复乳-溶剂挥发法制备氧化苦参碱脂质体.pdf

感都際。学、。,学、,报2010jn,5(1)
Journal of Chengdu Medical College
doi:10.3969/j. Issh.1674-2257.2010.01.005
论著
复乳溶剂挥发法制备氧化苦参碱脂质体
王浩,顾吉晋2,邓英杰
(1.中南大学药学院,湖南长沙410013;2.复且大学药学院,上海201203;3:沈阳药科大学药学院,辽宁沈阻10016)
【摘要】目的利用复乳-溶剂挥发法制备脂质体,并考察其对水溶性药物氧化苦参碱的包封率。方法按文
猷利用高速剪切机制备水相溶有氧化苦参碱的W/O乳剂,再将此乳剂滴入水相中二次乳化并继续快速搅拌、挥干
溶剂即得。并且采用超滤- HPLC法测定了脂质体的包封率。结果复乳法制备的脂质体包封率较低,绝大多数情
况小于10%,当水化液的离子强度较高时包封率在15%左右,样品低温储存2周后有药物晶体析出。结论采用
复乳法制得氧化苦参碱脂质体包封率较低,与文献报道的情形相符。
关键词】脂质体;复乳溶剂挥发法;氧化苦参碱;大豆磷脂;包封率
【中图分类号】R283【文献标识码
文章编号】1674-2257(2010)01-0021-
reparation of liposomal oxymatrine by multiple emulsification-solvent evaporation method
WANG Hao, Guji-jin, DENG Ying-jie
(1. School of Pharmacy, Central South University, Changsha 410013, China; 2. School of Pharmacy, Fudan Oni
versity, Shanghai 201203, hina: 3. School of Pharmacy, Shenyang Pharmaceutical niversity, Shenyang 110016
Abstract) Objective To prepare liposomal oxymatrine by multiple emulsificating solvent evaporating process.
Methods W/) emulsion that contained oxymatrine was prepared by employing high-speed homogenizer Lipos
soma
oxymatrine was obtained by adding the W/O emulsion into aqueous media dropwise and stirring the mixture vigor
ously until the organic solvent was evaporated thoroughly. 10 times higher of phospholipid concentration was used
compared to that reported in literature. Ultrafiltration-hplc method is adopted to determine the encapsulation effi-
ciency of oxymatrine liposome. Results The encapsulation efficiency was rather low by employing multiple emulsifi-
cating and solvent evaporating method that it was below 10% in most cases but some cases around 15%. Drug crys
tal could be found after the samples were stored 4 C for 2 weeks. Conclusion The result is accordant with the reports
in references that water soluble small molecular compound could be difficultly loaded in liposome with high encapsu
lation efficiency by the method adapted
K Key words] liposome; multiple emulsification-solvent evaporation; oxymatrine; soybean phospholipids; cncap
sulation efticiency
氧化苦参碱( oxymatrine,OMT)是从中药苦参炎的临床治疗?。但是该药全身分布,消除半衰期
和苦豆子中提取的有效成分,是近年来临床治疗肝短,而且该药在肝脏中的有效血药浓度持续时间
炎效果较好的药物之一日,国内已广泛用于乙型肝短。脂质体作为一种药物载体,可以被动靶向到
肝脾等网状内皮系统丰富的器官,从而较多地分布
收稿日期2009-10-09修回日期2009-10-22
于肝脏,提高药物在肝脏中的浓度,且能维持药物的
基金项目国家自然科学基金资動项目(30472100)
释放时间。OMT在水中的溶解度大于1(g
作者简介王浩(1980-),男,辽宁瓦房店人,博士研究生,主要从事
脂质体,乳剂等微粒分敝药物制剂的研究
m)/L,是一个亲水性很强的弱碱性小分子药物,其
通讯作者邓英太(195),女,黑龙江牡丹江人,研究员,主要从事结构式见图1
药物新剂型的研究。
文献介绍的复乳法制备的脂质体采用的磷脂浓
电话:15040370483,E-mail:wanghaowfd@sohu.com