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泊洛沙姆188修饰的蜂毒素脂质体在大鼠体内的药动学
引用本文:柯学,王长江,胡一桥.泊洛沙姆188修饰的蜂毒素脂质体在大鼠体内的药动学[J].中国医院药学杂志,2010(3).
作者姓名:柯学  王长江  胡一桥
作者单位:南京大学生命科学学院;中国药科大学药剂教研室;
摘    要:目的:考察泊洛沙姆188(poloxamer188)修饰的蜂毒素脂质体在大鼠体内的药动学。方法:大鼠尾静脉分别注射蜂毒素溶液(MLT-I)、2%及5%Poloxamer188修饰的蜂毒素脂质体(MLT-LIPO-2%和MLT-LIPO-5%),采用酶联免疫吸附(ELISA)方法测定大鼠体内的蜂毒素。结果:采用Kinetica4.4统计软件,经统计矩拟合后,与MLT-I相比,MLT-LIPO-2%和MLT-LIPO-5%在大鼠体内的药动学行为发生显著变化,清除率(CL)分别为溶液组的48.3%及33.2%;血药浓度-时间曲线下面积(AUC)分别为溶液组的2.01倍及2.82倍;平均滞留时间(MRT)分别为溶液组的1.80倍及2.18倍。结论:经poloxamer188修饰后的脂质体显著延长了药物在大鼠体内的驻留时间,提高了药物的生物利用度,且与膜修饰剂的用量有一定的正相关性。

关 键 词:蜂毒素  脂质体  poloxamer188  药动学  酶联免疫吸附  

Pharmacokinetics of melittin liposomes modified with poloxamer188 in rats
KE Xue,WANG Chang-jiang,HU Yi-qiao.Pharmacokinetics of melittin liposomes modified with poloxamer188 in rats[J].Chinese Journal of Hospital Pharmacy,2010(3).
Authors:KE Xue    WANG Chang-jiang  HU Yi-qiao
Institution:KE Xue1,2,WANG Chang-jiang2,HU Yi-qiao1(1.School of Life Science,Nanjing University,Jiangsu Nanjing 210032,2.Department of Pharmaceutics,China Pharmaceutical University,Jiangsu Nanjing 210009,China)
Abstract:OBJECTIVE To evaluate the pharmacokinetics of melittin(MLT) liposomes(LIPO) modified with poloxamer188 in rats.METHODS Following administration of MLT solution(MLT-I),MLT liposome with 2% and 5% poloxamer188(MLT-LIPO-2% and MLT-LIPO-5%) to rats via tail veins,respectively,the concentration of MLT in vivo was determined by ELISA.RESULTS The PK studies showed that behavior of MLT-LIPO-2% and MLT-LIPO-5% in vivo changed significantly compared to MLT-I.The gained data fitted the two compartment model,the CL was...
Keywords:melittin  liposomes  poloxamer188  pharmacokinetics in vivo  ELISA  
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