LETELE Filipp (FR),ЛЕТЕЛЬЕ Филипп (FR),LINCH Majkl (FR),ЛИНЧ Майкл (FR),PEAN ZHan-Manyuel (FR),ПЕАН Жан-Манюэль (FR),LETELE Filipp,ЛЕТЕЛЬЕ Филипп,LINCH Majkl,ЛИНЧ Майкл,PEAN ZHan-Manyuel,ПЕАН Жан-Манюэль
申请号：
RU2013158816/04
公开号：
RU0002593749C2
申请日:
2012.06.08
申请国别(地区):
RU
年份:
2016
代理人:
摘要：
FIELD: chemistry.SUBSTANCE: invention relates to agomelatine co-crystall, which is characterised by that it consists of agomelatine, or N-[2-(7-methoxy-1-naphtyl)ethyl]acetamide of formula (I), and organic acid, which is in solid state at ambient temperature, which is selected from a steam-hydroxybenzoic acid, citric acid, oxalic acid, Gallic acid, maleic acid, malonic acid, glutaric acid, glycolic acid or ketoglutaric acid. Agomelatine co-crystall and organic acid are obtained by mixing two components in organic solvent in desirable proportions: 1 agomelatine equivalent at 0.25-4 mol equivalent of organic acid, than obtained solution is stirred and optionally is heated at temperature not exceeding boiling point of selected solvent, then mixture is cooled while stirring, and deposited co-crystall naturally or precipitates after absorption in second solvent, obtained precipitate is filtered and dried. Also co-crystall is obtained by combined grinding of two components. Also co-crystall is obtained by mixing two components in organic or aqueous-organic solvent, followed by freezing and drying at very low temperature. Alternative method of preparing co-crystall involves mixing powders agomelatine and said acid in mixer, and then mixture is extruded by extrusion in twin-screw mixers without matrix to obtain solid granulated product directly at extrusion device outlet. Agomelatine co-crystall and organic acid are applicable for preparing drugs for treating disturbed melatonin aergic system.EFFECT: technical result is agomelatine co-crystalls permitting to modify rate of active ingredient dissolution.19 cl, 13 exИзобретение относится к сокристаллу агомелатина, который характеризуется тем, что он состоит из агомелатина, или N-[2-(7-метокси-1-нафтил)этил]ацетамида формулы (I), и органической кислоты, которая находится в твердом состоянии при температуре окружающей среды, которая выбрана из пара-оксибензойной кислоты, лимонной кислоты, щавелевой кислоты, галловой кислоты, ма
