硫酸铵梯度法制备重酒石酸长春瑞滨脂质体及其在大鼠体内的药动学参数  

Preparation and pharmacokinetics in rat of vinorelbine biartrate liposomes by ammonium sulfate gradient method

作　　者：郑召磊[1] 李亚平[1,2] 陈伶俐 

机构地区：[1]江苏大学药学院,江苏镇江212013 [2]中国科学院上海药物研究所药物制剂中心,上海201203

出　　处：《江苏大学学报（医学版）》2015年第3期256-259,共4页Journal of Jiangsu University：Medicine Edition

摘　　要：目的:采用硫酸铵梯度法制备重酒石酸长春瑞滨脂质体,并研究其理化性质及在大鼠体内的药动学行为。方法:采用硫酸铵梯度法制备重酒石酸长春瑞滨脂质体,并考察其形态、粒径、包封率、稳定性;采用HPLC测定长春瑞滨在大鼠体内的血药浓度。结果:重酒石酸长春瑞滨脂质体的平均粒径为(88.7±11.2)nm(n=3);包封率为(90.71±0.16)%(n=3);在10%胎牛血清中48 h释放率低于20%;SD大鼠尾静脉注射重酒石酸长春瑞滨脂质体后,药物半衰期为(5.38±0.29)h;AUC0→t=(98.11±0.12)mg·h-1·L-1。结论:重酒石酸长春瑞滨脂质体包封率较高,在血清中的稳定性良好,能够显著延长体内循环时间,提高其生物利用度。Objective: To prepare vinorelbine bitartrate( NVB) liposomes by ammonium sulfate gradient method,and to study the properties and pharmacokinetics of NVB liposomes. Methods: NVB liposomes were prepared by ammonium sulfate gradient method. The mean diameter of liposomes was determined by dynamic light scattering. Encapsulation efficiency was determined by sephadex column,pharmacokinetics was evaluated in SD rats. Results: Mean particle size and encapsulation efficiency of NVB liposomes were( 88. 7 ± 11. 2) nm( n = 3) and( 90. 71 ± 0. 16) %( n = 3). In addition,less than 20% of NVB liposomes was released in 48 hours. The main pharmacokinetic parameters of NVB liposomes were as follows: t1 /2=( 5. 38 ± 0. 29) h and AUC0→t=( 98. 11 ± 0. 12) mg ·h- 1·L- 1. Conclusion: NVB liposomes exhibited high encapsulation efficiency. The pharmacokinetics of NVB liposomes showed prolonged elimination halflife and increased bioavailability.

关 键 词：重酒石酸长春瑞滨 脂质体 硫酸铵梯度法 药动学 

分 类 号：R943[医药卫生—药剂学]