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Lovaplatin crystal, preparation method and drug application
专利权人:
貴州益佰制葯股▲ふん▼有限公司
发明人:
竇 啓玲,隋 東虎,張 聖貴
申请号:
JP2017514760
公开号:
JP6404461B2
申请日:
2014.11.28
申请国别(地区):
JP
年份:
2018
代理人:
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.
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