积雪草苷修饰脂质体在大鼠体内的药动学及组织分布研究  

Pharmacokinetics and tissue distribution study in rats of asiaticoside-loaded modified liposomes

作　　者：陈静怡[1] 任翔 王晓辉[1] 彭倩 陈莉[1] 张岭[1] 李京洋[1] 张津宁 张莉[1] 

机构地区：[1]武警后勤学院救援医学系,生药与药剂学教研室,天津300309 [2]武警四川省总队成都医院药械科,四川成都610041

出　　处：《中草药》2017年第21期4419-4424,共6页Chinese Traditional and Herbal Drugs

基　　金：武警后勤学院基础研究项目(WHJ201501)

摘　　要：目的将积雪草苷制成修饰脂质体,考察该制剂在体内的药动学过程及组织分布情况。方法 SD大鼠尾iv积雪草苷溶液及经过D-甘露糖或十八胺修饰和未经修饰的脂质体制剂,不同时间点采集大鼠血浆及组织,样品处理后采用HPLC法检测血浆与组织中的药物浓度,绘制药-时曲线,计算药动学参数,比较积雪草苷剂型间在体内药动学参数和组织分布的差异。结果积雪草苷、积雪草苷脂质体、D-甘露糖-积雪草苷脂质体、十八胺-积雪草苷脂质体4种制剂的药-时曲线均符合权重为1/C2的单室模型。积雪草苷溶液及各脂质体的消除半衰期(t1/2)分别为(14.52±0.56)、(101.35±12.47)、(149.82±20.00)、(159.58±16.46)min,药时曲线下面积(AUC)分别为(1 929.70±159.00)、(57 004.35±8 710.89)、(93 736.52±12 710.76)、(64 737.48±6 365.28)min·μg/m L。同时制成脂质体后,积雪草苷在各器官中的质量分数显著上升,在肺部的质量分数由(4.94±0.94)μg/g升至(39.12±12.04)μg/g。结论将积雪草苷制成修饰脂质体制剂后,缓释明显,并能增强靶向作用。Objective To prepare asiaticoside-loaded modified liposomes and to investigate the distribution and pharmacokinetics.Methods Different asiaticoside-loaded preparations（include solution,modified,and unmodified liposomes） were injected by tail vein in SD rats.HPLC method was used to detect the concentration of asiaticoside in the tissue and plasma samples.And the concentration-time profiles and pharmacokinetic parameters were then obtained and compared to get the variances.Results The concentration-time profiles of asiaticoside-loaded preparations guided along the single compartment model which the weight is 1/C2.The elimination half-life of asiaticoside solution and different asiaticoside liposomes were（14.52 ± 0.56）,（101.35 ± 12.47）,（149.82 ± 20.00）,and（159.58 ± 16.46） min,respectively.The AUC of asiaticoside solution and different asiaticoside liposomes were（1 929.70 ± 159.00）,（57 004.35 ± 8 710.89）,（93 736.52 ± 12 710.76）,and（64 737.48 ± 6 365.28） min·μg/m L,respectively.The mass fraction of asiaticoside in each organ increased,especially in the pulmonary which increased from（4.94 ± 0.94） μg/g to（39.12 ± 12.04） μg/g.Conclusion The sustained release and targeting effects in SD rats were obvious of the asiaticoside-loaded modified liposomes.

关 键 词：积雪草苷 修饰脂质体 药动学 组织分布 HPLC 缓释 靶向作用 

分 类 号：R94[医药卫生—药剂学]