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达氟沙星脂质体在蛋雏鸡体内的组织动力学及靶向性研究 被引量:1

The tissue pharmacokinetics and targeting of danofloxacin mesylate liposomes in egg chickens
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摘要 将260只28日龄试验鸡(体质量215-230 g)随机分成5组:健康对照组20只,甲磺酸达氟沙星溶液静注给药组和内服给药组、甲磺酸达氟沙星脂质体静注给药组和内服给药组,每组60只。以5 mg/kg体质量剂量分别采用静脉注射和内服2种给药途径给予健康蛋雏鸡甲磺酸达氟沙星溶液和脂质体混悬液,于给药后0.167、0.333、0.5、0.75、1、1.5、2、4、6、9、12、24 h各剖杀5只鸡,取血液、肝脏、肾脏、肺脏和肌肉样品。采用反相HPLC色谱内标法测定各组织中达氟沙星浓度。应用MCPKP分析软件处理血浆药物浓度-时间数据,比较2种剂型的组织药动学参数。结果显示,与溶液组相比,甲磺酸达氟沙星脂质体组肝脏、肺脏中的药物分布明显提高,肾脏中的分布降低;通过相对摄取率、靶向效率和峰浓度比3个靶向指标的对比,脂质体组明显提高了肺部靶向性,且在肺部有一定的缓释作用。 The objective of this study is to compare the disposition of danofloxacin mesylate liposomes with its solution in tissues of healthy egg chickens following intravenous and oral administration,respectively.260 chickens(with 215-230 g of body weight)were divided randomly into five groups,i.e.control group,intravenous and oral administration groups with danofloxacin mesylate solution and its liposomes,respectively.Danofloxacin mesylate solution and liposomes were separately administered to the chickens intravenously and orally at the dose of 5 mg/kg,five chickenns were killed at 0.167,0.333,0.5,0.75,1,1.5,2,4,6,9,12,24 h after administration,meanwhile,tissues including liver,kidney,lunger and muscle were collected.The concentrations of danofloxacin in tissue samples were determined by reversed-phase HPLC method,and the pharmacokinetic parameters of the two dosage forms in the tissues were calculated by MCPKP analysis software.Compared the liposomes to the solution,the drug distribution in the liver and lung was obviously elevated,but the kidney was properly the reverse.Contrasting to the three targeting indexes(relative targeting efficiency,targeting efficiency,peak concentration ratio),liposomes groups obviously elevated the lung targeting and the release of drug was prolonged in the lung.
出处 《中国兽医学报》 CAS CSCD 北大核心 2010年第4期480-484,共5页 Chinese Journal of Veterinary Science
基金 哈尔滨市青年科技创新人才资金项目(RC2007QH002031)
关键词 甲磺酸达氟沙星 脂质体 蛋雏鸡 组织药代动力学 danofloxacin mesylate liposomes egg chickens tissue pharmacokinetics
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