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公开(公告)号:EP2416758B1
公开(公告)日:2017-09-06
申请号:EP10714491.7
申请日:2010-04-09
发明人: KOBAYASHI, Hirokazu , KOSUGI, Eiko , KUBOTA, Nobuo
IPC分类号: A61K9/08
CPC分类号: A61K9/7015 , A61K9/0014 , A61K9/08 , A61K31/4178
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公开(公告)号:EP2025337B1
公开(公告)日:2014-09-10
申请号:EP06811053.5
申请日:2006-10-02
CPC分类号: A61K31/4178 , A61K31/19 , A61K2300/00
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公开(公告)号:EP2579847A1
公开(公告)日:2013-04-17
申请号:EP11730088.9
申请日:2011-06-10
IPC分类号: A61K9/06 , A61K9/08 , A61K9/10 , A61K9/12 , A61K9/14 , A61K9/16 , A61K9/20 , A61K9/48 , A61K31/385 , A61K31/4178 , A61K47/10 , A61K47/14 , A61K47/34 , A61K47/44
CPC分类号: A61K31/4178 , A61K9/0014 , A61K9/08 , A61K31/385 , A61K47/10 , A61K47/14 , A61K47/22
摘要: An object is to provide a medicament preparation which is excellent in the solubilization stability in relation to a compound represented by the general formula (1) during the storage in a low temperature region and a high temperature region. The present invention resides in a pharmaceutical composition comprising 1) the compound represented by the general formula (1) and/or a salt thereof and 2) a polyhydric alcohol derivative. General formula (1) (In the formula, R
1 , R
2 independently represent hydrogen atom or halogen atom respectively, and at least one of R
1 , R
2 is halogen atom.)-
公开(公告)号:EP2470178A1
公开(公告)日:2012-07-04
申请号:EP10744747.6
申请日:2010-07-29
发明人: KOBAYASHI, Hirokazu , KUBOTA, Nobuo
IPC分类号: A61K31/4178 , A61P17/00 , A61P31/10 , A61K47/08
CPC分类号: A61K31/4178 , A61K9/0014 , A61K47/08 , A61P17/00 , A61P31/10
摘要: A pharmaceutical composition which comprises 1) a compound represented by the following general formula (1) and/or a salt thereof; and 2) a ketone such as methyl ethyl ketone. Preferably, the compound represented by the following general formula (1) is luliconazole, where R1═R2=a chlorine atom: where R1 and R2 each independently represents a hydrogen atom or a halogen atom, and at least one of R1 and R2 represents a halogen atom. The present invention provides a preparation excellent in solubilization stability for a compound represented by the general formula (1) and/or a salt thereof in low-temperature or high-temperature storage.
摘要翻译: 1。一种药物组合物,其含有1)下述通式(1)表示的化合物和/或其盐; 和2)酮如甲乙酮。 优选地,下述通式(1)表示的化合物为卢立康唑,其中R 1 = R 2 =氯原子:其中R 1和R 2各自独立地表示氢原子或卤素原子,且R 1且R 2表示卤素原子。 本发明提供一种在低温或高温储存下对由通式(1)表示的化合物和/或其盐的溶解稳定性优异的制剂。
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公开(公告)号:EP2416758B8
公开(公告)日:2017-10-18
申请号:EP10714491.7
申请日:2010-04-09
发明人: KOBAYASHI, Hirokazu , KOSUGI, Eiko , KUBOTA, Nobuo
IPC分类号: A61K9/08
CPC分类号: A61K9/7015 , A61K9/0014 , A61K9/08 , A61K31/4178
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公开(公告)号:EP2416757A2
公开(公告)日:2012-02-15
申请号:EP10714490.9
申请日:2010-04-09
发明人: KOBAYASHI, Hirokazu , KOSUGI, Eiko , KUBOTA, Nobuo
IPC分类号: A61K9/08
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.
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公开(公告)号:EP2470178B1
公开(公告)日:2018-10-17
申请号:EP10744747.6
申请日:2010-07-29
发明人: KOBAYASHI, Hirokazu , KUBOTA, Nobuo
IPC分类号: A61K31/4178 , A61P17/00 , A61P31/10 , A61K47/08 , A61K9/00
CPC分类号: A61K31/4178 , A61K9/0014 , A61K47/08 , A61P17/00 , A61P31/10
摘要: A pharmaceutical composition which comprises 1) a compound represented by the following general formula (1) and/or a salt thereof; and 2) a ketone such as methyl ethyl ketone. Preferably, the compound represented by the following general formula (1) is luliconazole, where R1═R2=a chlorine atom: where R1 and R2 each independently represents a hydrogen atom or a halogen atom, and at least one of R1 and R2 represents a halogen atom. The present invention provides a preparation excellent in solubilization stability for a compound represented by the general formula (1) and/or a salt thereof in low-temperature or high-temperature storage.
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公开(公告)号:EP2416758A2
公开(公告)日:2012-02-15
申请号:EP10714491.7
申请日:2010-04-09
发明人: KOBAYASHI, Hirokazu , KOSUGI, Eiko , KUBOTA, Nobuo
IPC分类号: A61K9/08
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: 在含有诸如卢立康唑和/或其盐的化合物的外用药物组合物中,包括在1大气压和25℃下处于液体状态的高级醇和/或二元酸的二酯, 排除碳酸二酯,聚氧乙烯烷基醚和/或聚氧乙烯烯基醚。 本发明提供使用克罗他米通以外的溶剂,碳酸丙烯酯和N-甲基-2-吡咯烷酮作为增溶和空间稳定化的溶剂的制剂,具有以下性质:1)当由通式(1)表示的化合物和 /或其盐具有立体异构体,在60℃的保存条件下生产的化合物和/或其盐的立体异构体的量为3周时相对于总质量为1质量% 该化合物和/或其盐在保存开始时; 2)制备后立即在20°C的恒温下保存时,制剂处于透明液体状态; 和3)当制剂在制备后在5℃下保存2周后,不沉积晶体。
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公开(公告)号:EP2025337A1
公开(公告)日:2009-02-18
申请号:EP06811053.5
申请日:2006-10-02
CPC分类号: A61K31/4178 , A61K31/19 , A61K2300/00
摘要: Provided is a pharmaceutical composition for external use, including: (i) luliconazole represented by the following structural formula (1) and/or a salt thereof; and (ii) α-hydroxycarboxylic acid and/or a salt thereof.
摘要翻译: 本发明提供一种外用药物组合物,其包括:(i)由以下结构式(1)表示的联利康唑和/或其盐; 和(ii)± - 羟基羧酸和/或其盐。
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公开(公告)号:EP2116241B1
公开(公告)日:2016-04-27
申请号:EP08702781.9
申请日:2008-01-17
申请人: Pola Pharma Inc.
CPC分类号: A61K31/4168 , A61K9/0019 , A61K47/12 , A61K47/18 , A61K47/22
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