白藜芦醇磷脂复合物制备工艺的优化及理化性质的研究

Optimization of the preparation process and physical and chemical properties of resveratrol-phospholipid complex

目的优化白藜芦醇磷脂复合物的制备工艺,研究磷脂复合物的理化性质。方法以白藜芦醇与磷脂的复合率为评价标准,采用单因素影响试验考察反应时间、温度、浓度、溶剂、投料比等因素对复合率的影响。测定白藜芦醇磷脂复合物在水中的溶解度,用差示扫描量热法(DSC)研究其热力学性质,用X-射线衍射法研究白藜芦醇在磷脂复合物中的存在状态。结果确定了复合物的最佳反应条件,即以乙酸乙酯为反应溶剂,在40℃下反应1 h,白藜芦醇与磷脂的投料比为1∶3,白藜芦醇的反应浓度为10 mg·mL-1。复合物中白藜芦醇在水中的溶解度显著增大,DSC研究显示复合物是不同于白藜芦醇、磷脂及二者物理混合物的新物相,X-射线衍射研究显示复合物中白藜芦醇为无定形形态。结论白藜芦醇磷脂复合物的形成受反应溶剂、投料比的影响较大,白藜芦醇与磷脂形成复合物后,理化性质变化较大。

OBJECTIVE To optimize the preparation process of resveratrol - phospholipid complex and study its physical and chemical properties. METHODS With the complex yield of resveratrol and phospholipid as criteria, we adopted single factor test to investigate the influence of reaction time, reaction temperature, concentration, reaction solvent and the ratio of resveratrol and phospholipid. The water solubility of resveratrol in the complex was determined, the thermodynamic properties of the complex were investigated by differential scanning calorimetry （ DSC ） and the morphous of resveratrol in the complex was studied by X - ray diffraction. RESULTS The optimal preparation process was as follows ： the solvent was ethyl acetate, the reaction temperature was 40℃, the reaction time was 1 h,the ratio of resveratrol and phospholipid was 1 ： 3,and the concentration of resveratrol was 10 mg·mL^-1. The water solubility of resveratrol in the complex was improved significantly. The DSC demonstrated that resveratrol - phospholipid complex was different from resveratrol, phospholipid and their physical mixture. The X - ray diffraction analysis showed that resveratrol in the complex was in an amorphous form. CONCLUSION The reaction solvent and the ratio of resveratrol and phospholipid had prominent effect on the preparation of resveratrol - phospholipid complex. The physical and chemical properties of resveratrol were changed greatly after forming phospholipid complex.