| ORIGINAL ARTICLES |
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Crystal Structures, Stability, and Solubility Evaluation of a 2: 1 Diosgenin-Piperazine Cocrystal |
| Ningbo Gong1, Hongmei Yu1, Ying Wang1, Cheng Xing1, Kun Hu1, Guanhua Du2, Yang Lu1 |
1 Beijing Key Laboratory of Polymorphic Drugs, Institute of Materia Medica, Chinese Academy of Medical Sciences and Peking Union Medical College, Beijing 100050, China;
2 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 |
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Abstract 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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| Keywords
Diosgenin
Piperazine
Cocrystal
Characterization
Solubility
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| Fund:We thank the financial 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) and National Science and Technology Major Project of China (Grant No. 2018ZX09711001-010). |
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Corresponding Authors:
Guanhua Du, Yang Lu
E-mail: dugh@imm.ac.cn;luy@imm.ac.cn
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Issue Date: 19 August 2020
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