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1. 发明授权

US06506407B2 Colon-specific drug release system 有权
公开(公告)号：US06506407B2
公开(公告)日：2003-01-14
申请号：US09952992
申请日：2001-09-14
申请人： Shunsuke Watanabe , Hitoshi Kawai , Masataka Katsuma , Muneo Fukui
发明人： Shunsuke Watanabe , Hitoshi Kawai , Masataka Katsuma , Muneo Fukui
IPC分类号： A61K948
CPC分类号： A61K9/2886 , A61K9/2018 , A61K9/2826 , A61K9/2846 , A61K9/4808
摘要： A system for releasing a drug specifically in the colon of the gastrointestinal tract, which comprises a drug (b) coated with an organic acid-soluble polymer material (a), and a saccharide (c) which rapidly generates an organic acid by the action of enterobacteria in the lower part of the gastrointestinal tract; a colon-specific drug release oral preparation, which comprises a composition comprising a drug (b) coated with an organic acid-soluble polymer material (a) and a saccharide (c) which rapidly generates an organic acid by the action of enterobacteria in the lower part of the gastrointestinal tract, said composition being coated with an enteric coating polymer material (d). The invention provides a drug release system and a preparation which utilize enterobacteria, which do not form harmful substances due to the release-starting mechanism, show rapid degradation, and have higher colon specificity.

2. 发明授权

US06368629B1 Colon-specific drug release system 有权
标题翻译：结肠特异性药物释放系统
公开(公告)号：US06368629B1
公开(公告)日：2002-04-09
申请号：US09183339
申请日：1998-10-30
申请人： Shunsuke Watanabe , Hitoshi Kawai , Masataka Katsuma , Muneo Fukui
发明人： Shunsuke Watanabe , Hitoshi Kawai , Masataka Katsuma , Muneo Fukui
IPC分类号： A61K932
CPC分类号： A61K9/2886 , A61K9/2018 , A61K9/2826 , A61K9/2846 , A61K9/4808
摘要： A system for releasing a drug specifically in the colon of the gastrointestinal tract, which comprises a drug (b) coated with an organic acid-soluble polymer material (a), and a saccharide (c) which rapidly generates an organic acid by the action of enterobacteria in the lower part of the gastrointestinal tract; a colon-specific drug release oral preparation, which comprises a composition comprising a drug (b) coated with an organic acid-soluble polymer material (a) and a saccharide (c) which rapidly generates an organic acid by the action of enterobacteria in the lower part of the gastrointestinal tract, said composition being coated with an enteric coating polymer material (d). The invention provides a drug release system and a preparation which utilize enterobacteria, which do not form harmful substances due to the release-starting mechanism, show rapid degradation, and have higher colon specificity.
摘要翻译：一种用于特别在胃肠道结肠中释放药物的系统，其包括用有机酸溶性聚合物材料（a）涂覆的药物（b）和通过动作快速产生有机酸的糖（c）的胃肠道下部的肠细菌; 一种结肠特异性药物释放口服制剂，其包含包含有机酸溶性聚合物材料（a）的药物（b）和通过肠杆菌的作用快速产生有机酸的糖（c）的组合物所述组合物涂覆有肠溶衣聚合物材料（d）。本发明提供一种药物释放系统和利用肠杆菌的制剂，其不会由于释放启动机制而形成有害物质快速降解，并具有更高的结肠特异性。

3. 发明申请

US20050175689A1 Coated fine particles containing drug for intrabuccally fast disintegrating tablet 审中-公开
标题翻译：含有药物的包衣微粒含有快速崩解片剂
公开(公告)号：US20050175689A1
公开(公告)日：2005-08-11
申请号：US10975210
申请日：2004-10-27
申请人： Ippei Kurimoto , Yuki Kasashima , Hitoshi Kawai , Yuuki Takaishi , Masataka Katsuma , Hiroshi Ohi , Takayuki Yoshida , Hiroaki Tasaki
发明人： Ippei Kurimoto , Yuki Kasashima , Hitoshi Kawai , Yuuki Takaishi , Masataka Katsuma , Hiroshi Ohi , Takayuki Yoshida , Hiroaki Tasaki
IPC分类号： A61K9/14 , A61K9/20
CPC分类号： A61K9/0056 , A61K9/2081
摘要： The present invention makes it possible to provide drug-containing coated microparticles for quick-disintegrating oral tablets wherein microparticles containing a drug with an unpleasant taste are coated with a film composed of (1) a pH-independent water-insoluble polymer accounting for 60% or more but less than 80% of the film and (2) a pH-independent water-soluble substance accounting for more than 20% to 40% or less of the film, these microparticles being characterized in that the rate of dissolution of the drug from the drug-containing microparticles is 0% to 10% in one minute and 80% to 100% in 30 minutes, and the average particle diameter is 350 μm or less, in order to realize sufficient control of oral drug dissolution and fast gastrointestinal drug dissolution.
摘要翻译：本发明使得可以提供用于快速崩解口服片剂的药物包衣微粒，其中含有具有令人不快的味道的药物的微粒被包被（1）不含pH的水不溶性聚合物占60％或更多但小于80％的膜，（2）占pH超过20％至40％以下的pH不依赖性水溶性物质，这些微粒的特征在于药物的溶解速率含药微粒在1分钟内为0％〜10％，30分钟为80％〜100％，平均粒径为350μm以下，为了实现口服药物溶解和快速胃肠药物的充分控制溶解

4. 发明授权

US06328979B1 Sustained release medicinal compositions 失效
标题翻译：缓释药物组合物
公开(公告)号：US06328979B1
公开(公告)日：2001-12-11
申请号：US09582384
申请日：2000-06-23
申请人： Noboru Yamashita , Akira Takagi , Masataka Katsuma , Katsumi Saito , Yuuki Takaishi , Tatsuo Yasuda , Yutaka Takahashi , Mitsuo Mitomi
发明人： Noboru Yamashita , Akira Takagi , Masataka Katsuma , Katsumi Saito , Yuuki Takaishi , Tatsuo Yasuda , Yutaka Takahashi , Mitsuo Mitomi
IPC分类号： A61K900
CPC分类号： A61K9/0024 , A61K9/0019 , A61K9/06 , A61K31/557 , A61K31/5575 , A61K31/5585 , A61K47/10 , A61K47/12 , A61K47/14 , A61K47/186 , A61K47/20 , A61K47/36 , A61K47/42 , A61K47/44
摘要： The present invention relates to sustained-release pharmaceutical compositions for ionic pharmaceutically active substances (excluding ionic prostanoic acid derivatives) containing ionic compounds having opposite charges to those of the active substances and increasing hydrophobicity of the active substances. More specifically, the invention relates to sustained-release pharmaceutical compositions comprising the ionic pharmaceutically active substances and the ionic compounds having opposite charges to those of the active substances and increasing hydrophobicity of the active substances that contain hydrophobic groups in the molecule thereof. The pharmaceutical composition of the invention can exhibit excellent sustained release effect of the active substance, irrespective of water solubility possessed by the ionic pharmaceutically active substances.
摘要翻译：本发明涉及含有与活性物质具有相反电荷的离子化合物的离子药物活性物质（不含离子前列腺酸衍生物）的持续释放药物组合物，并且活性物质的疏水性增加。更具体地，本发明涉及包含离子药物活性物质和具有与活性物质相反的电荷的离子化合物的缓释药物组合物，并且其分子中含有疏水基团的活性物质的疏水性增加。本发明的药物组合物可以表现出优异的活性物质的缓释作用，而与离子药物活性物质所具有的水溶性无关。

5. 发明授权

US09050249B2 Oral pharmaceutical compositions in timed-release particle form and fast-disintegrating tablets containing this composition 有权
标题翻译：定时释放颗粒形式的口服药物组合物和含有该组合物的快速崩解片剂
公开(公告)号：US09050249B2
公开(公告)日：2015-06-09
申请号：US11119460
申请日：2005-04-28
申请人： Takayuki Yoshida , Hiroaki Tasaki , Masataka Katsuma , Atsushi Maeda
发明人： Takayuki Yoshida , Hiroaki Tasaki , Masataka Katsuma , Atsushi Maeda
IPC分类号： A61K9/16 , A61K31/135 , A61K47/02 , A61K47/04 , A61K47/10 , A61K47/12 , A61K47/18 , A61K47/24 , A61K47/26 , A61K47/32 , A61K47/34 , A61K47/36 , A61K47/38 , A61K47/40 , A61K47/42 , A61K9/00 , A61K9/20 , A61K9/50
CPC分类号： A61K9/0056 , A61K9/2077 , A61K9/2081 , A61K9/2095 , A61K9/501 , A61K9/5015 , A61K9/5026 , A61K9/5042 , A61K9/5047 , A61K9/5078 , A61K31/135
摘要： The present invention relates to an oral pharmaceutical composition in particle form, which comprises particles that contain a drug at the core of the pharmaceutical composition in particle form; a middle layer that contains two types of water-soluble components, an insolubilizer and an insolubilizing substance; and an outer layer for controlling water penetration that contains a water-insoluble substance. The present invention makes it possible to provide a pharmaceutical composition in particle form for oral use with which initial drug release is suppressed, the drug is quickly released thereafter, and lag time can be controlled as needed, and fast-disintegrating tablets containing this composition.
摘要翻译：本发明涉及一种颗粒形式的口服药物组合物，其包含以粒子形式含有药物组合物核心的药物的颗粒; 含有两种水溶性组分的中间层，不溶物和不溶物质; 以及用于控制含水不溶性物质的水渗透的外层。本发明使得可以提供一种用于口服使用的颗粒形式的药物组合物，其中抑制初始药物释放，此后快速释放药物，并且可以根据需要控制滞后时间，以及含有该组合物的快速崩解片剂。

6. 发明申请

US20050287211A1 Oral pharmaceutical compositions in timed-release particle form and fast-disintegrating tablets containing this composition 有权
标题翻译：定时释放颗粒形式的口服药物组合物和含有该组合物的快速崩解片剂
公开(公告)号：US20050287211A1
公开(公告)日：2005-12-29
申请号：US11119460
申请日：2005-04-28
申请人： Takayuki Yoshida , Hiroaki Tasaki , Masataka Katsuma , Atsushi Maeda
发明人： Takayuki Yoshida , Hiroaki Tasaki , Masataka Katsuma , Atsushi Maeda
IPC分类号： A61K9/00 , A61K9/16 , A61K9/20 , A61K9/26 , A61K9/50 , A61K31/135 , A61K47/02 , A61K47/04 , A61K47/10 , A61K47/12 , A61K47/18 , A61K47/24 , A61K47/26 , A61K47/32 , A61K47/34 , A61K47/36 , A61K47/38 , A61K47/40 , A61K47/42
CPC分类号： A61K9/0056 , A61K9/2077 , A61K9/2081 , A61K9/2095 , A61K9/501 , A61K9/5015 , A61K9/5026 , A61K9/5042 , A61K9/5047 , A61K9/5078 , A61K31/135
摘要： The present invention relates to an oral pharmaceutical composition in particle form, which comprises particles that contain a drug at the core of the pharmaceutical composition in particle form; a middle layer that contains two types of water-soluble components, an insolubilizer and an insolubilizing substance; and an outer layer for controlling water penetration that contains a water-insoluble substance. The present invention makes it possible to provide a pharmaceutical composition in particle form for oral use with which initial drug release is suppressed, the drug is quickly released thereafter, and lag time can be controlled as needed, and fast-disintegrating tablets containing this composition.
摘要翻译：本发明涉及一种颗粒形式的口服药物组合物，其包含以粒子形式含有药物组合物核心的药物的颗粒; 含有两种水溶性组分的中间层，不溶物和不溶物质; 以及用于控制含水不溶性物质的水渗透的外层。本发明使得可以提供一种用于口服使用的颗粒形式的药物组合物，其中抑制初始药物释放，此后快速释放药物，并且可以根据需要控制滞后时间，以及含有该组合物的快速崩解片剂。

7. 发明申请

US20050181031A1 Solifenacin transdermal preparation and method for enhancing transdermal permeation thereof 审中-公开
标题翻译：索非那新透皮制剂及其透皮渗透增强方法
公开(公告)号：US20050181031A1
公开(公告)日：2005-08-18
申请号：US11061858
申请日：2005-02-18
申请人： Katsumi Saito , Masataka Katsuma
发明人： Katsumi Saito , Masataka Katsuma
IPC分类号： A61K9/70 , A61K31/439 , A61K31/4745 , A61K47/08 , A61K47/10 , A61K47/14 , A61K47/26 , A61P11/00 , A61P13/00 , A61L15/16
CPC分类号： A61K31/4745
摘要： The transdermal permeable property of solifenacin or a salt thereof as a biologically active substance, is remarkably improved using a fatty acid ester, a terpene or the like as a selected transdermal permeable promoter. The difference in effect exceeded expectations by producing an enhancement in permeability that represents an increase of several hundredfold at most, and several tenfold for practical application, enabling the provision of extremely useful means for preventive and therapeutic agents for urologic diseases or respiratory diseases that use solifenacin.
摘要翻译：作为生物活性物质的索非那新或其盐的透皮渗透性，使用脂肪酸酯，萜烯等作为选择的透皮可渗透促进剂显着改善。通过产生渗透性的增加，其渗透性的增加最多增加了几百倍，实际应用的几十倍，使得能够为使用索非那新的泌尿系统疾病或呼吸系统疾病的预防和治疗剂提供极其有用的手段。

8. 发明授权

US06919372B1 Sustained release pharmaceutical compositions 失效
标题翻译：持续释放药物组合物
公开(公告)号：US06919372B1
公开(公告)日：2005-07-19
申请号：US09582404
申请日：1998-12-25
申请人： Noboru Yamashita , Akira Takagi , Masataka Katsuma , Katsumi Saito , Yuuki Takaishi , Tatsuo Yasuda , Yutaka Takahashi , Mitsuo Mitomi , Michio Hara
发明人： Noboru Yamashita , Akira Takagi , Masataka Katsuma , Katsumi Saito , Yuuki Takaishi , Tatsuo Yasuda , Yutaka Takahashi , Mitsuo Mitomi , Michio Hara
IPC分类号： A61K9/00 , A61K9/06 , A61K31/557 , A61K31/5575 , A61K31/5585 , A61K47/10 , A61K47/12 , A61K47/14 , A61K47/18 , A61K47/20 , A61K47/36 , A61K47/42 , A61K47/44 , A01N43/08 , A61K31/34
CPC分类号： A61K9/0024 , A61K9/0019 , A61K9/06 , A61K31/557 , A61K31/5575 , A61K31/5585 , A61K47/10 , A61K47/12 , A61K47/14 , A61K47/186 , A61K47/20 , A61K47/36 , A61K47/42 , A61K47/44
摘要： The present invention relates to sustained-release pharmaceutical compositions for ionic pharmaceutically active substances containing ionic compounds having opposite charges to those of ionic prostanoic acid derivatives and increasing hydrophobicity of the active substances. More specifically, the invention relates to sustained-release pharmaceutical compositions comprising the ionic prostanoic acid derivatives and the ionic compounds having opposite charges to those of the prostanoic acid derivatives and increasing hydrophobicity of these derivatives that contain hydrophobic groups in the molecule thereof.The pharmaceutical composition of the invention can exhibit excellent sustained release effect of the ionic prostanoic acid derivatives, irrespective of water solubility possessed by the ionic prostanoic acid derivatives.
摘要翻译：本发明涉及含离子化合物的离子药物活性物质的缓释药物组合物，其具有与离子前列腺酸衍生物相反的电荷并增加活性物质的疏水性。更具体地，本发明涉及包含离子前列腺酸衍生物和具有与前列腺酸衍生物相反电荷的离子化合物的缓释药物组合物，并且在其分子中含有疏水基团的这些衍生物的疏水性增加。本发明的药物组合物可以表现出优异的离子前列腺酸衍生物的缓释作用，而与离子前列腺酸衍生物具有的水溶性无关。

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