目的 制備阿普斯特E晶型的單晶，并對(duì)其進(jìn)行結(jié)構(gòu)表征和穩(wěn)定性研究。方法 通過(guò)溶劑揮法制備出阿普斯特E晶型的單晶，采用差式掃描量熱儀（DSC）、粉末X射線（PXRD）及單晶X射線儀（SXRD）對(duì)其進(jìn)行表征，利用均漿實(shí)驗(yàn)對(duì)其晶型穩(wěn)定性進(jìn)行考察。結(jié)果 乙腈溶劑揮發(fā)法可制備得到阿普斯特E晶型的單晶，其DSC和PXRD圖譜與文獻(xiàn)報(bào)道一致。SXRD結(jié)果表明阿普斯特E晶型的單位化學(xué)計(jì)量式為C₂₂H₂₄N₂O₇S，相對(duì)分子質(zhì)量為460.49，晶體密度為1.262 g/cm³，該晶胞屬于正方晶系，空間群為P4₁2₁2。均漿穩(wěn)定性實(shí)驗(yàn)結(jié)果表明，不同極性溶劑中得到的晶體DSC圖譜發(fā)生變化。結(jié)論 實(shí)驗(yàn)確證了阿普斯特E晶型的立體構(gòu)型，不同溶劑中晶型發(fā)生變化。

Objective To prepare single crystals of apremilast form E, and to investigate the corresponding structure and thermodynamic stability. Methods Evaporation method was used to grow single crystals of apremilast form E, which were then characterized using differential scanning calorimetry (DSC), powder X-ray diffraction (PXRD), and single X-ray diffraction (SXRD). Results Single crystals of apremilast form E could be obtained through acetonitrile evaporation. DSC graph and PXRD spectrum was in good agreement with data reported in literatures. SXRD results showed that the unit stoichiometric of apremilast form E was C₂₂H₂₄N₂O₇S, and the relative molecular mass was 460.49, and crystal density was 1.262 g/cm³. The unit cell belonged to a tetragonal system, and the space group was P4₁2₁2. The slurry experiment results showed that DSC graphs of apremilast samples suspended in different polar solvents were different. Conclusion Crystal structure of apremilast form E is characterized, and the crystallization changes in different solvents.

國(guó)家自然科學(xué)基金資助項(xiàng)目（21406071）；中央高?；究蒲袠I(yè)務(wù)費(fèi)資助項(xiàng)目（22A201514006）