公开(公告)号：US10130610B2

公开(公告)日：2018-11-20

申请号：US13258114

申请日：2010-04-09

申请人： Hirokazu Kobayashi ,  Eiko Kosugi ,  Nobuo Kubota

发明人： Hirokazu Kobayashi ,  Eiko Kosugi ,  Nobuo Kubota

IPC分类号： A61K31/4178 ,  A61K9/00 ,  A61K9/08 ,  A61K9/70 ,  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.

公开(公告)号：US20120022120A1

公开(公告)日：2012-01-26

申请号：US13258324

申请日：2010-04-09

申请人： Hirokazu Kobayashi ,  Eiko Kosugi ,  Nobuo Kubota

发明人： Hirokazu Kobayashi ,  Eiko Kosugi ,  Nobuo Kubota

IPC分类号： A61K31/427 ,  A61P31/10

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 stereoisomer, 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： 在含有诸如卢可康唑和/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， 不包括碳酸二酯，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，碳酸亚丙酯和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％ 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。

公开(公告)号：US09050271B2

公开(公告)日：2015-06-09

申请号：US13258324

申请日：2010-04-09

申请人： Hirokazu Kobayashi ,  Eiko Kosugi ,  Nobuo Kubota

发明人： Hirokazu Kobayashi ,  Eiko Kosugi ,  Nobuo Kubota

IPC分类号： A61K31/4178 ,  A61K9/70 ,  A61K9/00 ,  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 stereoisomer, 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： 在含有诸如卢可康唑和/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， 不包括碳酸二酯，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，碳酸亚丙酯和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％ 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。

公开(公告)号：US20130011351A2

公开(公告)日：2013-01-10

申请号：US13258114

申请日：2010-04-09

申请人： Hirokazu Kobayashi ,  Eiko Kosugi ,  Nobuo Kubota

发明人： Hirokazu Kobayashi ,  Eiko Kosugi ,  Nobuo Kubota

IPC分类号： A61K31/4178 ,  A61P31/10

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％以上的化合物如卢立康唑和/或其盐的外用药物组合物中，丙酮，聚氧乙烯烷基（碳原子数为8〜30）的醚，以及 /或聚氧乙烯烯基（碳原子数为8〜30）的醚。 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％ 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。

公开(公告)号：US20120014893A1

公开(公告)日：2012-01-19

申请号：US13258114

申请日：2010-04-09

申请人： Hirokazu Kobayashi ,  Eiko Kosugi ,  Nobuo Kubota

发明人： Hirokazu Kobayashi ,  Eiko Kosugi ,  Nobuo Kubota

IPC分类号： A61K31/4178 ,  A61P31/10

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％以上的化合物如卢立康唑和/或其盐的外用药物组合物中，丙酮，聚氧乙烯烷基（碳原子数为8〜30）的醚，以及 /或聚氧乙烯烯基（碳原子数为8〜30）的醚。 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％ 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。