中国畜牧兽医

• 生理生化 • 上一篇    下一篇

连翘酯苷脂质体在雏鸡体内的药动学研究

赵海焦1,徐卫康1,贾志华1,孙玉成2,侯晓林1,陆彦1,吴国娟1,张中文1   

  1. 1.北京农学院动物科学技术学院,北京 102206;2.黑龙江省宝泉岭农场机关,黑龙江鹤岗 154211
  • 收稿日期:2013-08-26 修回日期:2014-02-19 出版日期:2014-02-20 发布日期:2014-03-27
  • 通讯作者: 吴国娟(1955—),女,吉林人,博士,教授,主要从事中药药理与毒理研究。E-mail:wgj9288@sina.com;Tel:010-80796702 张中文,男,教授。E-mail:zwzhang9288@sina.com;Tel:010-80799146

Study on Pharmacokinetics of Forsythiaside Liposome in Chicks

ZHAO Hai-jiao1, XU Wei-kang1, JIA Zhi-hua1, SUN Yu-cheng2, HOU Xiao-lin1, LU Yan1, WU Guo-juan1, ZHANG Zhong-wen1   

  1. 1. Department of Animal Science and Technology, Beijing University of Agriculture, Beijing 102206, China;2. Heilongjiang Baoquanling Farm Authority, Hegang 154211, China
  • Received:2013-08-26 Revised:2014-02-19 Online:2014-02-20 Published:2014-03-27

摘要: 试验旨在考察连翘酯苷脂质体静脉给药后在雏鸡体内的药物动力学和组织分布。将连翘酯苷脂质体与连翘酯苷水溶液分别以20 mg/kg体重剂量给雏鸡静脉注射,于不同时间点取心脏、肝脏、脾脏、肺脏、肾脏组织和血液。HPLC法测定各时间点血液及各组织中连翘酯苷浓度。连翘酯苷脂质体和连翘酯苷溶液的血药浓度—时间曲线均符合二室开放模型,药动学参数消除半衰期(t1/2β)分别为(1.79±0.050) 和(0.11±0.006)h,药时曲线下面积(AUC)分别为(39.95±2.32) 和(4.26±0.39) (μg·h)/mL,体清除率(CLs)分别为(0.56±0.04)和(4.73±0.41) mg/(h·kg),连翘酯苷脂质体给药后在肝脏、脾脏、肺脏中的分布较连翘酯苷水溶液有明显提高。连翘酯苷脂质体明显改变了连翘酯苷的药动学行为,与游离药物相比,其有效延长了药物作用时间,在网状内皮系统丰富的组织有靶向性聚集作用。

关键词: 翘酯苷; 脂质体; 药动学; 高效液相色谱法

Abstract: The study was aimed to evaluate the pharmacokinetics and tissue distribution of forsythiaside liposome in chicks by intravenous administration. The pharmacokinetics of chicks with intravenous administration of forsythiaside liposome and forsythiaside solution 20 mg/kg was studied and the concentrations of forsythiaside in heart, liver, spleen, lung, kidney and plasma were determined by HPLC. The plasma concentration-time curves of forsythiaside liposome and forsythiaside solution were both fit to the two-compartment model and the pharmacokinetic parameters were (1.79±0.050) and (0.11±0.006) h for t1/2β, (39.95±2.32) and (4.26±0.39) (μg·h)/mL for AUC, (0.56±0.04) and (4.73±0.41) mg/(h·kg) for CLs. Compared with the liposome to the solution, the drug distribution in liver, spleen and lung were obviously elevated. Compared with forsythiaside solution, the forsythiaside liposome could significantly prolong the resident time of forsythiaside in the blood circulating system and could be concentrated at the target tissue rich in the reticuloendothelial system.