9-硝基喜树碱磷脂/胆盐混合胶束的制备及其性质研究
Preparation and characterization of 9-nitrocamptothecin incorporated in egg phasphatidylcboline-sodium deoxycholate mixed micelles
作者：黄蕊;龚涛;张志荣;
Author：
收稿日期： 年卷（期）页码：2013,28(02):-117-120
期刊名称：华西药学杂志
Journal Name：WEST CHINA JOURNAL OF PHARMACEUTICAL SCIENCES
关键字：9-硝基喜树碱;胆盐;磷脂;混合胶束;溶解度
Key words：
基金项目：
中文摘要
目的制备9-硝基喜树碱磷脂/胆盐混合胶束(9-NC MMs),进行单因素处方筛选及初步性质研究。方法采用共沉淀法制备9-NC MMs;通过单因素考察,研究蛋黄卵磷脂(EPC)/脱氧胆酸钠(SDC)比例、辅料总浓度、水化介质离子强度对9-NC在混合胶束中溶解度的影响及抗氧剂叔丁基羟基茴香醚(BHA)用量筛选;拟定处方,考察9-NC MMs的粒径、形态、稀释稳定性和溶血性。结果 9-NC MMs优化处方为:EPC/(EPC+SDC)为0.4;辅料总浓度为2.5%;水化介质为0.9%NaCl溶液,BHA用量为0.005%。在此处方下,9-NC在水中的溶解度可提高到1 mg.mL-1;9-NC MMs具有良好的稀释稳定性,载药胶束平均粒径为7.04 nm,透射电镜说明胶束形态为均匀类圆形,无溶血作用。结论 9-NC EPC/SDC MMs的制备工艺简便,能有效提高9-NC溶解度,粒径分布理想、稳定性好、安全性好,便于临床静脉注射的应用。
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