目的：制备洋金花总黄酮磷脂复合物并考察其理化性质。方法：以洋金花总黄酮与磷脂的复合率为指标，考察复合溶剂、复合时间、复合温度、初始浓度和投料比例对复合率的影响，优化制备工艺；对所得磷脂复合物的理化性质，包括油/水分配系数、粒径、在水溶液中的状态以及形成的单分子膜的特性等进行了研究。结果：洋金花总黄酮磷脂复合物的最佳制备工艺为：洋金花总黄酮与磷脂按1颐1.8 的质量比投料，于30益甲醇中复合1h，总黄酮的浓度为10g·L-1，复合率95%以上。差热扫描显示复合物的相变温度改变；透射电镜显示复合物在水中为圆整均匀的囊泡，平均粒径48.51依9.13nm；在pH 为1.0、6.5、9.0 的条件下，复合物的油/水分配系数分别为总黄酮的4.22、3.06、3.75 倍；和磷脂复合物的结构相对应，Langmuir-blodgett（LB）膜仔-A 等温曲线显示复合物具有比磷脂强的刚性。结论：通过在甲醇中复合，成功制备了洋金花总黄酮的磷脂复合物；复合物较黄酮的脂溶性增加，较磷脂亲水性增加，在水相中组装成纳米胶束。膜天平是研究磷脂复合物的又一有力工具。

This work aimed to prepare phytosomes of total flavonoids of Flos Daturae and investigate their properties. The effects of the complex solvent, time, temperature, the concentration of total flavonoids and the formulation on phytosomes preparation were investigated in terms of the yield. The physical properties of the resultant phytosomes were examined, including the diameter, size distribution, shape in the aqueous phase, and oil/water apparent partition coefficient. The optimized conditions for phytosomes preparation were as follows total flavonoids of Flos Daturae and phospholipids (1∶1.8, weight ratio) were complexed in methanol at 30℃ for 1 h with the final concentration of total flavonoids being 10 g·L-1. The yield turned out to be over 95%. The phytosomes formed round and uniform vesicles in water with the average diameter of 48.51±9.13 nm. The oil/water apparent partition coefficient of the phytosomes was respectively 4.22, 2.83 and 3.75 times higher than that of the original total flavonoids in pH 1.0, 6.5 and 9.0 water. Different from the elastic Langmuir-blodgett (LB) monolayer film formed by soy phospholipid, the phytosomes tended to form much more rigid LB membranes. The results showed that the phytosomes of total flavonoids of Flos Daturae could be prepared in methanol, with greater lipophilicity than flavonoids and increased hydrophlicity than soy phospholipid. The resultant phytosomes may form nanosized micelles in the aqueous phase.

卫生部国家受新药创制重大专项（2009ZX09301-003）：医科院综合性新药研究开发技术大平台———制剂单元平台，主项目负责人：詹启敏，子项目负责人：王向涛。