公开(公告)号：US08354122B2

公开(公告)日：2013-01-15

申请号：US11736834

申请日：2007-04-18

申请人： Takafumi Hoshino ,  Fumie Kusaki ,  Ikuo Fukui

发明人： Takafumi Hoshino ,  Fumie Kusaki ,  Ikuo Fukui

IPC分类号： A61K9/20

CPC分类号： B05D1/02 ,  A61J3/005 ,  A61K9/146 ,  A61K9/1623 ,  A61K9/1652 ,  A61K9/167 ,  A61K9/2077 ,  A61K31/4422

摘要： Provided are a granule or a tablet of a solid dispersion that allows a drug in a preparation to be rapidly dissolved without impairing the dissolution of the solid dispersion, and a method for producing the same. More specifically, provided are a granule of a solid dispersion comprising a poorly soluble drug, a water-soluble polymer, an excipient and a disintegrator, wherein a content of the water-soluble polymer is 1 to 10% by weight and a content of the disintegrator is 15 to 50% by weight; a tablet of a solid dispersion comprising a poorly soluble drug, a water-soluble polymer, an excipient and a disintegrator, wherein a content of the water-soluble polymer is 1 to 5% by weight and a content of the disintegrator is 15 to 50% by weight; and a method for producing a granule or tablet of a solid dispersion comprising spraying a water-soluble polymer solution in which a poorly soluble drug has been dispersed or dissolved, on a mixed powder of an excipient and a disintegrator, and granulating and drying a resultant.

摘要翻译： 提供一种固体分散体的颗粒或片剂，其允许制剂中的药物快速溶解而不损害固体分散体的溶解，及其制备方法。 更具体地，提供了包含难溶性药物，水溶性聚合物，赋形剂和崩解剂的固体分散体的颗粒，其中水溶性聚合物的含量为1〜10重量％，含量为 崩解剂为15〜50重量％ 包含难溶性药物，水溶性聚合物，赋形剂和崩解剂的固体分散体片剂，其中所述水溶性聚合物的含量为1〜5重量％，所述崩解剂的含量为15〜50 重量％ 以及制备固体分散体的颗粒或片剂的方法，包括将难溶性药物已经分散或溶解的水溶性聚合物溶液喷雾到赋形剂和崩解剂的混合粉末上，并将所得物 。

公开(公告)号：US20080038339A1

公开(公告)日：2008-02-14

申请号：US11888445

申请日：2007-08-01

申请人： Takafumi Hoshino ,  Fumie Kusaki ,  Naosuke Maruyama ,  Yuichi Nishiyama ,  Ikuo Fukui ,  Hiroshi Umezawa

发明人： Takafumi Hoshino ,  Fumie Kusaki ,  Naosuke Maruyama ,  Yuichi Nishiyama ,  Ikuo Fukui ,  Hiroshi Umezawa

IPC分类号： A61K9/10 ,  A61K47/30 ,  A61K47/38

CPC分类号： A61K9/2054 ,  A61K31/44

摘要： Provided are a solid dosage form comprising a solid dispersion that allows a drug in the preparation to be rapidly dissolved without compromising the solubility of the solid dispersion, and a method for producing the same. More specifically, provided is a solid dosage form comprising a solid dispersion, the dispersion comprising: a poorly soluble drug, a water-soluble polymer and a disintegrant, wherein the disintegrant is low-substituted hydroxypropylcellulose having an average particle size of 10 to 100 μm and a specific surface area measured by BET method of at least 1.0 m2/g. Moreover, provided is a method for producing a solid dosage form comprising a solid dispersion, the method comprising steps of: spraying a water-soluble polymer solution in which a poorly soluble drug has been dispersed or dissolved, on a powder of low-substituted hydroxypropylcellulose having an average particle size of 10 to 100 μm and a specific surface area measured by BET method of at least 1.0 m2/g and serving as a disintegrant and granulating the resultant; and drying.

摘要翻译： 提供了一种固体剂型及其制备方法，该固体分散体允许制剂中的药物快速溶解而不损害固体分散体的溶解性。 更具体地，提供了包含固体分散体的固体剂型，所述分散体包含：难溶性药物，水溶性聚合物和崩解剂，其中所述崩解剂是平均粒度为10至100μm的低取代羟丙基纤维素 并且通过BET法测量的比表面积为至少1.0m 2 / g。 此外，提供了一种制备包含固体分散体的固体剂型的方法，所述方法包括以下步骤：将难溶性药物已经分散或溶解的水溶性聚合物溶液喷雾到低取代羟丙基纤维素粉末上 平均粒径为10〜100μm，通过BET法测定的比表面积为至少1.0m 2 / g，作为崩解剂，造粒; 并干燥。

公开(公告)号：US08343547B2

公开(公告)日：2013-01-01

申请号：US11888445

申请日：2007-08-01

申请人： Takafumi Hoshino ,  Fumie Kusaki ,  Naosuke Maruyama ,  Yuichi Nishiyama ,  Ikuo Fukui ,  Hiroshi Umezawa

发明人： Takafumi Hoshino ,  Fumie Kusaki ,  Naosuke Maruyama ,  Yuichi Nishiyama ,  Ikuo Fukui ,  Hiroshi Umezawa

IPC分类号： A61K9/14 ,  A61K9/50

CPC分类号： A61K9/2054 ,  A61K31/44

摘要： Provided are a solid dosage form comprising a solid dispersion that allows a drug in the preparation to be rapidly dissolved without compromising the solubility of the solid dispersion, and a method for producing the same. More specifically, provided is a solid dosage form comprising a solid dispersion, the dispersion comprising: a poorly soluble drug, a water-soluble polymer and a disintegrant, wherein the disintegrant is low-substituted hydroxypropylcellulose having an average particle size of 10 to 100 μm and a specific surface area measured by BET method of at least 1.0 m2/g. Moreover, provided is a method for producing a solid dosage form comprising a solid dispersion, the method comprising steps of: spraying a water-soluble polymer solution in which a poorly soluble drug has been dispersed or dissolved, on a powder of low-substituted hydroxypropylcellulose having an average particle size of 10 to 100 μm and a specific surface area measured by BET method of at least 1.0 m2/g and serving as a disintegrant and granulating the resultant; and drying.

摘要翻译： 提供了一种固体剂型及其制备方法，该固体分散体允许制剂中的药物快速溶解而不损害固体分散体的溶解性。 更具体地，提供了包含固体分散体的固体剂型，所述分散体包含：难溶性药物，水溶性聚合物和崩解剂，其中所述崩解剂是平均粒度为10至100μm的低取代羟丙基纤维素 并且通过BET法测量的比表面积为至少1.0m 2 / g。 此外，提供了一种制备包含固体分散体的固体剂型的方法，所述方法包括以下步骤：将难溶性药物已经分散或溶解的水溶性聚合物溶液喷雾到低取代羟丙基纤维素粉末上 平均粒径为10〜100μm，BET法测定的比表面积为1.0m 2 / g以上，作为崩解剂造粒， 并干燥。

公开(公告)号：US20070248681A1

公开(公告)日：2007-10-25

申请号：US11736834

申请日：2007-04-18

申请人： Takafumi HOSHINO ,  Fumie KUSAKI ,  Ikuo FUKUI

发明人： Takafumi HOSHINO ,  Fumie KUSAKI ,  Ikuo FUKUI

IPC分类号： A61K9/14 ,  A61K9/62

CPC分类号： B05D1/02 ,  A61J3/005 ,  A61K9/146 ,  A61K9/1623 ,  A61K9/1652 ,  A61K9/167 ,  A61K9/2077 ,  A61K31/4422

摘要： Provided are a granule or a tablet of a solid dispersion that allows a drug in a preparation to be rapidly dissolved without impairing the dissolution of the solid dispersion, and a method for producing the same. More specifically, provided are a granule of a solid dispersion comprising a poorly soluble drug, a water-soluble polymer, an excipient and a disintegrator, wherein a content of the water-soluble polymer is 1 to 10% by weight and a content of the disintegrator is 15 to 50% by weight; a tablet of a solid dispersion comprising a poorly soluble drug, a water-soluble polymer, an excipient and a disintegrator, wherein a content of the water-soluble polymer is 1 to 5% by weight and a content of the disintegrator is 15 to 50% by weight; and a method for producing a granule or tablet of a solid dispersion comprising spraying a water-soluble polymer solution in which a poorly soluble drug has been dispersed or dissolved, on a mixed powder of an excipient and a disintegrator, and granulating and drying a resultant.

摘要翻译： 提供一种固体分散体的颗粒或片剂，其允许制剂中的药物快速溶解而不损害固体分散体的溶解，及其制备方法。 更具体地，提供了包含难溶性药物，水溶性聚合物，赋形剂和崩解剂的固体分散体的颗粒，其中水溶性聚合物的含量为1〜10重量％，含量为 崩解剂为15〜50重量％ 包含难溶性药物，水溶性聚合物，赋形剂和崩解剂的固体分散体片剂，其中所述水溶性聚合物的含量为1〜5重量％，所述崩解剂的含量为15〜50 重量％ 以及制备固体分散体的颗粒或片剂的方法，包括将难溶性药物已经分散或溶解的水溶性聚合物溶液喷雾到赋形剂和崩解剂的混合粉末上，并将所得物 。

公开(公告)号：US20080038340A1

公开(公告)日：2008-02-14

申请号：US11888529

申请日：2007-08-01

申请人： Fumie Kusaki ,  Takafumi Hoshino ,  Naosuke Maruyama ,  Yuichi Nishiyama ,  Ikuo Fukui ,  Hiroshi Umezawa

发明人： Fumie Kusaki ,  Takafumi Hoshino ,  Naosuke Maruyama ,  Yuichi Nishiyama ,  Ikuo Fukui ,  Hiroshi Umezawa

IPC分类号： A61K9/10 ,  A61K47/30 ,  A61K47/38

CPC分类号： A61K9/1652 ,  A61K9/1623 ,  A61K9/2018 ,  A61K9/2054 ,  A61K9/2059 ,  A61K31/44

摘要： Provided are a solid dosage form comprising an enteric solid dispersion that allows a drug in the preparation to be rapidly dissolved without compromising the solubility of the solid dispersion, and a method for producing the same. More specifically, provided is a solid dosage form comprising an enteric solid dispersion comprising a poorly soluble drug, an enteric polymer and a disintegrant, wherein the disintegrant is low-substituted hydroxypropylcellulose having an average particle size of 10 to 100 μm and a specific surface area measured by BET method of at least 1.0 m2/g. Moreover, provided is a method for producing a solid dosage form comprising an enteric solid dispersion, the method comprising steps of: spraying an enteric polymer solution in which a poorly soluble drug has been dispersed or dissolved, on a powder of low-substituted hydroxypropylcellulose having an average particle size of 10 to 100 μm and a specific surface area measured by BET method of at least 1.0 m2/g and serving as a disintegrant; and granulating the resultant; and drying.

摘要翻译： 提供了一种固体剂型，其包含允许制剂中的药物快速溶解而不损害固体分散体的溶解性的肠溶固体分散体及其制备方法。 更具体地，提供了一种固体剂型，其包含包含难溶性药物，肠溶性聚合物和崩解剂的肠溶固体分散体，其中所述崩解剂是平均粒度为10至100μm的低取代羟丙基纤维素和比表面积 通过BET法测量为至少1.0m 2 / g。 此外，提供了一种生产包含肠溶固体分散体的固体剂型的方法，所述方法包括以下步骤：将难溶性药物已经分散或溶解的肠溶性聚合物溶液喷雾到具有 平均粒径为10〜100μm，通过BET法测定的比表面积为至少1.0m 2 / g，作为崩解剂; 并造成结果; 并干燥。

公开(公告)号：US08343548B2

公开(公告)日：2013-01-01

申请号：US11888529

申请日：2007-08-01

申请人： Fumie Kusaki ,  Takafumi Hoshino ,  Naosuke Maruyama ,  Yuichi Nishiyama ,  Ikuo Fukui ,  Hiroshi Umezawa

发明人： Fumie Kusaki ,  Takafumi Hoshino ,  Naosuke Maruyama ,  Yuichi Nishiyama ,  Ikuo Fukui ,  Hiroshi Umezawa

IPC分类号： A61K9/14 ,  A61K9/50

CPC分类号： A61K9/1652 ,  A61K9/1623 ,  A61K9/2018 ,  A61K9/2054 ,  A61K9/2059 ,  A61K31/44

摘要： Provided are a solid dosage form comprising an enteric solid dispersion that allows a drug in the preparation to be rapidly dissolved without compromising the solubility of the solid dispersion, and a method for producing the same. More specifically, provided is a solid dosage form comprising an enteric solid dispersion comprising a poorly soluble drug, an enteric polymer and a disintegrant, wherein the disintegrant is low-substituted hydroxypropylcellulose having an average particle size of 10 to 100 μm and a specific surface area measured by BET method of at least 1.0 m2/g. Moreover, provided is a method for producing a solid dosage form comprising an enteric solid dispersion, the method comprising steps of: spraying an enteric polymer solution in which a poorly soluble drug has been dispersed or dissolved, on a powder of low-substituted hydroxypropylcellulose having an average particle size of 10 to 100 μm and a specific surface area measured by BET method of at least 1.0 m2/g and serving as a disintegrant; and granulating the resultant; and drying.

摘要翻译： 提供了一种固体剂型，其包含允许制剂中的药物快速溶解而不损害固体分散体的溶解性的肠溶固体分散体及其制备方法。 更具体地，提供了包含包含难溶性药物，肠溶性聚合物和崩解剂的肠溶性固体分散体的固体剂型，其中所述崩解剂是平均粒径为10〜100μm的低取代羟丙基纤维素，比表面积 通过BET法测量为至少1.0m 2 / g。 此外，提供了一种生产包含肠溶固体分散体的固体剂型的方法，所述方法包括以下步骤：将难溶性药物已经分散或溶解的肠溶性聚合物溶液喷雾到具有 平均粒径为10〜100μm，BET法测定的比表面积为1.0m 2 / g以上，作为崩解剂; 并造成结果; 并干燥。

公开(公告)号：US20070248682A1

公开(公告)日：2007-10-25

申请号：US11736846

申请日：2007-04-18

申请人： Takafumi HOSHINO ,  Fumie KUSAKI ,  Ikuo FUKUI

发明人： Takafumi HOSHINO ,  Fumie KUSAKI ,  Ikuo FUKUI

IPC分类号： A61K9/14 ,  A61K9/16

CPC分类号： A61K47/38 ,  A61K9/1652 ,  A61K31/4422 ,  A61K47/26 ,  A61K47/36

摘要： Provided are a solid preparation comprising an enteric solid dispersion that allows a drug in the preparation to be rapidly dissolved without impairing the dissolution of the solid preparation, and a method for producing the same. More specifically, provided are a solid preparation comprising a poorly soluble drug, an enteric polymer, an excipient and a disintegrator, a mixed powder comprising at least the excipient and the disintegratior is partly or entirely covered with a solid dispersion comprising the poorly soluble dug and the enteric polymer; and a method for producing a solid preparation, comprising steps of: spraying an enteric polymer solution in which a poorly soluble drug has been dispersed or dissolved, on a mixed powder comprising an excipient and a disintegrator; and granulating and drying a resultant.

摘要翻译： 本发明提供一种固体制剂，其包含使制剂中的药物快速溶解而不损害固体制剂的溶解的肠溶固体分散体及其制造方法。 更具体地，提供了包含难溶性药物，肠溶性聚合物，赋形剂和崩解剂的固体制剂，至少包含赋形剂和崩解剂的混合粉末部分或完全被包含难溶性挖掘和 肠溶聚合物; 以及制备固体制剂的方法，包括以下步骤：将其中分散或溶解难溶性药物的肠溶性聚合物溶液喷雾到包含赋形剂和崩解剂的混合粉末上; 并造粒并干燥所得物。

公开(公告)号：US20070196399A1

公开(公告)日：2007-08-23

申请号：US11675905

申请日：2007-02-16

申请人： Fumie KUSAKI ,  Hiroyasu KOKUBO ,  Shinji SAKUMA ,  Shinji YAMASHITA

发明人： Fumie KUSAKI ,  Hiroyasu KOKUBO ,  Shinji SAKUMA ,  Shinji YAMASHITA

IPC分类号： A61K9/24

CPC分类号： A61K9/5078 ,  A61K9/5026 ,  A61K9/5042

摘要： Provided is an enteric-coated preparation comprising an enteric coating material capable of delivering a drug to a site within the small intestine in a site-specific manner. More specifically, provided is an enteric-coated preparation for delivering a drug to a site within the small intestine in a site-specific manner, comprising a drug-containing preparation and an enteric coating material which covers the preparation, wherein, in Dissolution Test as specified in the Japanese Pharmacopoeia Fourteenth Edition, no dissolution of the drug is observed in the Japanese Pharmacopoeia first fluid (pH 1.2) while dissolution of the drug is observed in the Japanese Pharmacopoeia second liquid (pH 6.8) 20 minutes or later from start of the Dissolution Test. The enteric coating material is preferably selected from the group consisting of hydroxypropylmethyl cellulose acetate succinate, hydroxypropylmethyl cellulose phthalate, methacrylic acid copolymer and carboxymethylethyl cellulose.

摘要翻译： 提供一种肠溶包衣制剂，其包含能够以特定地点方式将药物递送至小肠内的部位的肠溶衣材料。 更具体地，提供了一种肠溶包衣制剂，其用于以局部特异性的方式将药物递送到小肠内的部位，其包含含药制剂和覆盖该制剂的肠溶衣材料，其中在溶出度试验中 在日本药典第十四版中规定，在日本药典第一液体（pH 1.2）中没有观察到药物溶解，而在日本药典第二液体（pH 6.8）中观察到药物溶解20分钟或更晚从 溶出度测试 肠溶衣材料优选选自乙酸琥珀酸羟丙基甲基纤维素，邻苯二甲酸羟丙基甲基纤维素，甲基丙烯酸共聚物和羧甲基乙基纤维素。