| 引用本文: | 程桂林,邓彩赟,蒋成君.姜黄素-邻苯二酚共晶溶度积的研究[J].中国现代应用药学,2018,35(5):623-627. |
| CHENG Guilin,DENG Caiyun,JIANG Chengjun.Research on Solubility Products of Curcumin-catechol Co-crystal[J].Chin J Mod Appl Pharm(中国现代应用药学),2018,35(5):623-627. |
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| 摘要: |
| 目的 以姜黄素为药物活性成分，邻苯二酚为共晶形成物，研究姜黄素-邻苯二酚共晶在不同溶剂（甲醇和乙酸乙酯）中和不同温度下形成的热力学。方法 通过固态研磨法制备姜黄素-邻苯二酚共晶，并用X射线衍射表征，测定其在不同溶剂（甲醇、乙酸乙酯）、不同温度下的溶解度，采用络合模型计算共晶的溶度积（Ksp）和络合常数（K11）。结果 姜黄素-邻苯二酚共晶在甲醇溶剂中符合1：1溶液络合模型，随着温度的升高，Ksp逐渐增大，K11逐渐减小。在乙酸乙酯溶剂中符合无溶液络合模型，Ksp随温度升高而逐渐增加。结论 比较共晶在2种溶剂中的溶度积，发现其在甲醇中容易络合。该热力学研究为姜黄素-邻苯二酚共晶的制备条件优化奠定了一定的理论和应用基础。 |
| 关键词: 姜黄素 邻苯二酚 共晶 溶度积 |
| DOI：10.13748/j.cnki.issn1007-7693.2018.05.001 |
| 分类号:R913 |
| 基金项目:国家自然科学基金项目（21602206） |
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| Research on Solubility Products of Curcumin-catechol Co-crystal |
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CHENG Guilin1, DENG Caiyun2, JIANG Chengjun2
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1.Academy of Chinese Medical Sciences, Zhejiang Chinese Medical University, Hangzhou 310053 China;2.School of Biological and Chemical Engineering, Zhejiang University of Science and Technology, Hangzhou 310023, China
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| Abstract: |
| OBJECTIVE To investigate the thermodynamics of curcumin-catechol co-crystals in which curcumin was used as the active pharmaceutical ingredient and catechol as the co-crystal conformer, in different solvents (methanol and ethyl acetate) and different temperature.METHODS Co-crystal was prepared by solid state grinding method, and characterized by X-ray diffraction. Solubility of curcumin-catechol co-crystals in different solvents (methanol and ethyl acetate solvent) and various temperatures were measured, followed by fitting the complexation model to calculate solubility products (Ksp) and complexation constants (K11).RESULTS Based on the non-linear simulation, 1:1 complexation model was well fitted to the curcumincatechol co-crystal formation in methanol, while no complexation model was more suitable for that in ethyl acetate. The data Ksp increased while K11 decreased with the reaction temperature.CONCLUSION The co-crystal is easily complexable in methanol when compared the co-crystal solubility products in two solvents. This thermodynamic study has provided a theoretical and applied foundation for the preparation and optimization of curcumin-catechol co-crystal. |
| Key words: curcumin catechol co-crystal solubility products |
