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溶剂对黄芩素-烟酰胺共晶形成热力学的影响

范玉洁, 宋逸婷, 张亚琪, 钱帅, 魏元锋, 张建军

范玉洁, 宋逸婷, 张亚琪, 钱帅, 魏元锋, 张建军. 溶剂对黄芩素-烟酰胺共晶形成热力学的影响[J]. 中国药科大学学报, 2016, 47(4): 437-441. DOI: 10.11665/j.issn.1000-5048.20160408
引用本文: 范玉洁, 宋逸婷, 张亚琪, 钱帅, 魏元锋, 张建军. 溶剂对黄芩素-烟酰胺共晶形成热力学的影响[J]. 中国药科大学学报, 2016, 47(4): 437-441. DOI: 10.11665/j.issn.1000-5048.20160408
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FAN Yujie, SONG Yiting, ZHANG Yaqi, QIAN Shuai, WEI Yuanfeng, ZHANG Jianjun. Effect of solvents on the formation thermodynamics of baicalein-nicotinamide cocrystals[J]. Journal of China Pharmaceutical University, 2016, 47(4): 437-441. DOI: 10.11665/j.issn.1000-5048.20160408
Citation: FAN Yujie, SONG Yiting, ZHANG Yaqi, QIAN Shuai, WEI Yuanfeng, ZHANG Jianjun. Effect of solvents on the formation thermodynamics of baicalein-nicotinamide cocrystals[J]. Journal of China Pharmaceutical University, 2016, 47(4): 437-441. DOI: 10.11665/j.issn.1000-5048.20160408
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溶剂对黄芩素-烟酰胺共晶形成热力学的影响

  • 1.

    中国药科大学药剂学教研室

  • 2.

    浙江震元制药有限公司

  • 3.

    中国药科大学中药制剂教研室

基金项目: 江苏省自然科学基金资助项目(No.BK20141351)；江苏高校优势学科建设工程资助项目(PAPD)；浙江省微生物发酵与合成制药工程技术中心资助项目(No.2013E10030)

Effect of solvents on the formation thermodynamics of baicalein-nicotinamide cocrystals

摘要

    摘要
  • 摘要: 考察了黄芩素-烟酰胺共晶在乙酸乙酯、丙酮和氯仿中的形成热力学。通过测定25 ℃下黄芩素、烟酰胺及黄芩素-烟酰胺共晶在这3种溶剂中的溶解度，建立了不同溶剂中黄芩素-烟酰胺-溶剂三相图。结果显示，黄芩素-烟酰胺共晶在3种溶剂中均符合1∶1溶液络合模型，共晶的形成为热力学自发反应(ΔG0<；0)，与其他两种溶剂相比，共晶在氯仿中形成的ΔG0绝对值最小，且在氯仿为溶剂的三相图中共晶形成区域远离化学计量比线。本研究利用热力学研究方法为选择共晶制备用溶剂及优化共晶制备条件奠定了理论和应用基础。
    Abstract: The purpose of this study was to investigate the formation thermodynamics of baicalein(BE)-nicotinamide(NCT)cocrystals in three solvents including ethyl acetate, acetone and trichloromethane. The solubilities of BE, NCT and BE-NCT in the above solvents at 25 °C were measured. Ternary phase diagrams(TPDs)of the BE-NCT-solvent systems were established. The non-linear fitting equation according to 1 ∶1 complexation mechanism of BE-NCT cocrystals demonstrated a good correlation between calculated and experiment data. ΔG0< 0 suggested that BE-NCT cocrystal formation was a spontaneous process. Among the organic solvents studied, the absolute value of ΔG0 in trichloromethane was significantly lower than that in the other two solvents. In addition, the cocrystallization zone in trichloromethane was far away from stoichiometric line. This study provides a theoretical foundation for solvent selection and preparation-condition optimization of BE-NCT cocrystals.
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    • 参考文献(12)
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  • 刊出日期:  2016-08-24

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