School of Chemical Engineering and Technology, Tianjin University, Tianjin, China; The Co-Innovation Center of Chemistry and Chemical Engineering of Tianjin, Tianjin University, Tianjin, China.
School of Chemical Engineering and Technology, Tianjin University, Tianjin, China.
Eur J Pharm Sci. 2017 Dec 15;110:19-25. doi: 10.1016/j.ejps.2017.06.001. Epub 2017 Jun 3.
Crystal engineering strategy was applied to develop new solid forms of lamotrigine. Two novel cocrystals of lamotrigine forming with 4,4'-bipyridine (2:1) and 2,2'-bipyridine cocrystal (1:1.5) were successfully obtained by neat grinding and liquid assisted grinding. The novel cocrystals were fully characterized and confirmed by X-ray diffraction, thermal and spectroscopic analysis. DXRxi Raman microscope was also used to identify the cocrystals. The factors such as solvent and the structure of coformers which influenced the cocrystal formation were discussed. Furthermore, the novel cocrystals were both obtained by slurry crystallization. Process analytical technologies including focused beam reflectance measurement and attenuated total reflectance Fourier Transform Infrared were applied to investigate the cocrystallization process and the mechanism. HPLC analysis showed that the dissolution rate and the solubility of the two novel cocrystals were both improved.
晶体工程策略被应用于开发拉莫三嗪的新固体形式。通过干法研磨和液辅助研磨成功获得了拉莫三嗪与 4,4'-联吡啶（2:1）和 2,2'-联吡啶共晶（1:1.5）的两种新型共晶。通过 X 射线衍射、热分析和光谱分析对新型共晶进行了充分的表征和确认。还使用 DXRxi 拉曼显微镜来鉴定共晶。讨论了影响共晶形成的因素，如溶剂和共晶形成物的结构。此外，通过浆态结晶也获得了这两种新型共晶。应用聚焦光束反射测量和衰减全反射傅里叶变换红外等过程分析技术研究了共晶化过程和机制。HPLC 分析表明，两种新型共晶的溶出速率和溶解度均得到提高。
