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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

US07871644B2 Pharmaceutical composition for oral use with improved absorption 有权
标题翻译：用于口服使用的药物组合物具有改善的吸收
公开(公告)号：US07871644B2
公开(公告)日：2011-01-18
申请号：US10949114
申请日：2004-09-10
申请人： Shunsuke Watanabe , Shigeo Takemura , Yuuki Tsutsui , Himoru Kondo , Kiyo Nakanishi , Kazuhiro Sako , Toyohiro Sawada
发明人： Shunsuke Watanabe , Shigeo Takemura , Yuuki Tsutsui , Himoru Kondo , Kiyo Nakanishi , Kazuhiro Sako , Toyohiro Sawada
IPC分类号： A61K9/22 , A61K9/20 , A61K9/28 , A61K9/32 , A61K9/48
CPC分类号： A61K9/2027 , A61K9/2846 , A61K9/2853 , A61K9/2893 , A61K31/65 , A61K31/663 , A61K47/12 , A61K47/32
摘要： The present invention presents a pharmaceutical composition for oral use with improved absorption, which comprises drug, aminoalkyl methacrylate copolymer E, and acidic substance and is obtained by bringing said 3 components together and uniformly mixing at least this polymer and this acidic substance, and a method of improving oral absorption/by using this pharmaceutical composition. Moreover, the present invention presents an agent for improving oral absorption that increases drug permeability of the digestive tract mucous membrane and/or mucous layer present on the surface of this membrane, whose active ingredient is aminoalkyl methacrylate copolymer E. In addition, the present invention presents an oral agent for improving absorption by increasing drug permeability of the digestive tract mucous membrane and/or the mucous layer distributed over this mucous membrane, whose effective component is aminoalkyl methacrylate copolymer E.
摘要翻译：本发明提供了具有改善吸收性的口服用药物组合物，其包括药物，甲基丙烯酸氨基烷基酯共聚物E和酸性物质，并且通过使所述3种组分一起并将至少该聚合物与该酸性物质均匀混合而获得，通过使用该药物组合物改善口服吸收。此外，本发明提供了改善口服吸收的药剂，其增加存在于该膜的表面上的消化道粘膜和/或粘膜层的药物通透性，其活性成分是甲基丙烯酸氨基烷基酯共聚物E.另外，本发明提出了通过增加分泌在该粘膜上的消化道粘膜和/或粘膜层的药物通透性来改善吸收的口服剂，其有效成分是甲基丙烯酸氨基烷基酯共聚物E.

4. 发明申请

US20050163840A1 Drug delivery system for averting pharmacokinetic drug interaction and method thereof 审中-公开
标题翻译：用于避免药代动力学药物相互作用的药物递送系统及其方法
公开(公告)号：US20050163840A1
公开(公告)日：2005-07-28
申请号：US10866524
申请日：2004-06-10
申请人： Toyohiro Sawada , Kazuhiro Sako , Tatsunobu Yoshioka , Shunsuke Watanabe
发明人： Toyohiro Sawada , Kazuhiro Sako , Tatsunobu Yoshioka , Shunsuke Watanabe
IPC分类号： A61K9/00 , A61K9/16 , A61K9/20 , A61K9/22 , A61K9/28 , A61K9/50 , A61K31/341 , A61K31/5517 , A61K31/554
CPC分类号： A61K31/554 , A61K9/1652 , A61K9/2013 , A61K9/2031 , A61K9/2054 , A61K9/2077 , A61K9/2846 , A61K9/2853 , A61K9/2866 , A61K9/2886 , A61K9/5026 , A61K9/5078 , A61K31/341 , A61K31/5517
摘要： The present invention is a system for averting undesirable pharmacokinetic drug interaction between a drug and concomitant drug(s), which consists of controlling the in vivo release time and/or release site of the drug and/or the concomitant drug.
摘要翻译：本发明是用于避免药物和伴随药物之间不期望的药代动力学药物相互作用的系统，其包括控制药物和/或伴随药物的体内释放时间和/或释放部位。

5. 发明授权

US06562375B1 Stable pharmaceutical composition for oral use 有权
标题翻译：稳定的口服药物组合物
公开(公告)号：US06562375B1
公开(公告)日：2003-05-13
申请号：US09629405
申请日：2000-08-01
申请人： Kazuhiro Sako , Toyohiro Sawada , Keiichi Yoshihara , Tatsunobu Yoshioka , Shunsuke Watanabe
发明人： Kazuhiro Sako , Toyohiro Sawada , Keiichi Yoshihara , Tatsunobu Yoshioka , Shunsuke Watanabe
IPC分类号： A61K914
CPC分类号： A61K9/2031 , A61K9/2009
摘要： The present invention is to provide a stable pharmaceutical composition for oral use and preparation thereof in which changes are prevented in drug release at stored even under the exposure to light by adding yellow ferric oxide and/or red ferric oxide in a matrix type sustained-release preparation containing a drug, hydrophilic base, and polyethylene oxide. The present invention is to further provide a method for preventing changes in drug release at stored under the exposure to light in a matrix type sustained-release preparation containing a drug, hydrophilic base, and polyethylene oxide. The quality assurance period of the product can be prolonged and the product value can be improved by the present invention.
摘要翻译：本发明提供一种用于口服使用的稳定药物组合物及其制备方法，其中通过在基质型缓释中加入黄色氧化铁和/或红色氧化铁，甚至在暴露于光下时，在药物释放期间可以防止变化含有药物，亲水性碱和聚环氧乙烷的制剂。本发明进一步提供一种在含有药物，亲水性碱和聚环氧乙烷的基质型缓释制剂中防止在暴露于光下储存的药物释放变化的方法。通过本发明可以延长产品的质量保证期并提高产品价值。

6. 发明申请

US20050112206A1 Pharmaceutical composition for oral use with improved absorption 有权
标题翻译：用于口服使用的药物组合物具有改善的吸收
公开(公告)号：US20050112206A1
公开(公告)日：2005-05-26
申请号：US10949114
申请日：2004-09-10
申请人： Shunsuke Watanabe , Shigeo Takemura , Yuuki Tsutsui , Himoru Kondo , Kiyo Nakanishi , Kazuhiro Sako , Toyohiro Sawada
发明人： Shunsuke Watanabe , Shigeo Takemura , Yuuki Tsutsui , Himoru Kondo , Kiyo Nakanishi , Kazuhiro Sako , Toyohiro Sawada
IPC分类号： A61K31/663 , A61K45/00 , A61K47/02 , A61K47/12 , A61K47/18 , A61K47/22 , A61K47/32 , A61P1/00 , A61P1/04 , A61P1/10 , A61P1/12 , A61P1/14 , A61P1/16 , A61P3/02 , A61P3/06 , A61P3/10 , A61P5/00 , A61P5/38 , A61P7/04 , A61P9/00 , A61P9/04 , A61P9/06 , A61P9/10 , A61P9/12 , A61P11/00 , A61P11/08 , A61P11/10 , A61P11/14 , A61P13/00 , A61P13/02 , A61P19/06 , A61P19/10 , A61P21/02 , A61P23/00 , A61P25/08 , A61P25/16 , A61P25/18 , A61P25/20 , A61P25/22 , A61P25/24 , A61P29/00 , A61P31/04 , A61P35/00 , A61P43/00 , A61K9/70 , A61K9/14
CPC分类号： A61K9/2027 , A61K9/2846 , A61K9/2853 , A61K9/2893 , A61K31/65 , A61K31/663 , A61K47/12 , A61K47/32
摘要： The present invention presents a pharmaceutical composition for oral use with improved absorption, which comprises drug, aminoalkyl methacrylate copolymer E, and acidic substance and is obtained by bringing said 3 components together and uniformly mixing at least this polymer and this acidic substance, and a method of improving oral absorption/by using this pharmaceutical composition. Moreover, the present invention presents an agent for improving oral absorption that increases drug permeability of the digestive tract mucous membrane and/or mucous layer present on the surface of this membrane, whose active ingredient is aminoalkyl methacrylate copolymer E. In addition, the present invention presents an oral agent for improving absorption by increasing drug permeability of the digestive tract mucous membrane and/or the mucous layer distributed over this mucous membrane, whose effective component is aminoalkyl methacrylate copolymer E.
摘要翻译：本发明提供了具有改善吸收性的口服用药物组合物，其包括药物，甲基丙烯酸氨基烷基酯共聚物E和酸性物质，并且通过使所述3种组分一起并将至少该聚合物与该酸性物质均匀混合而获得，通过使用该药物组合物改善口服吸收。此外，本发明提供了改善口服吸收的药剂，其增加存在于该膜的表面上的消化道粘膜和/或粘膜层的药物通透性，其活性成分是甲基丙烯酸氨基烷基酯共聚物E.另外，本发明提出了通过增加分泌在该粘膜上的消化道粘膜和/或粘膜层的药物通透性来改善吸收的口服剂，其有效成分是甲基丙烯酸氨基烷基酯共聚物E.

7. 发明授权

US06436441B1 Hydrogel-forming sustained-release preparation 失效
标题翻译：水凝胶形成持续释放制剂
公开(公告)号：US06436441B1
公开(公告)日：2002-08-20
申请号：US08403752
申请日：1995-03-20
申请人： Kazuhiro Sako , Hiroshi Nakashima , Toyohiro Sawada , Akira Okada , Muneo Fukui
发明人： Kazuhiro Sako , Hiroshi Nakashima , Toyohiro Sawada , Akira Okada , Muneo Fukui
IPC分类号： A61K922
CPC分类号： A61K9/2054 , A61K9/2018 , A61K9/2031
摘要： The invention provides a hydrogel-type sustained-release preparation comprising (1) at least one drug, (2) an additive which insures a penetration of water into the core of the preparation and (3) a hydrogel-forming polymer, wherein said preparation is capable of undergoing substantially complete gelation during its stay in the upper digestive tract such as stomach and small intestine and is capable of releasing the drug in the lower digestive tract including colon. By the preparation of the invention, the drug is efficiently released and absorbed even in the colon so that a steady and sustained release effect can be achieved.
摘要翻译：本发明提供一种水凝胶型持续释放制剂，其包含（1）至少一种药物，（2）确保水渗入制剂核心的添加剂，和（3）水凝胶形成聚合物，其中所述制剂能够在上消化道（如胃和小肠）停留期间发生基本上完全的凝胶化，并且能够在包括结肠的下消化道中释放药物。通过本发明的制备，药物被有效地释放和吸收即使在结肠中也能达到稳定和持续释放的效果。

8. 发明授权

US08128958B2 Sustained release pharmaceutical composition 失效
标题翻译：持续释放药物组合物
公开(公告)号：US08128958B2
公开(公告)日：2012-03-06
申请号：US10843005
申请日：2004-05-10
申请人： Kazuhiro Sako , Toyohiro Sawada , Hiromu Kondo , Keiichi Yoshihara , Hiroyuki Kojima
发明人： Kazuhiro Sako , Toyohiro Sawada , Hiromu Kondo , Keiichi Yoshihara , Hiroyuki Kojima
IPC分类号： A61K9/20 , A61K9/16 , A61K9/22 , A61K9/50 , A01N41/06 , C07C303/00
CPC分类号： A61K31/18
摘要： The present invention provides a sustained-release pharmaceutical composition, characterized in that, there are contained tamsulosin or a pharmaceutically acceptable salt thereof and a carrier for a sustained-release pharmaceutical composition and the ratio (Cmin/Cmax ratio) of the plasma tamsulosin concentration at 24 hours after the administration of the preparation per os (Cmin) to the maximum plasma tamsulosin concentration after the administration (Cmax) is about 0.4 or more.
摘要翻译：本发明提供一种缓释药物组合物，其特征在于，含有坦索罗辛或其药学上可接受的盐和缓释药物组合物的载体以及血浆中坦索罗辛浓度的比（Cmin / Cmax比）给药后每小时制剂24小时（Cmin）至给药后的最大血浆坦洛新浓度（Cmax）为约0.4以上。

9. 发明申请

US20080199522A1 TIMED-RELEASE COMPRESSION-COATED SOLID COMPOSITION FOR ORAL ADMINISTRATION 审中-公开
标题翻译：用于口服管理的定时释放压实固体组合物
公开(公告)号：US20080199522A1
公开(公告)日：2008-08-21
申请号：US11841731
申请日：2007-08-20
申请人： Toyohiro Sawada , Kazuhiro Sako , Tatsunobu Yoshioka , Shunsuke Watanabe
发明人： Toyohiro Sawada , Kazuhiro Sako , Tatsunobu Yoshioka , Shunsuke Watanabe
IPC分类号： A61K9/24 , A61K31/55
CPC分类号： A61K9/2853 , A61K9/2893
摘要： The present invention was completed based on these discoveries and relates to in a hydrogel-forming compression-coated solid pharmaceutical preparation comprising a core tablet containing drug and outer layer made from hydrogel-forming polymer substance and hydrophilic base, the improvement, a timed-release compression-coated solid composition for oral administration, said composition comprising (1) drug and freely erodible filler are mixed with the core tablet, (2) the percentage erosion of the core tablet is approximately 40 to approximately 90%, and (3) the outer layer essentially does not contain the same drug as the above-mentioned drug. By releasing a drug after a specific lag time, it becomes possible to effectively deliver a drug to a specific site in the digestive tract. It is therefore useful as presented as a timed-release solid composition for oral administration of a drug that is to be effectively delivered in high concentrations to the afflicted site in the lower digestive tract, a drug that is to be effectively absorbed in the lower digestive tract, a drug that is effective for chronopharmacotherapy, etc.
摘要翻译：本发明是基于这些发现而完成的，涉及一种含水凝胶形成压缩包衣的固体药物制剂，其包含含有药物的核心片剂和由形成水凝胶的聚合物和亲水基质制成的外层，改进，定时释放用于口服给药的压制包衣固体组合物，所述组合物包括（1）药物和自由侵蚀的填料与芯片混合，（2）芯片的侵蚀百分比为约40至约90％，和（3）外层基本上不含有与上述药物相同的药物。通过在特定滞后时间后释放药物，可以有效地将药物递送到消化道中的特定部位。因此，作为口服给药药物的定时释放固体组合物是有效的，其可以高浓度有效地递送到下消化道中的受影响的部位，这是有效地吸收在下消化道中的药物管道，一种对慢性药物疗法有效的药物等

10. 发明申请

US20060292221A1 TIMED-RELEASE COMPRESSION-COATED SOLID COMPOSITION FOR ORAL ADMINISTRATION 审中-公开
标题翻译：用于口服管理的定时释放压实固体组合物
公开(公告)号：US20060292221A1
公开(公告)日：2006-12-28
申请号：US11463570
申请日：2006-08-09
申请人： Toyohiro Sawada , Kazuhiro Sako , Tatsunobu Yoshioka , Shunsuke Watanabe
发明人： Toyohiro Sawada , Kazuhiro Sako , Tatsunobu Yoshioka , Shunsuke Watanabe
IPC分类号： A61K9/22
CPC分类号： A61K9/2853 , A61K9/2031 , A61K9/2893 , A61K31/55
摘要： The present invention was completed based on these discoveries and relates to in a hydrogel-forming compression-coated solid pharmaceutical preparation comprising a core tablet containing drug and outer layer made from hydrogel-forming polymer substance and hydrophilic base, the improvement, a timed-release compression-coated solid composition for oral administration, said composition comprising (1) drug and freely erodible filler are mixed with the core tablet, (2) the percentage erosion of the core tablet is approximately 40 to approximately 90%, and (3) the outer layer essentially does not contain the same drug as the above-mentioned drug. By releasing a drug after a specific lag time, it becomes possible to effectively deliver a drug to a specific site in the digestive tract. It is therefore useful as presented as a timed-release solid composition for oral administration of a drug that is to be effectively delivered in high concentrations to the afflicted site in the lower digestive tract, a drug that is to be effectively absorbed in the lower digestive tract, a drug that is effective for chronopharmacotherapy, etc.
摘要翻译：本发明是基于这些发现而完成的，涉及一种含水凝胶形成压缩包衣的固体药物制剂，其包含含有药物的核心片剂和由形成水凝胶的聚合物和亲水基质制成的外层，改进，定时释放用于口服给药的压制包衣固体组合物，所述组合物包括（1）药物和自由侵蚀的填料与芯片混合，（2）芯片的侵蚀百分比为约40至约90％，和（3）外层基本上不含有与上述药物相同的药物。通过在特定滞后时间后释放药物，可以有效地将药物递送到消化道中的特定部位。因此，作为口服给药药物的定时释放固体组合物是有效的，其可以高浓度有效地递送到下消化道中的受影响的部位，这是有效地吸收在下消化道中的药物管道，一种对慢性药物疗法有效的药物等

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