[关键词]
[摘要]
目的 制备高水溶性的水飞蓟素-磺丁基-β-环糊精包合物。方法 相溶解度法筛选环糊精包合材料,确定包合类型;正交试验法优选水飞蓟素包合物的工艺条件;对其溶解度进行测定并使用显微镜法、红外光谱分析、X-射线衍射分析对包合物结构进行表征。结果 磺丁基-β-环糊精对水飞蓟素的增溶作用更强,确定其为包合材料,药物与环糊精按1:n的方式进行包合;正交试验优选出的最佳工艺为水飞蓟素与磺丁基-β-环糊精的物质的量比1:8,包合温度60℃,包合时间3 h;溶解度、显微镜、红外光谱分析和X-射线衍射分析的结果均显示已形成包合物,且药物以非晶型或无定型存在于包合物中。结论 成功制备水飞蓟素-磺丁基-β-环糊精包合物,其可显著提高水飞蓟素的溶解度,为其临床应用提供了实验基础。
[Key word]
[Abstract]
Objective The inclusion compound of silymarin-SBE-β-CD was prepared. Methods Phase solubility method was used to screen the inclusion materials of cyclodextrin and determine the type of inclusion. The technological conditions of silymarin inclusion complex were optimized by orthogonal design. The solubility of inclusion was determined and its structure was characterized by means of microscope, infrared spectrum analysis and X-ray diffraction analysis. Results Due to its higher solubilization effect on silymarin, SBE-β-CD was determined as inclusion material. The ratio of drug to cyclodextrin was coated in the mode of 1:n. The process optimized by orthogonal design was as follow:molar ratio of silymarin to SBE-β-CD of 1:8, inclusion temperature of 60℃, and inclusion time of 3 h. Microscope, infrared spectrum analysis and X-ray diffraction analysis showed that the inclusion compound was formed and the drug existed in the inclusion compound as amorphous. Conclusion The inclusion compound of silymarin-SBE-β-CD has been successfully prepared, which can significantly improve the solubility of the drug, and provide experimental basis for its clinical application.
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[基金项目]
福建省自然科学基金项目(2015J01491)