Song Yunmei, Zhuang Jie, Guo Jianxin, Xiao Yanyu, Ping Qineng
Department of Pharmaceutics, China Pharmaceutical University, Nanjing, China.
Pharmazie. 2008 Jan;63(1):35-42.
Due to its poor solubility in water and oil, silybin is hardly absorbed orally and cannot be dissolved directly for parenteral preparations. In this study, a silybin-phospholipid complex was prepared by single-factor design and orthogonal experimental design. Lipophilicity was improved to a large extent, which was determined by solubility experiments and oil/water partition studies. Various methods were used to confirm the formation and explore the properties of the silybin-phospholipid complex, such as UV, IR, ATR, CNMR, XRD,DSC, SEM and TEM. The structure of the phytosome when the complex was dispersed in aqueous solution is suggested.
由于水飞蓟宾在水和油中的溶解度较差，其口服吸收困难，且不能直接溶解用于肠胃外制剂。在本研究中，通过单因素设计和正交实验设计制备了水飞蓟宾 - 磷脂复合物。通过溶解度实验和油/水分配研究确定，其亲脂性得到了很大程度的提高。采用了多种方法来确认水飞蓟宾 - 磷脂复合物的形成并探究其性质，如紫外光谱（UV）、红外光谱（IR）、衰减全反射光谱（ATR）、碳核磁共振谱（CNMR）、X射线衍射（XRD）、差示扫描量热法（DSC）、扫描电子显微镜（SEM）和透射电子显微镜（TEM）。文中还提出了该复合物分散于水溶液中时植物脂质体（phytosome）的结构。
