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Lovaplatin crystal, preparation method and drug application

机译:洛伐铂晶体,制备方法和药物应用

摘要

The present invention relates to new crystals A, B and F of lobaplatin as well as preparation methods therefor and pharmaceutical applications thereof. Lobaplatin crystal A has a melting point Tm.p.. of 220±5°C and is obtained by adding a lobaplatin trihydrate to a suspension crystallization solvent. Lobaplatin crystal B has a melting point Tm.p.. of 230±5°C and is obtained by performing solvent evaporation on a lobaplatin trihydrate or by adding a solvent to a lobaplatin dihydrate, and performing room temperature evaporation or solventing-out crystallization and then drying. Lobaplatin crystal F has a melting point Tm.p.. of 229±5°C and is obtained by adding methanol or ethanol to a lobaplatin dihydrate, stirring at room temperature until solids are dissolved, filtering out insolubles, slowly adding an organic solvent, crystallizing out, separating the crystal and drying the crystal. Compared with the existing lobaplatin and lobaplatin trihydrate, the lobaplatin crystals A, B and F have better stability and solubility, are more suitable for preparation of various forms of pharmaceutical preparations, are more suitable for storage and use, and can be better used for treating cancers such as breast cancer, small cell lung cancer, or chronic myeloid leukemia.
机译:本发明涉及洛巴铂的新晶体A,B和F及其制备方法和药物应用。洛铂铂晶体A的熔点Tm.p ..为220±5℃,并且是通过将洛铂铂三水合物添加到悬浮结晶溶剂中而获得的。洛铂铂晶体B的熔点Tm.p ..为230±5℃,是通过对洛铂铂三水合物进行溶剂蒸发或向洛铂铂二水合物中添加溶剂,然后进行室温蒸发或溶剂化结晶而获得的。然后干燥。洛铂铂晶体F的熔点Tm.p ..为229±5°C,是通过向洛铂铂二水合物中加入甲醇或乙醇,在室温下搅拌直至固体溶解,滤出不溶物,缓慢加入有机溶剂而制得的结晶出来,分离晶体并干燥晶体。与现有的洛铂铂和洛铂三水合物相比,洛铂晶体A,B和F具有更好的稳定性和溶解性,更适合于制备各种形式的药物制剂,更适合于储存和使用,并且可以更好地用于治疗癌症,例如乳腺癌,小细胞肺癌或慢性粒细胞白血病。

著录项

  • 公开/公告号JP6404461B2

    专利类型

  • 公开/公告日2018-10-10

    原文格式PDF

  • 申请/专利权人 貴州益佰制葯股▲ふん▼有限公司;

    申请/专利号JP20170514760

  • 发明设计人 竇 啓玲;隋 東虎;張 聖貴;

    申请日2014-11-28

  • 分类号C07C59/08;C07C51/43;C07C209/82;C07C211/65;A61K9/19;A61K31/132;A61K31/19;A61P11;A61P15;A61P35;A61P35/02;C07F15;A61K31/282;

  • 国家 JP

  • 入库时间 2022-08-21 13:08:24

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