脂质体对大黄游离蒽醌类成分的包封及其质量控制  

Liposomal Encapsulation of Free Anthraquinones in Rhizoma et Radix Rhei and Its Quality Control

作　　者：索绪斌[1] 刘艳[1] 吴燕红[1] 李苑新[1] 

机构地区：[1]广东药学院中药开发研究所,广东广州510006

出　　处：《中药材》2010年第4期614-616,共3页Journal of Chinese Medicinal Materials

基　　金：广东药学院"重点青年教师培养对象"基金支持

摘　　要：目的：将大黄游离蒽醌类成分（大黄酸、大黄酚、大黄素、大黄素甲醚及芦荟大黄素）包入脂质体,并对其相关性质进行考察。方法：采取Sephadex G-50柱分离游离药物和脂质体,采取高效液相法测定脂质体中游离蒽醌类各个成分的含量,计算包封率;采取乙醇注入法,在分散介质中加入适量的钙离子（Ca2＋）制备大黄游离蒽醌类成分脂质体;考察Ca2＋对不同膜组成脂质体中大黄游离蒽醌包封的影响;采用动态激光散射仪和透射电镜观察脂质体的粒径分布和外部形态。结果：在Ca2＋存在条件下,制备的大黄游离蒽醌类成分脂质体对大黄酸、大黄酚、大黄素、大黄素甲醚及芦荟大黄素的包封率分别为：27.63%、85.16%、100.14%、99.77%及66.16%,总包封率为80.67%;Ca2＋能将游离大黄蒽醌类成分在脂质体中的包封率从13.98%-23.78%提高到81.42%-89.43%;脂质体为白色球状,粒径主要集中于340 nm。结论：制备的大黄游离蒽醌类成分脂质体包封率高,质量控制方法简单快捷,重现性良好。Objective：To encapsulate the free anthraquiones in Rhizoma et Radix Rhei（rhein,chrysophanol,physcione,emodin and aloeemodin） in liposomes and characterize the liposomes.Methods：The liposomes were separated from free drug with sephadex G-50 with HPLC determination of the free anthraquinones in liposomes,then its entrapment efficiency was calculated.Ethanol injection method was used to prepare the liposomes with the addition of a suitable amount Ca2＋ in the medium.The influence of Ca2＋ on the entrapment efficiency of free anthraquinones in Rhizoma et Radix Rhei in liposomes has been studied.Dynamic laser scatterometer and transmission electron microscopy were used to study the sizes and morphology of the liposomes.Results： The entrapment efficiency of rhein,chrysophanol,physcione,emodin and aloeemodin in liposomes were 27.63%、 85.16%、100.14%、99.77% and 66.16%,respectively.The total entrapment efficiency of free anthraquinones in Rhizoma et Radix Rhei was 80.67%.Ca2＋ could greatly promote the liposomal encapsulation of free anthraquinones in Rhizoma et Radix Rhei from 13.98%-23.78% to 81.42%-89.43%.The liposomes were white spheres and its average size was mainly concentrated on 340 nm.Conclusion： The entrapment efficiency of the liposomal encapsulation of free anthraquinones in Rhizoma et Radix Rhei is high.The quality control method is simple and rapid with good repeatability.

关 键 词：脂质体 大黄 游离蒽醌类成分 质量控制 

分 类 号：R943[医药卫生—药剂学]