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    • 14. 发明授权
    • Crystal form of 5-hydroxy-1-methylimidazolidin-2,4-dione
    • 晶体形式的5-羟基-1-甲基咪唑烷-2,4-二酮
    • US07569701B2
    • 2009-08-04
    • US10508496
    • 2003-04-09
    • Kaoru OkamotoNaoharu NishimuraAkira Ishii
    • Kaoru OkamotoNaoharu NishimuraAkira Ishii
    • C07D233/80A61K31/4166
    • C07D233/72
    • Conventional I-form crystals of 5-hydroxy-1-methylhydantoin contain, remaining therein in a considerable amount, the organic solvent used in a purification step. In contrast, in II-form crystals, the amount of the organic solvent remaining therein is smaller than the detection limit. Namely, the II-form crystals contain substantially no residual organic solvent. The novel II-form crystals of 5-hydroxy-1-methylhydantoin obtained through recrystallization from water not only contain substantially no residual organic solvent, but also have a high bulk density and are hence advantageous for pharmaceutical preparation. They further have properties advantageous for production, such as low adhesion. The crystals are significantly useful as a material for medicines required to have high safety, such as drugs for renal insufficiency.
    • 常规的5-羟基-1-甲基乙内酰脲的I型晶体在其中保留相当量的纯化步骤中使用的有机溶剂。 相反,在II型晶体中,其中残留的有机溶剂的量小于检测限。 即,II型晶体基本上不含残留的有机溶剂。 通过从水中重结晶获得的5-羟基-1-甲基乙内酰脲的新型II型晶体不仅基本上不含有残留的有机溶剂,而且还具有高堆积密度,因此对于药物制剂是有利的。 它们还具有有利于生产的性质,例如低粘附性。 该晶体作为具有高度安全性的药物的材料,例如用于肾功能不全的药物是显着有用的。