吡非尼酮脂质体的药代动力学和组织分布研究  

Study on the pharmacokinetics and tissue distribution of pirfenidone liposomes

作　　者：胡艳秋[1] 胡俊华[2] 于莲[1] 苏瑾[1] 杨春荣[1] 孙维彤[1] 平洋[1] 

机构地区：[1]佳木斯大学药学院,黑龙江佳木斯154007 [2]佳木斯市疾病预防控制中心,黑龙江佳木斯154007

出　　处：《黑龙江医药科学》2018年第1期28-31,22,共5页Heilongjiang Medicine and Pharmacy

基　　金：黑龙江省卫生计生委科研课题,编号:2016-323;佳木斯大学基础研究类(自然类)面上项目,编号:JMSUJCMS2016-068;黑龙江省大学生创新创业训练计划项目,编号:201510222006

摘　　要：目的:研究吡非尼酮脂质体静脉给药后在大鼠体内药代动力学规律及在小鼠体内组织分布特征。方法:采用HPLC法测定大鼠血浆和小鼠各组织中吡非尼酮的浓度。结果:吡非尼酮脂质体在大鼠体内吡非尼酮药时曲线AUC是对照组的1.82倍,体内滞留时间延长,药代动力学行为符合二室模型;吡非尼酮脂质体组在小鼠心、肝、脾、肺、肾中吡非尼酮浓度分别在0.5h、4h、0.5h、4h、0.2h达最高后开始降低,静脉注射吡非尼酮脂质体后4h内肺中吡非尼酮的平均浓度较其他组织中显著升高。结论:载药脂质体明显改变吡非尼酮在大鼠血浆中的药代动力学规律和在小鼠组织中的靶向定位特征,吡非尼酮脂质体具有明显的肺靶向性特征。Objective:To study the pharmacokinetics and tissue distribution of pirfenidone liposomes in rats.Methods:Reversed phase HPLC was used to determine pirfenidone concentration in rats' plasma and mice tissues.Results:The AUC of pirfenidone liposomes was 1.82 times as much as that of control group.Meanwhile the MRT prolonged in bodies.The concentration-time curves of pirfenidone liposomes and pirfenidone solution conformed to a two-compartment model.The concentrations of pirfenidone in the heart,liver,spleen,lung and kidney of rats' reached the highest levels at the 0.5 h,4 h,0.5 h,4 h,0.2 h,respectively; and then decreased thereafter.The concentration of pirfenidone in lung was the highest during 4 h after intravenous injection for pirfenidone liposomes compared with other tissues.Conclusions:Our present studies demonstrate that pirfenidone liposomes significantly alter pirfenidone pharmacokinetics in plasma and tissues distribution.Pirfenidone liposomes had obvious lung targeting.

关 键 词：吡非尼酮 脂质体 药代动力学 组织分布 

分 类 号：R927.2[医药卫生—药学]