丹参酮ⅡA磷脂复合物的制备及鉴别

Preparation and Identification of Tanshinone Ⅱ A Phospholipid Complex

目的制备丹参酮ⅡA磷脂复合物并对复合物的形成进行验证。方法以丹参酮ⅡA与磷脂的复合率为评价标准,通过正交设计考察反应浓度、投料比例和反应温度对复合率的影响,并采用差式扫描量热分析(DSC)、X-射线衍射分析(X-ray)、红外分析法(IR)对所制得的复合物进行验证。结果确定了丹参酮ⅡA磷脂复合物的最佳制备工艺为:以乙酸乙酯为反应溶剂,反应温度为60℃,反应时间为2h,丹参酮ⅡA浓度为0.5mg/mL,丹参酮ⅡA与磷脂的投料比(摩尔比)为1∶1.5。差热扫描显示复合物的相变温度改变;X-射线衍射分析显示复合物呈现无定型特征;红外图谱发生变化。结论确定了制备丹参酮ⅡA磷脂复合物的最佳工艺,并且其磷脂复合物明显的改变了原药的理化性质。

ABSTRACT：OBJECTIVE To prepare tanshinone ⅡA-phospholipid complex and test the formation of phopholipid complex. METHODS The effects of the concentration of reactants,the ratio of reactants and the reactive temperature on preparation were investigated using orthogonal design,and the formation of complex was analyzed by using the differential scanning （DSC）,X-ray diffraction analysis（X-ray）and infrared spectrum（IR）.RESULTS The optimized conditions were obtained as follows：the solvent was ethyl acetate,the concentration of reactants was 0.5 mg/mL,the ratio of tanshinone ⅡA to phospho-lipid（molar）was 1∶1.5,the reactive temperature was 60 ℃ and the reactive was 2 h.The change of the transformation tem-perature was showed in DSC spectra.X-ray diffraction spectra indicated that the complex exhibits an amorphous characteristic. Infrared spectrum changed.CONCLUSION The best method to prepare tanshinone Ⅱ A-phospholipid complex is achieved, and its physic-chemical properties are significantly different from those of tanshinone ⅡA.