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1. 发明申请

US20090149554A1 WATER-SOLUBLE METAL ALCOHOLATE DERIVATIVES, PRODUCTION METHODS THEREOF, AND SOLID GELATINOUS EXTERNAL PREPARATIONS CONTAINING THE SAME 审中-公开
标题翻译：水溶性金属醇盐衍生物，其生产方法和含有其的固体外消旋制剂
公开(公告)号：US20090149554A1
公开(公告)日：2009-06-11
申请号：US12063275
申请日：2006-08-11
申请人： Yuko Ishikawa , Katzutami Sakamoto , Toshikhiko Seki , Isao Yajima , Shun Takahashi , Kei Watanabe
发明人： Yuko Ishikawa , Katzutami Sakamoto , Toshikhiko Seki , Isao Yajima , Shun Takahashi , Kei Watanabe
IPC分类号： A61K47/24 , C07F7/28 , C07F7/02
CPC分类号： C07F7/045 , A61K9/0014 , A61K47/10 , C07C31/20
摘要： The object of the present invention is to provide a production method of water-soluble silane derivatives, the separation and purification of which are easy, and the reaction for which can be conducted under an industrially practicable temperature condition (under the temperature condition of 90° C. or lower) and to provide compounds with which solid gelatinous external preparations, with excellent stability against a temperature change and against an effect of additives and with excellent usability, can be prepared. The water-soluble silane derivative could be formed by the substitution reaction of a metal alkoxide with a polyhydric alcohol under the presence of a solid catalyst. According to this production method, the separation of the catalyst from the product is very easy, and the reaction can be carried out under the temperature condition of 90° C. or lower. The obtained water-soluble metal alcoholate derivative can satisfactory solidify an aqueous formulation of an external preparation by its blending thereinto. The obtained solid gelatinous external preparation has excellent stability against a temperature change and against the effect of additives. In addition, the external preparation is easily disintegrated during use; thus the usability such as easiness to be scooped up with fingers and spreadability during application is excellent.
摘要翻译：本发明的目的是提供一种水溶性硅烷衍生物的制造方法，其分离纯化容易，其反应可以在工业上可行的温度条件下（在90℃的温度条件下进行） C.或更低），并且可以制备具有优异的耐温度变化稳定性和抗添加剂效果以及优异可用性的固体胶状外用制剂的化合物。水溶性硅烷衍生物可以通过金属醇盐与多元醇在固体催化剂存在下的取代反应形成。根据该制造方法，催化剂与产物的分离非常容易，反应可以在90℃以下的温度条件下进行。所得到的水溶性金属醇化物衍生物可以通过其混合来使外用制剂的水性制剂充分固化。所得固体凝胶状外用制剂对温度变化和添加剂的效果具有优异的稳定性。此外，外用制剂在使用过程中容易分解; 因此在使用时易于用手指舀起的可用性和铺展性优异。

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