[EN] 7-CARBOXYMETHYLOXY-3', 4', 5-TRIMETHOXY FLAVONE MONOHYDRATE, THE PREPARATION METHOD AND USES THEREOF<br/>[FR] MONOHYDRATE DE 7-CARBOXYMETHYLOXY-3',4',5-TRIMETHOXY FLAVONE, SON PROCEDE DE PREPARATION ET SON UTILISATION
申请人:DONG A PHARM CO LTD
公开号:WO2005023244A1
公开(公告)日:2005-03-17
The present invention relates to 7-carboxymethyloxy-3’, 4’, 5-trimethoxy flavone.monohydrate which is a non hygroscopic product suitable for the preparation of metered dose of 7-carboxymethyloxy-3’, 4’, 5-trimethoxy flavone having protective activity for gastrointestinal tract including the colon, and a preparation method and uses thereof. 7-carboxymethyloxy-3’, 4’, 5-trimethoxy flavone.monohydrate of the present invention has advantages such as mucus protecting activity for gastrointestinal tract including the colon, convenience for handling and storage under ordinary humidity owing to its non-hygroscopicity, and ability to contain an active compound consistently for the formulation production of a medicine. In addition, the preparation method of 7-carboxymethyloxy-3’, 4’, 5-trimethoxy flavone.monohydrate of the present invention reduces long steps of total synthesis and requires mild conditions for the production of a compound because autoclave condition is not necessary for methylation in this case, and makes mass-production possible without any purification process such as recrystallization or column chromatography.
本发明涉及7-羧甲氧基-3',4',5-三甲氧基黄酮一水合物,这是一种非吸湿性产品,适用于制备具有对胃肠道包括结肠具有保护活性的7-羧甲氧基-3',4',5-三甲氧基黄酮的定量剂量,以及其制备方法和用途。本发明的7-羧甲氧基-3',4',5-三甲氧基黄酮一水合物具有诸如对胃肠道包括结肠的黏膜保护活性、由于其非吸湿性而在普通湿度下方便处理和储存的优点,以及能够持续包含活性化合物以便制剂生产药物。此外,本发明的7-羧甲氧基-3',4',5-三甲氧基黄酮一水合物的制备方法减少了总合成的长步骤,并且在这种情况下,对于甲基化不需要高压灭菌条件,因此在生产化合物时需要温和条件,并且可以实现无需任何纯化过程(如重结晶或柱层析)的大规模生产。