黄芩素磷脂复合物制备及理化性质研究

Preparation of baicalein-phospholipid complex and its physic-chemical properties

目的:研究黄芩素磷脂复合物制备工艺,并考察其理化性质。方法:以黄芩素与磷脂的复合率为评价指标,通过单因素实验和正交设计实验考察反应溶剂、投料比例、反应温度、反应时间、反应初始浓度等对复合率的影响;研究黄芩素磷脂复合物的理化性质。结果:确定了黄芩素磷脂复合物的最佳制备工艺:反应溶剂为乙酸乙酯,黄芩素与磷脂的投料比为1∶4,反应温度为40℃,反应物质量浓度为5 mg/m l,搅拌回流2 h。X-射线衍射分析显示复合物呈现无定型特征;红外谱图显示黄芩素与磷脂之间无新的化学键形成。磷脂复合物明显改善了黄芩素在水及正辛醇中的溶解性能。结论:确定了制备黄芩素磷脂复合物的最佳工艺,并且其磷脂复合物明显改善了原药的理化性质。

Objective： To investigate the preparation and physic-chemical properties of baicalein-phospholipid.Methods： The effect of such factors as the solvent of reaction,the ratio of reactants,the reactive temperature,the reactive time and the concentration of reactants was studied by the single factor tests and orthogonal design.And the physic-chemical properties of baicalein phytosome were examined.Results： The optimal conditions were obtained as follows： the ratio of baicalein to phospholipid was 1∶4,the reactive time was 2 h,the reactive temperature was 40℃ and the concentration of reactants was 5 mg/ml.X-ray diffraction spectra indicated that drug encpasulated in the complex exhibits in an amorphous manner.IR spectrum didn′t show new chemical bonds formed in phospholipid complex.Moreover,there was a great improvement of the solubility of baicalein-phospholipid complex both in water and n-octanol.Conclusion： The best method to prepare baicalein-phospholipid complex was achieved,and its physic-chemical properties were significantly better from those of baicalein.