溶解
分子
化学
结晶学
拉曼光谱
甲醇
多态性(计算机科学)
热稳定性
生物制药
晶体结构
立体化学
有机化学
基因
光学
物理
基因型
生物
生物化学
遗传学
作者
Iryna Andrusenko,Victoria Hamilton,Arianna Lanza,Charlie L. Hall,Enrico Mugnaioli,Jason Potticary,Asma Buanz,Simon Gaisford,Anna Maria Piras,Ylenia Zambito,Simon R. Hall,Mauro Gemmi
标识
DOI:10.1016/j.ijpharm.2021.121067
摘要
The structure solution of the δ-polymorph of indomethacin was obtained using three-dimensional electron diffraction. This form shows a significantly enhanced dissolution rate compared with the more common and better studied α- and γ-polymorphs, indicating better biopharmaceutical properties for medicinal applications. The structure was solved in non-centrosymmetric space group P21 and comprises two molecules in the asymmetric unit. Packing and molecule conformation closely resemble indomethacin methyl ester and indomethacin methanol solvate. Knowledge of the structure allowed the rational interpretation of spectroscopic IR and Raman data for δ-polymorph and a tentative interpretation for still unsolved indomethacin polymorphs. Finally, we observed a solid–solid transition from δ-polymorph to α-polymorph that can be driven by similarities in molecular conformation.
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