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2. 发明申请

WO2012124907A2 I- AND II-TYPE CRYSTALS OF L-?-GLYCERYL PHOSPHORYL CHOLINE, AND METHOD FOR PREPARING SAME 审中-公开
标题翻译： L-β-甘油磷酸胆碱的I-和II-型晶体及其制备方法
公开(公告)号：WO2012124907A2
公开(公告)日：2012-09-20
申请号：PCT/KR2012001331
申请日：2012-02-22
申请人： HANSEOCHEM CO LTD , OH MIN-KEUN , KIM KI-NAM , SEO KI-HYEONG , KWON DAE-GIL
发明人： OH MIN-KEUN , KIM KI-NAM , SEO KI-HYEONG , KWON DAE-GIL
IPC分类号： C07F9/09 , C07B61/00 , C07C211/63
CPC分类号： C07F9/091
摘要： The present invention relates to I- and II-type crystals of L-a-glyceryl phosphoryl choline, and to a method for preparing same. More particularly, the present invention relates to noble I- and II-type anhydride crystals of L-a-glyceryl phosphoryl choline, which have a higher purity than conventional liquid L-a-glyceryl phosphoryl choline, and one advantage of which is that formulations and dosages of pharmaceuticals are easily modified, and another advantage of which is that the hygroscopicity of the crystals are much lower than that of conventional polymorphic crystals, providing excellent stability during storage. The present invention also relates to a method for preparing the I- and II-type crystals of L-a-glyceryl phosphoryl choline. The I-type crystal of L-a-glyceryl phosphoryl choline is characterized by having an onset temperature of 147°C and an absorption peak of 150°C based on differential scanning calorimeter (DSC) analysis, and by having diffraction patterns where 2?-diffraction angles are 9.8±0.2°, 12.0±0.2°, 14.3±0.2°, 15.8±0.2°, and 19.6±0.2° based on X-ray diffraction (XRD) analysis. The II-type crystal of L-a-glyceryl phosphoryl choline is characterized by having an onset temperature of 62°C and an absorption peak of 66°C, and an onset temperature of 141°C and an absorption peak of 145°C based on DSC analysis, and having diffraction patterns where 2?-diffraction angles are 10.3±0.2°, 12.2±0.2°, 13.4±0.2°, 14.8±0.2°, and 20.6±0.2° based on XRD analysis.
摘要翻译：本发明涉及L-α-甘油磷酰胆碱的I型和II型晶体，并涉及其制备方法。更具体地说，本发明涉及具有比常规液体La-甘油基磷酰胆碱更高纯度的La-甘油磷酰胆碱的惰性I-和II-型酸酐晶体，并且其一个优点是药物制剂和剂量容易改性，另一个优点是晶体的吸湿性远低于常规多晶型晶体，在储存期间提供优异的稳定性。本发明还涉及制备L-α-甘油磷酰胆碱的I型和II型晶体的方法。基于差示扫描量热计（DSC）分析，La-甘油磷酰胆碱的I型晶体的特征在于具有147℃的起始温度和150℃的吸收峰，并且通过具有2θ-衍射基于X射线衍射（XRD）分析，角度为9.8±0.2°，12.0±0.2°，14.3±0.2°，15.8±0.2°和19.6±0.2°。根据DSC，La-甘油磷酰胆碱的II型晶体的特征在于具有62℃的起始温度和66℃的吸收峰，并且起始温度为141℃并且吸收峰为145℃ 分析，并且具有基于XRD分析的2θ-衍射角为10.3±0.2°，12.2±0.2°，13.4±0.2°，14.8±0.2°和20.6±0.2°的衍射图案。

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