Crystal Structures, Stability, and Solubility Evaluation of a 2:1 Diosgenin-Piperazine Cocrystal
作者机构：Beijing Key Laboratory of Polymorphic DrugsInstitute of Materia MedicaChinese Academy of Medical Sciences and Peking Union Medical CollegeBeijing 100050China Beijing City Key Laboratory of Drug Target Identification and Drug ScreeningInstitute of Materia MedicaChinese Academy of Medical Sciences and Peking Union Medical CollegeBeijing 100050China
出 版 物：《Natural Products and Bioprospecting》 (应用天然产物（英文）)
年 卷 期：2020年第10卷第4期
页 面：261-267页
学科分类：0710[理学-生物学] 0832[工学-食品科学与工程（可授工学、农学学位）] 1007[医学-药学(可授医学、理学学位)] 1004[医学-公共卫生与预防医学(可授医学、理学学位)] 1002[医学-临床医学] 07[理学] 1001[医学-基础医学(可授医学、理学学位)] 070303[理学-有机化学] 0703[理学-化学] 0901[农学-作物学] 0902[农学-园艺学]
基 金：support by National Key research and development Program of China(Grant No.2016YFC1000900) CAMS Innovation Found for Medical Sciences(Grant No.2017-I2M-1-010) Construction and application of technology integration system for efficient identification of natural/effective active small molecules(Grant No.2018ZX09711001-001) National Science and Technology Major Project of China(Grant No.2018ZX09711001-010).
主 题：Diosgenin Piperazine Cocrystal Characterization Solubility
摘 要：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.
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