银杏内酯B多晶型的制备、表征与性质研究

Polymorphism preparation and characterization of ginkgolide B

目的研究银杏内酯B多晶型的制备、表征与性质。方法对银杏内酯B进行多晶型筛查,并制备了6种不同的晶型(A^F型),分别采用单晶X射线衍射法(SXRD)、差示扫描量热法(DSC)、热重分析法(TG)对样品进行表征分析,并进一步研究银杏内酯B不同晶型对谷氨酸导致的PC12细胞损伤保护作用的优劣。结果各晶型PXRD、DSC、TG图谱均存在明显的差异,可用上述方法进行鉴别。无溶剂晶型F型为稳定晶型,通过细胞实验证明了晶型F对PC12细胞的保护作用更强。结论银杏内酯B晶型F为优势用药晶型。

Objective To explore the preparation,characterization and properties of ginkgolide B-related polymorphs.Method By the methods of single crystal X-ray diffraction(SXRD),powder X-ray diffraction(PXRD),differential scanning calorimetry(DSC)as well as thermogravimetric analysis(TG),six kinds of crystal structure of ginkgolide B(form A-F)were prepared.To confirm the dominant crystal form of ginkgoide B,the protective effects of different crystal structures of ginkgolide B were further detected on glutamate-treated PC12 cells.Result The results indicated that there were significant differences among the crystal structures of ginkgolide B by using PXRD,DSC and TG.Furthermore,we observed that the form F was the most stable crystal form and showed better neural protective effects compared with the original form.Conclusion The form F is the dominant crystal form of ginkgoide B.