Gong Ningbo, Yu Hongmei, Wang Ying, Xing Cheng, Hu Kun, Du Guanhua, Lu Yang
Beijing Key Laboratory of Polymorphic Drugs, Institute of Materia Medica, Chinese Academy of Medical Sciences and Peking Union Medical College, Beijing, 100050, China.
Beijing City Key Laboratory of Drug Target Identification and Drug Screening, Institute of Materia Medica, Chinese Academy of Medical Sciences and Peking Union Medical College, Beijing, 100050, China.
Nat Prod Bioprospect. 2020 Aug;10(4):261-267. doi: 10.1007/s13659-020-00256-y. Epub 2020 Jul 6.
A cocrystal of diosgenin with piperazine in 2:1 stoichiometry was successfully synthesized. The solid form was prepared by liquid assisted grinding, slurry and crystallization methods. The cocrystal was characterized by powder X-ray diffraction, differential scanning calorimetry, thermogravimetric analysis, Fourier transform infrared spectroscopy, and structure determined by single crystal X-ray diffraction, the hydrogen bonds formed into fish bone structure along the [010] direction and all the molecules packed into 3D layer structure along a axis. After formation of cocrystal, the solubility of diosgenin was improved, and the solubility value in 0.2% SDS solution was approximately 1.5 times as large as that of the parent material.
成功合成了薯蓣皂苷元与哌嗪化学计量比为2:1的共晶体。通过液体辅助研磨、浆体法和结晶法制备了该固体形式。通过粉末X射线衍射、差示扫描量热法、热重分析、傅里叶变换红外光谱对共晶体进行了表征，并通过单晶X射线衍射确定了其结构，氢键沿[010]方向形成鱼骨结构，所有分子沿a轴堆积成三维层状结构。共晶体形成后，薯蓣皂苷元的溶解度得到提高，在0.2%十二烷基硫酸钠溶液中的溶解度值约为母体材料的1.5倍。
