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1. 发明申请

WO2010117089A3 ANTIMYCOTIC PHARMACEUTICAL COMPOSITION 审中-公开
标题翻译：抗氧化药物组合物
公开(公告)号：WO2010117089A3
公开(公告)日：2010-12-09
申请号：PCT/JP2010056881
申请日：2010-04-09
申请人： POLA PHARMA INC , NIHON NOHYAKU CO LTD , KOBAYASHI HIROKAZU , KOSUGI EIKO , KUBOTA NOBUO
发明人： KOBAYASHI HIROKAZU , KOSUGI EIKO , KUBOTA NOBUO
IPC分类号： A61K9/08 , A61K9/00 , A61K9/70 , A61K31/4178
CPC分类号： A61K31/4178 , A61K9/0014 , A61K9/08 , A61K9/7015 , A61K47/08 , A61K47/10 , A61K47/14
摘要： In a pharmaceutical composition for external use containing a compound such as luliconazole and/or a salt thereof in an amount of 5% by mass or more, comprised is/are acetone, a polyoxyethylene alkyl (having 8 to 30 carbon atoms) ether, and/or a polyoxyethylene alkenyl (having 8 to 30 carbon atoms) ether. Provided is a preparation using a solvent other than crotamiton, propylene carbonate, and N-methyl-2-pyrrolidone as a solvent for solubilization and steric stabilization and having the following properties: 1) when a compound represented by the general formula (1) and/or a salt thereof has a stereoisomer, the amount of the stereoisomer of the compound and/or a salt thereof produced under a preservation condition of 60°C. for 3 weeks is 1% by mass or less with respect to the total mass of the compound and/or a salt thereof at the beginning of preservation; 2) the preparation is in a clear liquid state when preserved at a constant temperature of 20°C. immediately after manufacture; and 3) no crystal is deposited when the preparation is preserved at 5°C. for 2 weeks after manufacture.
摘要翻译：在含有5质量％以上的卢立克唑等化合物和/或其盐的外用药物组合物中含有丙酮，聚氧乙烯烷基（碳原子数为8〜30），以及 /或聚氧乙烯烯基（具有8至30个碳原子）醚。本发明提供使用克罗他米通以外的溶剂，碳酸亚丙酯和N-甲基-2-吡咯烷酮作为用于增溶和空间稳定的溶剂的制剂，其具有以下性质：1）当通式（1）和 /或其盐具有立体异构体，在60℃的保存条件下产生的化合物和/或其盐的立体异构体的量。在保存开始时相对于化合物和/或其盐的总质量为3质量％以下为1质量％以下; 2）当在20℃的恒定温度下保存时，制剂处于澄清的液体状态。在制造之后立即; 和3）当制剂在5℃保存时，没有晶体沉积。在制造后2周。

2. 发明申请

WO2010117091A3 ANTIMYCOTIC PHARMACEUTICAL COMPOSITION 审中-公开
标题翻译：抗氧化药物组合物
公开(公告)号：WO2010117091A3
公开(公告)日：2010-12-02
申请号：PCT/JP2010056884
申请日：2010-04-09
申请人： POLA PHARMA INC , NIHON NOHYAKU CO LTD , KOBAYASHI HIROKAZU , KOSUGI EIKO , KUBOTA NOBUO
发明人： KOBAYASHI HIROKAZU , KOSUGI EIKO , KUBOTA NOBUO
IPC分类号： A61K9/08 , A61K9/00 , A61K9/70 , A61K31/4178
CPC分类号： A61K9/7015 , A61K9/0014 , A61K9/08 , A61K31/4178
摘要： In a pharmaceutical composition for external use containing a compound such as luliconazole and/or a salt thereof, comprised are a higher alcohol which is in a liquid state at 1 atm and 25°C. and/or a diester of a dibasic acid, provided that a diester carbonate is excluded, and a polyoxyethylene alkyl ether and/or a polyoxyethylene alkenyl ether. Provided is a preparation using a solvent other than crotamiton, propylene carbonate, and N-methyl-2-pyrroridone as a solvent for solubilization and steric stabilization and having the following properties: 1) when a compound represented by the general formula (1) and/or a salt thereof has a steroisomer, the amount of the stereoisomer of the compound and/or a salt thereof produced under a preservation condition of 60 degrees C. for 3 weeks is 1% by mass or less with respect to the total mass of the compound and/or a salt thereof at the beginning of preservation; 2) the preparation is in a clear liquid state when preserved at a constant temperature of 20°C. immediately after manufacture; and 3) no crystal is deposited when the preparation is preserved at 5°C. for 2 weeks after manufacture.
摘要翻译：含有卢立康唑等化合物和/或其盐的外用药物组合物含有在1atm，25℃下为液态的高级醇。和/或二元酸的二酯，条件是不包括碳酸二酯，以及聚氧乙烯烷基醚和/或聚氧乙烯链烯基醚。本发明提供一种使用克罗他米通以外的溶剂，碳酸亚丙酯和N-甲基-2-吡咯烷酮作为用于增溶和空间稳定的溶剂的制剂，其具有以下性质：1）当通式（1）和 /或其盐具有立体异构体时，在60℃的保存条件下制备的化合物和/或其盐的立体异构体的量相对于总质量为1质量％保存开始时的化合物和/或其盐; 2）当在20℃的恒定温度下保存时，制剂处于澄清的液体状态。在制造之后立即; 和3）当制剂在5℃保存时，没有晶体沉积。在制造后2周。

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