β-榄香烯脂质体的制备及其在大鼠体内的组织分布  

Preparation ofβ-elemene liposomes and their tissue distribution in rats

作　　者：宋笑丹[1] 王学军[2] 杜霞[1] 魏华[1] 董迪[1] 吴琳华[1] 

机构地区：[1]哈尔滨医科大学附属第二医院药学部 [2]黑龙江省中医研究院,黑龙江哈尔滨150036

出　　处：《中国新药与临床杂志》2007年第10期733-736,共4页Chinese Journal of New Drugs and Clinical Remedies

摘　　要：目的:研制β-榄香烯脂质体并考察其在大鼠体内的组织分布。方法:采用薄膜分散法制备β-榄香烯脂质体,考察其形态、粒径、Zeta电位、药物含量及包封率。并以榄香烯注射液为对照,大鼠尾静脉注射给药,考察β-榄香烯脂质体在血浆及心、肝、脾、肺、肾的分布特征。结果:制备的β-榄香烯脂质体均匀圆整,粒径为(158±s 37)nm,Zeta电位为(-67±4)mV,药物含量为(5.76±0.21)g·L^(-1),包封率为(45.08±0.15)%(n=3)。大鼠尾静脉注射β-榄香烯脂质体和榄香烯注射液后,2种制剂在心、肝、脾、肾中的AUC_(0-t)均有显著差异,其中β-榄香烯脂质体在肝、脾、肾组织中分布相对较多,在心脏中分布较少。结论:薄膜分散法制备β-榄香烯脂质体方法可行,β-榄香烯脂质体在大鼠体内的分布特性有不同程度的改变,可提高疗效,降低心脏毒性。AIM： To study the preparation of β-elemene liposomes and their tissue distribution in rats.METHODS： β-elemene liposomes were prepared by film dispersion method. Its physical properties, particle size, Zeta potential, content and its entrapment efficiency were detected. The tissue distribution （plasma, heart, liver, spleen, lung and kidney） of β-elemene liposomes and elemene injection （control） was measured after intravenous injection in rats. RESULTS： β-elemene liposomes were spherical vesicle with particle size of （158 ± s 37） nm, Zeta potential of （-67 ± 4） mV, content of （5.76 ± 0.21） g.L^-1, entrapment efficiency of （45.08 ± 0.15） % in = 3） . There was significant difference in the AUC0-4, of heart, liver, spleen and kidney in rats between β-elemene liposomes and elemene injection. Compared with elemene injection, β-elemene liposomes distributed mainly in liver, spleen and kidney while less in heart after intravenous injection in rats. CONCLUSION： The preparation of β-elemene liposomes by film dispersion method is feasible. There is a certain degree change of β-elemene liposomes distributed in rats, which can improve curative effects and reduce heart toxicity.

关 键 词：脂质体 大鼠 组织分布 β-揽香烯 

分 类 号：R944.9[医药卫生—药剂学] R945[医药卫生—药学]