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首页> 外文期刊>Crystal growth & design >Crystal Structures, Stability, and Solubility Evaluation of Two Polymorphs of a 2:1 Melatonin-Piperazine Cocrystal
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Crystal Structures, Stability, and Solubility Evaluation of Two Polymorphs of a 2:1 Melatonin-Piperazine Cocrystal

机译：晶体结构，稳定性和溶解度评价2：1褪黑素 - 哌嗪烯晶的两种多晶型物

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摘要

The polymorphism of cocrystals is not studied as widely as that of single-component crystals. In this work, two polymorphic forms of a cocrystal of melatonin with piperazine (MLT-PIP I and MLT-PIP II) in a 2:1 stoichiometry were successfully obtained and fully characterized. The crystal structures exhibit differences in hydrogen bonding modes and molecular packing arrangements across two polymorphs. Theoretical computations were carried out to compare their crystal lattice energy. They were also evaluated by thermal analysis, variable temperature X-ray powder diffraction, and dynamic vapor sorption measurements, as well as powder and intrinsic dissolution experiments. The results of experimental and theoretical studies conclude that MLT-PIP II, as the stable form, exhibits a significantly improved solubility and dissolution rate and is suitable to be developed into a more efficient formulation of melatonin.
机译：通过单组分晶体的基础上的聚晶的多态性并不是广泛的。 在这项工作中，成功地获得了2：1化学计量中的哌嗪（MLT-PIP I和MLT-PIP II）的两种多晶形式的褪黑素（MLT-PIP I和MLT-PIP II）。 晶体结构在两种多晶型物上表现出氢键合模式和分子包装布置的差异。 进行理论计算以比较它们的晶格能量。 还通过热分析，可变温度X射线粉末衍射和动态蒸汽吸附测量以及粉末和内在溶解实验来评估它们。 实验和理论研究的结果得出结论，作为稳定形式的MLT-PIP II表现出显着提高的溶解度和溶解速率，并且适合于更有效的褪黑素的制剂。

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  • 来源
    《Crystal growth & design》 |2020年第2期|共9页
  • 作者

    Yan Yan; Dai Xia-Lin; Jia Jun-Long; Zhao Xing-Hua; Li Zhi-Wei; Lu Tong-Bu; Chen Jia-Mei;

  • 作者单位

    Jiangsu Normal Univ Sch Chem &

    Mat Sci Jiangsu Key Lab Green Synthet Chem Funct Mat Xuzhou 221116 Jiangsu Peoples R China;

    Sun Yat Sen Univ Sch Pharmaceut Sci Guangzhou 510006 Peoples R China;

    Tianjin Univ Technol Sch Chem &

    Chem Engn Inst New Energy Mat &

    Low Carbon Technol Tianjin 300384 Peoples R China;

    Hebei Agr Univ Coll Vet Med Baoding 071000 Peoples R China;

    Shenzhen Cloud Comp Ctr Natl Supercomp Ctr Shenzhen Shenzhen 518000 Guangdong Peoples R China;

    Tianjin Univ Technol Sch Chem &

    Chem Engn Inst New Energy Mat &

    Low Carbon Technol Tianjin 300384 Peoples R China;

    Tianjin Univ Technol Sch Chem &

    Chem Engn Inst New Energy Mat &

    Low Carbon Technol Tianjin 300384 Peoples R China;

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  • 原文格式 PDF
  • 正文语种 eng
  • 中图分类 晶体学;
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