公开(公告)号：US08420662B2

公开(公告)日：2013-04-16

申请号：US12597475

申请日：2008-04-25

申请人： Suguru Takaki ,  Kotoe Ohta ,  Yasuhide Horiuchi ,  Masato Kobayashi ,  Junko Kawasaki ,  Eijiro Horisawa

发明人： Suguru Takaki ,  Kotoe Ohta ,  Yasuhide Horiuchi ,  Masato Kobayashi ,  Junko Kawasaki ,  Eijiro Horisawa

IPC分类号： A61K31/44 ,  A61K9/00 ,  A61K9/16 ,  A61K9/20

CPC分类号： A61K31/485 ,  A61K9/2009 ,  A61K9/2018 ,  A61K9/2054

摘要： It is an object of the present invention to provide a stable solid preparation comprising a 4,5-epoxymorphinan derivative or a pharmacologically acceptable acid addition salt thereof as an effective ingredient.That is, the present invention provides the stable solid preparation comprising the 4,5-epoxymorphinan derivative or the pharmacologically acceptable acid addition salt thereof as the effective ingredient, and comprising sodium thiosulfate, a sugar or a sugar alcohol and hydroxypropylcellulose having a low degree of substitution in an amount of 1 to 30% by weight per weight of a unit containing the effective ingredient.

摘要翻译： 本发明的目的是提供一种稳定的固体制剂，其包含4,5-环氧吗啡喃衍生物或其药理学上可接受的酸加成盐作为有效成分。 也就是说，本发明提供了包含4,5-环氧吗啡喃衍生物或其药理学上可接受的酸加成盐作为有效成分的稳定的固体制剂，并且包含硫代硫酸钠，糖或糖醇和羟丙基纤维素 以含有有效成分的单位重量计1〜30重量％的量的替代。

公开(公告)号：US20100120815A1

公开(公告)日：2010-05-13

申请号：US12597475

申请日：2008-04-25

申请人： Suguru Takaki ,  Kotoe Ohta ,  Yasuhide Horiuchi ,  Masato Kobayashi ,  Junko Kawasaki ,  Eijiro Horisawa

发明人： Suguru Takaki ,  Kotoe Ohta ,  Yasuhide Horiuchi ,  Masato Kobayashi ,  Junko Kawasaki ,  Eijiro Horisawa

IPC分类号： A61K31/485 ,  A61P17/04

CPC分类号： A61K31/485 ,  A61K9/2009 ,  A61K9/2018 ,  A61K9/2054

摘要： It is an object of the present invention to provide a stable solid preparation comprising a 4,5-epoxymorphinan derivative or a pharmacologically acceptable acid addition salt thereof as an effective ingredient.That is, the present invention provides the stable solid preparation comprising the 4,5-epoxymorphinan derivative or the pharmacologically acceptable acid addition salt thereof as the effective ingredient, and comprising sodium thiosulfate, a sugar or a sugar alcohol and hydroxypropylcellulose having a low degree of substitution in an amount of 1 to 30% by weight per weight of a unit containing the effective ingredient.

摘要翻译： 本发明的目的是提供一种稳定的固体制剂，其包含4,5-环氧吗啡喃衍生物或其药理学上可接受的酸加成盐作为有效成分。 也就是说，本发明提供了包含4,5-环氧吗啡喃衍生物或其药理学上可接受的酸加成盐作为有效成分的稳定的固体制剂，并且包含硫代硫酸钠，糖或糖醇和羟丙基纤维素 以含有有效成分的单位重量计1〜30重量％的量的替代。

公开(公告)号：US08829019B2

公开(公告)日：2014-09-09

申请号：US13125726

申请日：2009-10-23

申请人： Kotoe Ohta ,  Suguru Takaki ,  Yasuhide Horiuchi

发明人： Kotoe Ohta ,  Suguru Takaki ,  Yasuhide Horiuchi

IPC分类号： A61K31/44 ,  A61K9/00 ,  A61K9/16 ,  A61K9/20 ,  A61K31/485

CPC分类号： A61K9/2059 ,  A61K9/1623 ,  A61K9/1676 ,  A61K9/2009 ,  A61K9/2018 ,  A61K9/2027 ,  A61K31/485

摘要： The present invention relates to a stable tablet comprising a 4,5-epoxymorphinan derivative or a pharmacologically acceptable acid addition salt thereof as an effective ingredient. That is, the tablet according to the present invention comprises: (1) as the effective ingredient, a specific 4,5-epoxymorphinan derivative or a pharmacologically acceptable acid addition salt; (2) sodium thiosulfate; (3) at least one selected from the group consisting of saccharides and sugar alcohols; and (4) crospovidone, sodium carboxymethyl starch or a mixture thereof, in which tablet the content of the aforementioned (4) is 1 to 20% by weight per unit weight containing the aforementioned effective ingredient.

摘要翻译： 本发明涉及包含4,5-环氧吗啡喃衍生物或其药理学上可接受的酸加成盐作为有效成分的稳定片剂。 也就是说，根据本发明的片剂包括：（1）作为有效成分的特定的4,5-环氧吗啡喃衍生物或药理学上可接受的酸加成盐; （2）硫代硫酸钠; （3）选自糖和糖醇的至少一种; 和（4）交聚维酮，羧甲基淀粉钠或其混合物，其中上述（4）的含量为含有上述有效成分的每单位重量的1至20重量％。

公开(公告)号：US20120114752A1

公开(公告)日：2012-05-10

申请号：US13125726

申请日：2009-10-23

申请人： Kotoe Ohta ,  Suguru Takaki ,  Yasuhide Horiuchi

发明人： Kotoe Ohta ,  Suguru Takaki ,  Yasuhide Horiuchi

IPC分类号： A61K31/485 ,  A61P17/04 ,  A61K9/28

CPC分类号： A61K9/2059 ,  A61K9/1623 ,  A61K9/1676 ,  A61K9/2009 ,  A61K9/2018 ,  A61K9/2027 ,  A61K31/485

摘要： The present invention relates to a stable tablet comprising a 4,5-epoxymorphinan derivative or a pharmacologically acceptable acid addition salt thereof as an effective ingredient. That is, the tablet according to the present invention comprises: (1) as the effective ingredient, a specific 4,5-epoxymorphinan derivative or a pharmacologically acceptable acid addition salt; (2) sodium thiosulfate; (3) at least one selected from the group consisting of saccharides and sugar alcohols; and (4) crospovidone, sodium carboxymethyl starch or a mixture thereof, in which tablet the content of the aforementioned (4) is 1 to 20% by weight per unit weight containing the aforementioned effective ingredient.

摘要翻译： 本发明涉及包含4,5-环氧吗啡喃衍生物或其药理学上可接受的酸加成盐作为有效成分的稳定片剂。 也就是说，根据本发明的片剂包括：（1）作为有效成分的特定的4,5-环氧吗啡喃衍生物或药理学上可接受的酸加成盐; （2）硫代硫酸钠; （3）选自糖和糖醇的至少一种; 和（4）交聚维酮，羧甲基淀粉钠或其混合物，其中上述（4）的含量为含有上述有效成分的每单位重量的1至20重量％。

公开(公告)号：US20120058186A1

公开(公告)日：2012-03-08

申请号：US13257820

申请日：2010-03-29

申请人： Suguru Takaki ,  Kotoe Ohta ,  Yasuhide Horiuch

发明人： Suguru Takaki ,  Kotoe Ohta ,  Yasuhide Horiuch

IPC分类号： A61K9/32 ,  A61K31/4422 ,  A61K31/18 ,  A61P25/14 ,  A61K31/445 ,  A61K31/4439 ,  A61K31/7008 ,  A61K31/551 ,  A61K31/485 ,  A61K31/426

CPC分类号： A61K31/133 ,  A61K9/0056 ,  A61K9/2077 ,  A61K9/2826 ,  A61K9/284 ,  A61K9/2866 ,  A61K31/18 ,  A61K31/426 ,  A61K31/4422 ,  A61K31/4439 ,  A61K31/4515 ,  A61K31/5517

摘要： The present invention relates to a stable orally disintegrating coated tablet containing a drug, wherein the tablet is coated with a coating layer containing a water-soluble substance and a polyvinyl alcohol resin of not less than 5% by weight based on the weight of the coating layer, the water-soluble substance dissolving in an amount of 1 g or more in less than 10 mL of water at 20° C., having a hydroxyl group(s) in its molecule, and having a molecular weight of not more than 200 per a unit hydroxyl group. There is provided a stable orally disintegrating coated tablet which does not cause a crack in the coating layer even when the orally disintegrating tablet has been swollen by moisture absorption under high humidity, while ensuring rapid disintegration properties in an oral cavity. In the case of an orally disintegrating tablet containing a light-unstable drug, degradation of the drug can be suppressed by blending a light shading agent in the coating layer.

摘要翻译： 本发明涉及一种含有药物的稳定的口腔崩解型包衣片剂，其中片剂的涂层含有不少于5重量％的水溶性物质和聚乙烯醇树脂，基于涂层的重量 层，在20℃下在少于10mL的水中溶解1g或更多的水溶性物质，其分子中具有羟基，分子量不大于200 每单位羟基。 提供了一种稳定的口腔崩解性包衣片剂，即使在口腔崩解片剂在高湿度下通过吸湿而膨胀，同时确保口腔中快速崩解性能，也不会在包衣层中引起裂纹。 在含有光不稳定药物的口腔崩解片剂的情况下，可以通过在遮光层中混合遮光剂来抑制药物的降解。

公开(公告)号：US08715730B2

公开(公告)日：2014-05-06

申请号：US13257820

申请日：2010-03-29

申请人： Suguru Takaki ,  Kotoe Ohta ,  Yasuhide Horiuch

发明人： Suguru Takaki ,  Kotoe Ohta ,  Yasuhide Horiuch

IPC分类号： A61K9/32

CPC分类号： A61K31/133 ,  A61K9/0056 ,  A61K9/2077 ,  A61K9/2826 ,  A61K9/284 ,  A61K9/2866 ,  A61K31/18 ,  A61K31/426 ,  A61K31/4422 ,  A61K31/4439 ,  A61K31/4515 ,  A61K31/5517

摘要： The present invention relates to a stable orally disintegrating coated tablet containing a drug, wherein the tablet is coated with a coating layer containing a water-soluble substance and a polyvinyl alcohol resin of not less than 5% by weight based on the weight of the coating layer, the water-soluble substance dissolving in an amount of 1 g or more in less than 10 mL of water at 20° C., having a hydroxyl group(s) in its molecule, and having a molecular weight of not more than 200 per a unit hydroxyl group. There is provided a stable orally disintegrating coated tablet which does not cause a crack in the coating layer even when the orally disintegrating tablet has been swollen by moisture absorption under high humidity, while ensuring rapid disintegration properties in an oral cavity. In the case of an orally disintegrating tablet containing a light-unstable drug, degradation of the drug can be suppressed by blending a light shading agent in the coating layer.

摘要翻译： 本发明涉及一种含有药物的稳定的口腔崩解型包衣片剂，其中片剂的涂层含有不少于5重量％的水溶性物质和聚乙烯醇树脂，基于涂层的重量 层，在20℃下在少于10mL的水中溶解1g或更多的水溶性物质，其分子中具有羟基，分子量不大于200 每单位羟基。 提供了一种稳定的口腔崩解性包衣片剂，即使在口腔崩解片剂在高湿度下通过吸湿而膨胀，同时确保口腔中快速崩解性能，也不会在包衣层中引起裂纹。 在含有光不稳定药物的口腔崩解片剂的情况下，可以通过在遮光层中混合遮光剂来抑制药物的降解。

公开(公告)号：US20100215750A1

公开(公告)日：2010-08-26

申请号：US12600021

申请日：2008-05-20

申请人： Kotoe Ohta ,  Satoshi Minakami ,  Hiroyuki Tokumitsu

发明人： Kotoe Ohta ,  Satoshi Minakami ,  Hiroyuki Tokumitsu

IPC分类号： A61K9/14 ,  A61K31/439 ,  A61P13/02 ,  A61P13/10 ,  A61P13/08

CPC分类号： A61K47/12 ,  A61K9/08 ,  A61K9/145 ,  A61K9/2009 ,  A61K9/2013 ,  A61K9/2018 ,  A61K9/205 ,  A61K9/282 ,  A61K9/2866 ,  A61K9/4858 ,  A61K31/485 ,  A61K47/183 ,  C07D489/02

摘要： A chemically stable oral preparation with an excellent dissolution property comprising as an effective ingredient a specific morphinan derivative or a pharmaceutically acceptable acid addition salt thereof is disclosed. The oral preparation according to the present invention comprises a specific morphinan derivative or a pharmaceutically acceptable acid addition salt thereof as an effective ingredient and an organic acid, wherein 1 g of said organic acid requires not less than 30 mL of water to dissolve in at 20° C. The method for improving dissolution property and chemical stability of an oral preparation according to the present invention comprises incorporating an organic acid in the oral preparation comprising as an effective ingredient a specific morphinan derivative or a pharmaceutically acceptable acid addition salt thereof, wherein 1 g of said organic acid requires not less than 30 mL of water to dissolve in at 20° C.

摘要翻译： 公开了具有优异溶解性的化学稳定的口服制剂，其包含具体的吗啡喃衍生物或其药学上可接受的酸加成盐作为有效成分。 根据本发明的口服制剂包含特定的吗啡喃衍生物或其药学上可接受的酸加成盐作为有效成分和有机酸，其中1g所述有机酸在20℃下需要不少于30mL的水溶解 ℃。根据本发明的口腔制剂的溶出性质和化学稳定性的改善方法包括将口服制剂中的有机酸掺入作为有效成分的特定吗啡喃衍生物或其药学上可接受的酸加成盐，其中1 g所述有机酸需要不少于30mL的水在20℃下溶解。

公开(公告)号：US09084817B2

公开(公告)日：2015-07-21

申请号：US12600021

申请日：2008-05-20

申请人： Kotoe Ohta ,  Satoshi Minakami ,  Hiroyuki Tokumitsu

发明人： Kotoe Ohta ,  Satoshi Minakami ,  Hiroyuki Tokumitsu

IPC分类号： A61K47/12 ,  A61K47/18 ,  A61K9/20 ,  A61K9/48 ,  A61K9/14 ,  A61K31/485 ,  C07D489/02 ,  A61K9/08 ,  A61K9/28

CPC分类号： A61K47/12 ,  A61K9/08 ,  A61K9/145 ,  A61K9/2009 ,  A61K9/2013 ,  A61K9/2018 ,  A61K9/205 ,  A61K9/282 ,  A61K9/2866 ,  A61K9/4858 ,  A61K31/485 ,  A61K47/183 ,  C07D489/02

摘要： A chemically stable oral preparation with an excellent dissolution property comprising as an effective ingredient a specific morphinan derivative or a pharmaceutically acceptable acid addition salt thereof is disclosed. The oral preparation according to the present invention comprises a specific morphinan derivative or a pharmaceutically acceptable acid addition salt thereof as an effective ingredient and an organic acid, wherein 1 g of said organic acid requires not less than 30 mL of water to dissolve in at 20° C. The method for improving dissolution property and chemical stability of an oral preparation according to the present invention comprises incorporating an organic acid in the oral preparation comprising as an effective ingredient a specific morphinan derivative or a pharmaceutically acceptable acid addition salt thereof, wherein 1 g of said organic acid requires not less than 30 mL of water to dissolve in at 20° C.

摘要翻译： 公开了具有优异溶解性的化学稳定的口服制剂，其包含具体的吗啡喃衍生物或其药学上可接受的酸加成盐作为有效成分。 根据本发明的口服制剂包含特定的吗啡喃衍生物或其药学上可接受的酸加成盐作为有效成分和有机酸，其中1g所述有机酸在20℃下需要不少于30mL的水溶解 ℃。根据本发明的口腔制剂的溶出性质和化学稳定性的改善方法包括将口服制剂中的有机酸掺入作为有效成分的特定吗啡喃衍生物或其药学上可接受的酸加成盐，其中1 g所述有机酸需要不少于30mL的水在20℃下溶解。

公开(公告)号：US20060073205A1

公开(公告)日：2006-04-06

申请号：US10958048

申请日：2004-10-04

申请人： Kotoe Ohta ,  Masayoshi Fuji ,  Takashi Takei ,  Masatoshi Chikazawa ,  Kenzo Toyoshima

发明人： Kotoe Ohta ,  Masayoshi Fuji ,  Takashi Takei ,  Masatoshi Chikazawa ,  Kenzo Toyoshima

IPC分类号： A61K9/24

CPC分类号： A61K9/143 ,  A61K9/5047

摘要： The present invention relates to controlled release granules for medical use comprising a drug loaded porous silica particle, and at least one layer of a controlled release coating material, characterized in that the drug loaded porous silica core is prepared by immersing dry porous silica particles with a solution, suspension or emulsion comprising at least one pharmacologically active drug and the resulting wet drug loaded porous silica core is subsequently dried again. Furthermore, the invention concerns a method for preparing the controlled release composition.

摘要翻译： 本发明涉及用于医疗用途的控制释放颗粒，其包含负载药物的多孔二氧化硅颗粒，以及至​​少一层控释包衣材料，其特征在于，通过将干燥的多孔二氧化硅颗粒浸入 包含至少一种药理学活性药物的溶液，悬浮液或乳液，然后再次干燥所得的湿药物加载的多孔二氧化硅核心。 此外，本发明涉及一种制备控释组合物的方法。

公开(公告)号：US20050244491A1

公开(公告)日：2005-11-03

申请号：US10470647

申请日：2005-04-06

申请人： Toshimitsu Ohki ,  Wakuko Yamaguchi ,  Kotoe Ohta

发明人： Toshimitsu Ohki ,  Wakuko Yamaguchi ,  Kotoe Ohta

IPC分类号： A61K9/00 ,  A61K9/20 ,  A61K31/5415

CPC分类号： A61K9/0056 ,  A61K9/2018 ,  A61K9/2059 ,  A61K31/5415

摘要： The present invention relates to a fast disintegrating tablet comprising meloxicam or a pharmaceutically acceptable salt thereof, starch or various starches, glidant and at least one additional excipient.

摘要翻译： 本发明涉及包含美洛昔康或其药学上可接受的盐，淀粉或各种淀粉，助流剂和至少一种其它赋形剂的快速崩解片剂。