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1. 发明公开

KR1020080059212A 3-(2-디메틸아미노메틸 사이클로헥실) 페놀 지연 제형 无效
标题翻译： 3-（2-二甲基氨基甲酰基环己基）酚残基配方
公开(公告)号：KR1020080059212A
公开(公告)日：2008-06-26
申请号：KR1020087009033
申请日：2006-09-15
申请人： 그뤼넨탈 게엠베하
发明人： 융토비아스 , 바르톨로마우스요하네스
IPC分类号： A61K9/22 , A61K31/133
CPC分类号： A61K9/286 , A61K9/2018 , A61K9/2054 , A61K31/133 , A61K47/38 , A61K2300/00
摘要： The invention relates to a form of administration for the controlled releasing of the active substance 3-(2-dimethylaminomethyl cyclohexyl) phenol, preferably (1R,2R)-3-(2-dimethylaminomethyl cyclohexyl) phenol, or one of the pharmaceutically acceptable salts thereof. Said form of administration (i) in vivo reaches the peak plasma level of the active substance after 2 to 10 h, and/or (ii) in vitro releases 3.0 to 37 percent by weight of the active substance originally contained therein after 05 hours, 5.0 to 56 percent by weight after 1 hour, 10 to 77 percent by weight after 2 hours, 15 to 88 percent by weight after 3 hours, at least 30 percent by weight after 6 hours, at least 50 percent by weight after 12 hours, at least 70 percent by weight after 18 hours, and at least 80 percent by weight after 24 hours when measured according to the European pharmacopoeia by means of a blade mixer in buffer solution at a pH value of 6.9 (preferably 900 ml), a temperature of 37 °C, and 75 U/min.
摘要翻译：本发明涉及活性物质3-（2-二甲基氨基甲基环己基）苯酚，优选（1R，2R）-3-（2-二甲基氨基甲基环己基）苯酚或其药学上可接受的盐之一的受控释放的给药形式它们。所述给药形式（i）体内在2至10小时后达到活性物质的峰值血浆水平，和/或（ii）体外释放05至05之后最初含有的活性物质的3.0至37重量％ 1小时后为5.0〜56重量％，2小时后为10〜77重量％，3小时后为15〜88重量％，6小时后为至少30重量％，12小时后为至少50重量％ 18小时后至少70重量％，24小时后至少80重量％，根据欧洲药典，通过桨式混合器在pH值为6.9（优选900毫升）的缓冲溶液中测量，至少80重量％，温度 37°C和75 U / min。

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