【摘要】 艾曲波帕二乙醇胺是一种非肽类、小分子的促血小板生成素受体激动剂,已被批准用于治疗肝炎、肝硬化和免疫性血小板减少性紫癜^[1-2]。通过元素分析（EA）、质谱（MS）、核磁共振波谱（NMR）、扫描电子显微分析（SEM）、傅里叶变换红外光谱（FTIR）、差示扫描量热法（DSC）和X射线粉末衍射法（PXRD）等手段对其结构进行表征。采用X射线粉末衍射原位升温附件与热重-差热联用仪（TG-DTA）对其晶型I进行热稳定性研究。EA, MS和NMR的检测结果与艾曲波帕二乙醇胺分子结构一致。扫描电镜表明其微观形貌呈粒子状和片层状且具有较干净的表面。DSC曲线显示在133.3℃开始出现脱溶峰。PXRD图谱显示在2θ=5.59°, 7.35°, 8.16°, 11.26°, 13.81°, 17.02°, 22.81°, 26.55°处有可用来定性鉴别的特征峰。艾曲波帕二乙醇胺晶型I在程序升温条件下于167.8～193.5℃和193.5～226.9℃出现两个阶段的失重并伴随着晶型结构的改变。以上的分析结果为我国仿制药的生产和鉴定提供了较为全面的参考。更多还原

【Abstract】 Eltrombopag diethanolamine, a nonpeptide and small molecular thrombopoietin receptor agonist, has been approved for the treatment of patients with cirrhosis associated with hepatitis and immune thrombocytopenic purpura. Here, we have successfully elucidated its structure by using elemental analyses(EA), mass spectra(MS), nuclear magnetic resonance spectra(NMR), scanning electron microscopy(SEM), fourier transform infrared spectroscopy(FTIR), differential scanning calorimetry(DSC) and powder X-ray diffraction(PXRD). The stability of the form-Ⅰ of eltrombopag diethanolamine was investigated by using thermogravimetric and differential thermal analyses(TG-DTA) and powder X-ray diffraction with in-situ high temperature accessories. The results of EA, MS, NMR are consistent with the molecular structure of eltrombopag diethanolamine. The SEM examination indicates that the morphological of it possess a particle shape, a lamellar shape and a relatively clean surface. The DSC thermogram of it showed a desolvation peak starting at 133.3 ℃. The PXRD patterns of it indicated peaks at 2θ=5.59°, 7.35°, 8.16°, 11.26°, 13.81°, 17.02°, 22.81°, 26.55°. It is seem that a few unique peaks and can be used for the identification. In the heating process, the result observed in the PXRD analysis and TG-DTA curve that two weight losses happened within the range 167.8～193.5 ℃ and 193.5～226.9 ℃ and the crystal structure was changed in the meantime. The above analysis providing a relatively comprehensive reference for the production and identification of generic drugs.更多还原