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1. 发明申请

US20090035372A1 METHOD FOR MANUFACTURING A PHARMACEUTICAL COMPOSITION FOR CONTROLLED RELEASE OF AN ACTIVE SUBSTANCE 审中-公开
标题翻译：制造用于控制释放活性物质的药物组合物的方法
公开(公告)号：US20090035372A1
公开(公告)日：2009-02-05
申请号：US12244719
申请日：2008-10-02
申请人： Akio Sugihara , Kazuhiro Sako , Toyohiro Sawada
发明人： Akio Sugihara , Kazuhiro Sako , Toyohiro Sawada
IPC分类号： A61K9/22 , A61K47/34 , A61K47/32 , A61K31/18
CPC分类号： A61K31/18 , A61K9/1641 , A61K9/2031
摘要： The present invention pertains to a sized product, which contains a drug, polyethylene oxide with a molecular weight of 2,000,000 or higher, and a specific size controlling agent for polyethylene oxide (substance with the appropriate plasticity and binding force) and wherein at least the above-mentioned specific size controlling agent is uniformly dispersed in the above-mentioned polyethylene oxide, a controlled-release pharmaceutical composition containing this sized product, and a method of manufacturing a controlled-release pharmaceutical composition containing this sized product.A controlled-release pharmaceutical composition with good uniformity of content can be presented by using powder particles of polyethylene oxide with powder properties suitable for tableting, which is obtained by uniform dispersion of the specific size controlling agent for polyethylene oxide of the present invention.
摘要翻译：本发明涉及含有药物，分子量为200万以上的聚环氧乙烷和聚环氧乙烷的特定尺寸控制剂（具有适当的可塑性和结合力的物质）的尺寸的产品，其中至少上述上述特定尺寸控制剂均匀地分散在上述聚环氧乙烷中，含有这种尺寸的产品的控释药物组合物，以及含有这种尺寸的产品的控释药物组合物的制造方法。通过使用本发明的聚环氧乙烷特定尺寸控制剂的均匀分散得到的适合于压片的粉末性能的聚环氧乙烷粉末颗粒，可以提供具有良好的含量均匀性的控释药物组合物。

2. 发明授权

US07442387B2 Pharmaceutical composition for controlled release of active substances and manufacturing method thereof 失效
标题翻译：活性物质的控释药物组合物及其制造方法
公开(公告)号：US07442387B2
公开(公告)日：2008-10-28
申请号：US10746562
申请日：2003-12-23
申请人： Akio Sugihara , Kazuhiro Sako , Toyohiro Sawada
发明人： Akio Sugihara , Kazuhiro Sako , Toyohiro Sawada
IPC分类号： A61K9/22 , A61K9/20 , A61K9/26 , A61K9/32 , A61K9/14 , A61K33/26 , A61K31/295 , A01N55/02 , A01N59/16
CPC分类号： A61K31/18 , A61K9/1641 , A61K9/2031
摘要： The present invention pertains to a sized product, which contains a drug, polyethylene oxide with a molecular weight of 2,000,000 or higher, and a specific size controlling agent for polyethylene oxide (substance with the appropriate plasticity and binding force) and wherein at least the above-mentioned specific size controlling agent is uniformly dispersed in the above-mentioned polyethylene oxide, a controlled-release pharmaceutical composition containing this sized product, and a method of manufacturing a controlled-release pharmaceutical composition containing this sized product.A controlled-release pharmaceutical composition with good uniformity of content can be presented by using powder particles of polyethtylene oxide with powder properties suitable for tableting, which is obtained by uniform dispersion of the specific size controlling agent for polyethylene oxide of the present invention.
摘要翻译：本发明涉及含有药物，分子量为200万以上的聚环氧乙烷和聚环氧乙烷的特定尺寸控制剂（具有适当的可塑性和结合力的物质）的尺寸的产品，其中至少上述上述特定尺寸控制剂均匀地分散在上述聚环氧乙烷中，含有这种尺寸的产品的控释药物组合物，以及含有这种尺寸的产品的控释药物组合物的制造方法。通过使用本发明的聚环氧乙烷特定尺寸控制剂的均匀分散得到的适合于压片的粉末特性的聚氧乙烯粉末颗粒，可以提供具有良好的含量均匀性的控释药物组合物。

3. 发明授权

US09198904B2 Pharmaceutical composition for oral administration 有权
标题翻译：用于口服给药的药物组合物
公开(公告)号：US09198904B2
公开(公告)日：2015-12-01
申请号：US12698566
申请日：2010-02-02
申请人： Takehiko Yasuji , Noriyuki Kinoshita , Hiroyuki Yoshino , Shuuya Kawahama , Kazuhiro Sako , Akio Sugihara
发明人： Takehiko Yasuji , Noriyuki Kinoshita , Hiroyuki Yoshino , Shuuya Kawahama , Kazuhiro Sako , Akio Sugihara
IPC分类号： A61K31/47 , A61K9/22 , A61P13/02 , A61K9/20 , A61K9/48 , A61K31/18 , A61K31/439
CPC分类号： A61K31/47 , A61K9/2086 , A61K9/4866 , A61K31/18 , A61K31/439 , A61K2300/00
摘要： The present invention relates to a pharmaceutical composition for oral administration comprising a modified release portion containing tamsulosin or a pharmaceutically acceptable salt thereof, and an immediate release portion containing solifenacin or a pharmaceutically acceptable salt thereof and a hydrophilic substance.In the pharmaceutical composition, the dissolution rate of each drug (in particular, solifenacin contained in the immediate release portion) is similar to those of the current single drug formulations, and the maximum percentage of drag dissolution of each drug (in particular, solifenacin contained in the immediate release portion) is 90% or more. Therefore, the pharmaceutical composition is a single formulation (i.e., a combined formulation) with a bioavailability equivalent to those of the current single drug formulations.
摘要翻译：本发明涉及口服给药的药物组合物，其包含含有坦索罗辛或其药学上可接受的盐的改性释放部分，以及含有索非那新或其药学上可接受的盐和亲水性物质的速释部分。在药物组合物中，每种药物（特别是立即释放部分中所含的solifenacin）的溶解速率与当前单一药物制剂的溶出速率相似，并且每种药物（特别是含有solifenacin的溶剂的最大百分比）在立即释放部分中）为90％以上。因此，药物组合物是具有与当前单一药物制剂相当的生物利用度的单一制剂（即组合制剂）。

4. 发明申请

US20100233260A1 PHARMACEUTICAL COMPOSITION FOR ORAL ADMINISTRATION 有权
标题翻译：用于口服管理的药物组合物
公开(公告)号：US20100233260A1
公开(公告)日：2010-09-16
申请号：US12698566
申请日：2010-02-02
申请人： Takehiko Yasuji , Noriyuki Kinoshita , Hiroyuki Yoshino , Shuuya Kawahama , Kazuhiro Sako , Akio Sugihara
发明人： Takehiko Yasuji , Noriyuki Kinoshita , Hiroyuki Yoshino , Shuuya Kawahama , Kazuhiro Sako , Akio Sugihara
IPC分类号： A61K31/47 , A61K9/22 , A61P13/02
CPC分类号： A61K31/47 , A61K9/2086 , A61K9/4866 , A61K31/18 , A61K31/439 , A61K2300/00
摘要： The present invention relates to a pharmaceutical composition for oral administration comprising a modified release portion containing tamsulosin or a pharmaceutically acceptable salt thereof, and an immediate release portion containing solifenacin or a pharmaceutically acceptable salt thereof and a hydrophilic substance.In the pharmaceutical composition, the dissolution rate of each drug (in particular, solifenacin contained in the immediate release portion) is similar to those of the current single drug formulations, and the maximum percentage of drag dissolution of each drug (in particular, solifenacin contained in the immediate release portion) is 90% or more. Therefore, the pharmaceutical composition is a single formulation (i.e., a combined formulation) with a bioavailability equivalent to those of the current single drug formulations.
摘要翻译：本发明涉及口服给药的药物组合物，其包含含有坦索罗辛或其药学上可接受的盐的改性释放部分，以及含有索非那新或其药学上可接受的盐和亲水性物质的速释部分。在药物组合物中，每种药物（特别是立即释放部分中所含的solifenacin）的溶解速率与当前单一药物制剂的溶出速率相似，并且每种药物（特别是含有solifenacin的溶剂的最大百分比）在立即释放部分中）为90％以上。因此，药物组合物是具有与当前单一药物制剂相当的生物利用度的单一制剂（即组合制剂）。

5. 发明授权

US07220873B2 Conjugated fatty acid containing monoglycerides and process for producing them 失效
标题翻译：含有单酸甘油酯的共轭脂肪酸及其制备方法
公开(公告)号：US07220873B2
公开(公告)日：2007-05-22
申请号：US10210207
申请日：2002-08-02
申请人： Yoshie Yamauchi , Takaya Yamamoto , Kentaro Tsutsumi , Yuji Shimada , Yomi Watanabe , Akio Sugihara , Yoshio Tominaga
发明人： Yoshie Yamauchi , Takaya Yamamoto , Kentaro Tsutsumi , Yuji Shimada , Yomi Watanabe , Akio Sugihara , Yoshio Tominaga
IPC分类号： C11C3/00
CPC分类号： C11C3/025 , A23D9/013 , C11C1/10 , C11C3/02 , C12P7/6472
摘要： This invention provides monoglycerides containing a conjugated fatty acid, and a process for producing the above described conjugated fatty acid containing monoglycerides in which all kinds of lipases can be used as catalysts.This invention relate to monoglycerides containing a conjugated fatty acid (preferably in an amount of 50% or more of fatty acids).This invention also relates to a process for producing the conjugated fatty acid containing monoglycerides, in which the conjugated fatty acid containing a free fatty acid and glycerol are subjected to the reaction of esterification, or of esterification and glycerolysis in the presence of lipase as a catalyst.
摘要翻译：本发明提供含有共轭脂肪酸的单酸甘油酯，以及含有单酸甘油酯的上述共轭脂肪酸的制造方法，其中可以使用各种脂肪酶作为催化剂。本发明涉及含有共轭脂肪酸的单酸甘油酯（优选为脂肪酸的50％以上的量）。本发明还涉及含有单酸甘油酯的共轭脂肪酸的制造方法，其中含有游离脂肪酸和甘油的共轭脂肪酸在脂肪酶作为催化剂存在下进行酯化反应或酯化和甘油分解。

6. 发明授权

US07794748B2 Stable oral solid drug composition 有权
标题翻译：稳定的口服固体药物组合物
公开(公告)号：US07794748B2
公开(公告)日：2010-09-14
申请号：US10928464
申请日：2004-08-27
申请人： Akio Sugihara , Katsuhiro Masaki , Takehiko Yasuji
发明人： Akio Sugihara , Katsuhiro Masaki , Takehiko Yasuji
IPC分类号： A61K9/20
CPC分类号： A61K31/19 , A61K31/4184 , A61K47/12 , A61K47/14 , A61K47/183 , A61K47/32 , C07D213/61
摘要： This invention is aimed to provide a stabilized formulation of ramosetron or a pharmaceutically acceptable salt thereof under a temperature/humidity condition, especially at a low content and relates to a stable oral solid drug composition of ramosetron or a pharmaceutically acceptable salt thereof, which is characterized by containing one or two or more members selected from the group consisting of an aliphatic carboxylic acid or an ester thereof, a hydroxycarboxylic acid or an ester thereof, an acidic amino acid, an enolic acid, an aromatic carboxyl compound or an ester thereof, and a carboxyl group-containing high-molecular substance, and to a stabilization method of the same. Also, this invention relates to a therapeutic agent of diarrhea-predominant irritable bowel syndrome containing from 0.002 to 0.02 mg of ramosetron hydrochloride as a daily dose or an equivalent molar amount of ramosetron or its pharmaceutically acceptable other salt as an active ingredient.
摘要翻译：本发明的目的是提供一种稳定的雷莫司琼或其药物上可接受的盐在温度/湿度条件下，特别是低含量的制剂，并且涉及一种稳定的雷莫司琼口服固体药物组合物或其药学上可接受的盐，其特征在于通过含有选自脂肪族羧酸或其酯，羟基羧酸或其酯，酸性氨基酸，烯醇酸，芳香族羧基化合物或其酯的一种或两种以上的成分，以及含羧基的高分子物质及其稳定化方法。此外，本发明涉及腹泻型肠易激综合征治疗剂，其含有0.002至0.02mg盐酸雷莫司琼作为日剂量或等摩尔量的雷莫司琼或其药学上可接受的其它盐作为活性成分。

7. 发明授权

US08039482B2 Composition of solifenacin or salt thereof for use in solid formulation 有权
标题翻译：用于固体制剂的索非那新或其盐的组合物
公开(公告)号：US08039482B2
公开(公告)日：2011-10-18
申请号：US10594127
申请日：2005-03-24
申请人： Akio Sugihara , Takehiko Yasuji , Katsuhiro Masaki , Daisuke Murayama
发明人： Akio Sugihara , Takehiko Yasuji , Katsuhiro Masaki , Daisuke Murayama
IPC分类号： C07D453/02 , C07D453/04 , A01N43/90
CPC分类号： C07D453/02 , A61K9/2031 , A61K31/439
摘要： A solid pharmaceutical preparation of solifenacin or a salt thereof, the preparation being stable and inhibited from decomposing with time when supplied to clinical fields. In a pharmaceutical preparation containing solifenacin or a salt thereof, the compound in an amorphous form was revealed to be causative of cardinal-drug decomposition with time. The composition for a solid pharmaceutical preparation of solifenacin or a salt thereof contains solifenacin or its salt each in a crystalline from, and the content provided are: a process for producing the composition; and a medicinal composition for solid pharmaceutical preparations which contains solifenacin and an amorphization inhibitor.
摘要翻译：索利诺辛或其盐的固体药物制剂，当供应到临床领域时，该制剂是稳定的并且被抑制随时间分解。在含有索非那新或其盐的药物制剂中，显示无定形形式的化合物随着时间的推移与原药分解有关。索非塞星或其盐的固体药物制剂的组合物含有solifenacin或其盐，各自为结晶，所提供的内容为：制备组合物的方法; 以及含有solifenacin和非晶化抑制剂的固体药物制剂用药物组合物。

8. 发明申请

US20080039516A1 Composition of Solifenacin or Salt Thereof for Use in Solid Formulation 有权
标题翻译：索非那新或其盐的组合用于固体制剂
公开(公告)号：US20080039516A1
公开(公告)日：2008-02-14
申请号：US10594127
申请日：2005-03-24
申请人： Akio Sugihara , Takehiko Yasuji , Katsuhiro Masaki , Daisuke Murayama
发明人： Akio Sugihara , Takehiko Yasuji , Katsuhiro Masaki , Daisuke Murayama
IPC分类号： A61K31/40 , A61P43/00 , C07D453/02
CPC分类号： C07D453/02 , A61K9/2031 , A61K31/439
摘要： A solid pharmaceutical preparation of solifenacin or a salt thereof, the preparation being stable and inhibited from decomposing with time when supplied to clinical fields. In a pharmaceutical preparation containing solifenacin or a salt thereof, the compound in an amorphous form was revealed to be causative of cardinal-drug decomposition with time. The composition for a solid pharmaceutical preparation of solifenacin or a salt thereof contains solifenacin or its salt each in a crystalline from, and the content provided are: a process for producing the composition; and a medicinal composition for solid pharmaceutical preparations which contains solifenacin and an amorphization inhibitor.
摘要翻译：索利诺辛或其盐的固体药物制剂，当供应到临床领域时，该制剂是稳定的并且被抑制随时间分解。在含有索非那新或其盐的药物制剂中，显示无定形形式的化合物随着时间的推移与原药分解有关。索非塞星或其盐的固体药物制剂的组合物含有solifenacin或其盐，各自为结晶，所提供的内容为：制备组合物的方法; 以及含有solifenacin和非晶化抑制剂的固体药物制剂用药物组合物。

9. 发明申请

US20050026981A1 Stable oral solid drug composition 有权
标题翻译：稳定的口服固体药物组合物
公开(公告)号：US20050026981A1
公开(公告)日：2005-02-03
申请号：US10928464
申请日：2004-08-27
申请人： Akio Sugihara , Katsuhiro Masaki , Takehiko Yasuji
发明人： Akio Sugihara , Katsuhiro Masaki , Takehiko Yasuji
IPC分类号： A61K47/04 , A61K9/14 , A61K9/20 , A61K31/00 , A61K31/19 , A61K31/4184 , A61K47/02 , A61K47/12 , A61K47/14 , A61K47/18 , A61K47/22 , A61K47/30 , A61K47/32 , A61K47/36 , A61K47/38 , A61P1/00 , A61P1/12 , A61P25/00 , A61P43/00 , C07D213/61 , C07D403/06
CPC分类号： A61K31/19 , A61K31/4184 , A61K47/12 , A61K47/14 , A61K47/183 , A61K47/32 , C07D213/61
摘要： This invention is aimed to provide a stabilized formulation of ramosetron or a pharmaceutically acceptable salt thereof under a temperature/humidity condition, especially at a low content and relates to a stable oral solid drug composition of ramosetron or a pharmaceutically acceptable salt thereof, which is characterized by containing one or two or more members selected from the group consisting of an aliphatic carboxylic acid or an ester thereof, a hydroxycarboxylic acid or an ester thereof, an acidic amino acid, an enolic acid, an aromatic carboxyl compound or an ester thereof, and a carboxyl group-containing high-molecular substance, and to a stabilization method of the same. Also, this invention relates to a therapeutic agent of diarrhea-predominant irritable bowel syndrome containing from 0.002 to 0.02 mg of ramosetron hydrochloride as a daily dose or an equivalent molar amount of ramosetron or its pharmaceutically acceptable other salt as an active ingredient.
摘要翻译：本发明的目的是提供一种稳定的雷莫司琼或其药物上可接受的盐在温度/湿度条件下，特别是低含量的制剂，并且涉及一种稳定的雷莫司琼口服固体药物组合物或其药学上可接受的盐，其特征在于通过含有选自脂肪族羧酸或其酯，羟基羧酸或其酯，酸性氨基酸，烯醇酸，芳香族羧基化合物或其酯的一种或两种以上的成分，以及含羧基的高分子物质及其稳定化方法。此外，本发明涉及腹泻型肠易激综合征治疗剂，其含有0.002至0.02mg盐酸雷莫司琼作为日剂量或等摩尔量的雷莫司琼或其药学上可接受的其它盐作为活性成分。

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