绿原酸磷脂复合物制备工艺的研究  

Research on the preparation of Chlorogenic acid-phospholipid complex

作　　者：赵安权 王倩倩[1] 李佳[1] 贺英菊[1] 

机构地区：[1]四川大学华西药学院,四川成都610041

出　　处：《华西药学杂志》2015年第2期155-157,共3页West China Journal of Pharmaceutical Sciences

摘　　要：目的考察绿原酸与磷脂形成复合物的最佳工艺条件,并初步评价复合物的脂溶性。方法以绿原酸与磷脂的复合率为评价指标,采用单因素和正交设计试验进行系统性评价,考察药物浓度、药物与磷脂投料比、反应时间、反应温度等因素对磷脂复合物形成的影响,并通过测定表观油水分配系数初步考察复合物对绿原酸脂溶性的改善情况。结果确定了绿原酸磷脂复合物的最佳制备工艺,即20℃时以无水乙醇为溶剂,绿原酸与磷脂比例为1∶1,反应2 h。形成复合物后,绿原酸的表观油水分配系数提高了28.6倍。结论绿原酸磷脂复合物的形成受投药比、反应温度、绿原酸的浓度影响较大,所采用复合物的制备工艺稳定可行,且显著改善了绿原酸的脂溶性。OBJECTIVE To study the optimal conditions for the formation of chlorogenic acid （CA） complex with phospholipids and evaluate its lipid solubility. METHODS A reasonable criterion of recombination rate was established by testing the concentration of reactants, the ratio of CA to phospholipids, reaction time and temperature during the single - factor test and the orthographic design. The apparent oil - water partition coefficient was used to evaluate the improvement of lipid solubility. RESULTS The optimized preparation conditions for CA complex were obtained as follows ： Solvent was absolute ethanol. The ratio of CA to phospholipids was 1 to 1. The temperature was 20 ~C. The reaction time was 2 h. After forming complexes, the apparent oil - water partition coefficient of CA increased 28.6 times. CONCLUSION The formation of CA complex with phospholipids is affected by the ratio of CA to phospholipids, reaction temperature and the concentration of CA. The method of this article established is stable and feasible and the compound significantly improved the lipid solubility of CA.

关 键 词：绿原酸 磷脂复合物 油水分配系数 脂溶性 正交设计试验 工艺优化 

分 类 号：R94[医药卫生—药剂学]