01) after infection when given intramammarily.

关 键 词：恩诺沙星 实验性感染 乳房炎 奶山羊 接种 金黄色葡萄球菌悬液 人工诱发 给药途径 

分 类 号：S859.79[农业科学—临床兽医学]