复乳溶剂挥发法制备氧化苦参碱脂质体.docVIP

复乳溶剂挥发法制备氧化苦参碱脂质体 目录 TOC \o 1-9 \h \z \u 目录 1 正文 1 文1：复乳溶剂挥发法制备氧化苦参碱脂质体 1 1 仪器与试药 3 2 方法与结果 3 3 讨论 5 文2：溶剂非溶剂法制备四逆汤微囊研究 7 1? 材料与方法 7 四逆汤微囊的制备 8 2? 结果与讨论 10 参考文摘引言： 11 原创性声明（模板） 12 文章致谢（模板） 13 正文 复乳溶剂挥发法制备氧化苦参碱脂质体 文1：复乳溶剂挥发法制备氧化苦参碱脂质体 【Abstract】 Objective To prepare liposomal oxymatrine by multiple emulsificatingsolvent evaporating W/O emulsion that contained oxymatrine was prepared by employing highspeed oxymatrine was obtained by adding the W/O emulsion into aqueous media dropwise and stirring the mixture vigorously until the organic solvent was evaporated times higher of phospholipid concentration was used compared to that reported in HPLC method is adopted to determine the encapsulation efficiency of oxymatrine The encapsulation efficiency was rather low by employing multiple emulsificating and solvent evaporating method that it was below 10% in most cases but some cases around 15%.Drug crystal could be found after the samples were stored 4 ℃ for 2 The result is accordant with the reports in references that watersoluble small molecular compound could be difficultly loaded in liposome with high encapsulation efficiency by the method adapted。 【Key words】 liposome;multiple emulsificationsolvent evaporation;oxymatrine;soybean phospholipids;encapsulation efficiency 氧化苦参碱(oxymatrine，OMT)是从中药苦参和苦豆子中提取的有效成分，是近年来临床治疗肝炎效果较好的药物之一[1]，国内已广泛用于乙型肝炎的临床治疗[2]。但是该药全身分布，消除半衰期短，而且该药在肝脏中的有效血药浓度持续时间短[34]。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，从而较多地分布于肝脏，提高药物在肝脏中的浓度，且能维持药物的释放时间[5]。OMT在水中的溶解度大于1(g·m)/L，是一个亲水性很强的弱碱性小分子药物，其结构式见图1。 文献介绍的复乳法制备的脂质体采用的磷脂浓度比较低，且药脂比亦较低[6]，本研究试用较高药脂比(mol:mol，1:1)和较大原料药浓度(约 mg/ml， mg/ml)来制备氧化苦参碱脂质体，采用粒度测定仪分析有机溶剂挥发后其粒径大小的分布情况，并采用超声法对其粒径进行了进一步的减小。并且通过微孔滤膜超滤HPLC法对其包封率进行了测定。 1 仪器与试药 高效液相色谱仪(日本Shimadzu公司);扫描电子显微镜(日本Hitachi公司);微粒粒度测定仪(英国Beckman公司);高速均质机(广州，UITRA TURRAX，T18Basic);DZDW2型电子恒温不锈钢水浴锅(上海路达实验仪器有限公司);Amicon 8010 搅拌超滤器(美国Milipore公司);PHS2C型精密酸度计(上海雷磁仪器厂);Adventure AR1140电子天平(美国Ohaus 公司);DF10B集热式恒温磁力搅拌器(浙江省乐清县乐成仪