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1. 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

2. 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。

3. 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。

4. 发明申请

US20110236436A1 PHARMACEUTICAL COMPOSITION FOR MODIFIED RELEASE 有权
标题翻译：用于改性释放的药物组合物
公开(公告)号：US20110236436A1
公开(公告)日：2011-09-29
申请号：US13073677
申请日：2011-03-28
申请人： Yuuki Takaishi , Soichiro Nakamura
发明人： Yuuki Takaishi , Soichiro Nakamura
IPC分类号： A61K9/00 , A61K31/426 , A61P1/00 , A61P3/00 , A61P3/04 , A61P3/06 , A61P13/00 , A61P13/10 , A61P3/10
CPC分类号： A61K9/2031 , A61K9/0004 , A61K9/205 , A61K9/2054 , A61K9/2086 , A61K9/2846 , A61K31/426
摘要： A pharmaceutical composition for modified release comprising (R)-2-(2-aminothiazol-4-yl)-4′-[2-[(2-hydroxy-2-phenylethyl)amino]ethyl]acetic acid anilide or a pharmaceutically acceptable salt thereof, and a carrier for a sustained release pharmaceutical composition, wherein a dissolution rate of the drug from the composition is less than 85% after 30 minutes from the beginning of a dissolution test, is disclosed.
摘要翻译：包含（R）-2-（2-氨基噻唑-4-基）-4' - [2 - [（2-羟基-2-苯基乙基）氨基]乙基]乙酸酰苯胺或其药学上可接受的盐，以及缓释药物组合物用载体，其中，从溶出试验开始30分钟后，药物从组合物中的溶出速度小于85％。

5. 发明申请

US20100144807A1 PHARMACEUTICAL COMPOSITION FOR MODIFIED RELEASE 审中-公开
标题翻译：用于改性释放的药物组合物
公开(公告)号：US20100144807A1
公开(公告)日：2010-06-10
申请号：US12568313
申请日：2009-09-28
申请人： Yuuki Takaishi , Yutaka Takahashi , Takashi Nishizato , Daisuke Murayama , Emiko Murayama , Soichiro Nakamura , Kazuhiro Sako
发明人： Yuuki Takaishi , Yutaka Takahashi , Takashi Nishizato , Daisuke Murayama , Emiko Murayama , Soichiro Nakamura , Kazuhiro Sako
IPC分类号： A61K31/426 , A61P3/08
CPC分类号： A61K31/426 , A61K9/2009 , A61K9/2013 , A61K9/2031 , A61K9/2054 , A61K9/2095 , A61K9/2853 , A61K9/2866
摘要： A pharmaceutical composition for modified release, comprising (1) (R)-2-(2-aminothiazol-4-yl)-4′-[2-[(2-hydroxy-2-phenylethyl)amino]ethyl]acetic acid anilide, or a pharmaceutically acceptable salt thereof, (2) at least one additive which ensures penetration of water into the pharmaceutical composition and which has a solubility such that the volume of water required for dissolving 1 g of the additive is 5 mL or less, and (3) a hydrogel-forming polymer having an average molecular weight of approximately 100,000 or more, or a viscosity of 12 mPa·s or more at a 5% aqueous solution at 25° C. is disclosed.
摘要翻译：一种用于改性释放的药物组合物，其包含（1）（R）-2-（2-氨基噻唑-4-基）-4' - [2 - [（2-羟基-2-苯乙基）氨基]乙基]乙酰苯胺，或其药学上可接受的盐，（2）至少一种添加剂，其确保水渗透到药物组合物中并且具有使得溶解1g添加剂所需的水的体积为5mL或更小的溶解度，（3）公开了在25℃下5％水溶液下的平均分子量为约100,000以上或粘度为12mPa·s以上的水凝胶形成性聚合物。

6. 发明申请

US20050100599A1 Quick disintegrating tablet in buccal cavity and manufacturing method thereof 审中-公开
公开(公告)号：US20050100599A1
公开(公告)日：2005-05-12
申请号：US11009644
申请日：2004-12-09
申请人： Yuuki Takaishi , Takao Mizumoto , Yoshinori Masuda
发明人： Yuuki Takaishi , Takao Mizumoto , Yoshinori Masuda
IPC分类号： A61K9/00 , A61K9/20 , A61K9/14
CPC分类号： A61K9/0056
摘要： The present invention relates to a quick-disintegrating tablet in the buccal cavity comprising a drug, a diluent, and a saccharide with a relatively lower melting point than the drug and the diluent, which is obtained by uniformly mixing the saccharide with a low melting point in the tablet so that a bridge will be formed between said drug and/or said diluent particles by the product of melting and then solidification of this saccharide with a low melting point. Moreover, the present invention relates to a method of manufacturing a quick-disintegrating tablet in the buccal cavity comprising a drug, a diluent and a saccharide with a relatively lower melting point than the drug and the diluent, which comprises (a) the process whereby tablet starting materials including a drug, a diluent, and a saccharide with a relatively lower melting point than the drug and the diluent are molded under the low pressure necessary for retaining the shape of a tablet, (b) the process whereby the molded product obtained in process (a) is heated to at least the temperature at which this saccharide with a low melting point will melt, and (c) the process whereby the molded product obtained in process (b) is cooled to at least the temperature at which the molten saccharide with a low melting point solidifies. The present invention presents a quick-disintegrating tablet in the buccal cavity that can be used for practical purposes in that it has almost the same properties as conventional oral pharmaceutical tablets, that is, it has sufficient tablet strength that it can be used with automatic unit dosing machines, and it is produced by conventional tableting machines, and a manufacturing method thereof. Moreover, the present invention presents a quick-disintegrating tablet in the buccal cavity which, in comparison to conventional quick-disintegrating tablets in the buccal cavity, has increased tablet strength and an improved friability without prolonging the disintegration time in the buccal cavity, and a manufacturing method thereof.

7. 发明申请

US20070202168A1 COMPOSITION COMPRISES SUSTAINED-RELEASE FINE PARTICLES AND MANUFACTURING METHOD THEREOF 失效
标题翻译：组合物包含持续释放的细颗粒及其制造方法
公开(公告)号：US20070202168A1
公开(公告)日：2007-08-30
申请号：US11743616
申请日：2007-05-02
申请人： Tatsuki Shinoda , Atsushi Maeda , Naoki Itou , Takao Mizumoto , Shigeru Yamazaki , Yuuki Takaishi
发明人： Tatsuki Shinoda , Atsushi Maeda , Naoki Itou , Takao Mizumoto , Shigeru Yamazaki , Yuuki Takaishi
IPC分类号： A61K9/26
CPC分类号： A61K9/2081 , A61K9/0056 , A61K9/2018 , A61K9/5026 , A61K31/18
摘要： The present invention relates to a composition comprising sustained-release fine particles, characterized in that it contains sustained-release fine particles that can be used in quick-disintegrating tablets in the buccal cavity, one or more fillers selected from the group consisting of sugars or sugar alcohols, and one or more binders for quick-disintegrating tablets in the buccal cavity selected from the group consisting of sugars of high moldability and water-soluble polymer substances, and in that the sustained-release fine particles are granulated with filler and binder for quick-disintegrating tablets in the buccal cavity, and a manufacturing method thereof.
摘要翻译：本发明涉及包含持续释放微粒的组合物，其特征在于其含有可用于颊腔中快速崩解片剂的缓释微粒，一种或多种选自以下的填料：糖或糖醇和一种或多种选自高成型性糖和水溶性聚合物物质的颊腔中的快速崩解片的粘合剂，并且缓释微粒用填料和粘合剂造粒，颊腔中的快速崩解片及其制造方法。

8. 发明授权

US06872405B2 Quick-disintegrating tablet in buccal cavity and manufacturing method thereof 失效
公开(公告)号：US06872405B2
公开(公告)日：2005-03-29
申请号：US10142081
申请日：2002-05-08
申请人： Yuuki Takaishi , Takao Mizumoto , Yoshinori Masuda
发明人： Yuuki Takaishi , Takao Mizumoto , Yoshinori Masuda
IPC分类号： A61K9/00 , A61K9/20
CPC分类号： A61K9/0056
摘要： The present invention relates to a quick-disintegrating tablet in the buccal cavity comprising a drug, a diluent, and a saccharide with a relatively lower melting point than the drug and the diluent, which is obtained by uniformly mixing the saccharide with a low melting point in the tablet so that a bridge will be formed between said drug and/or said diluent particles by the product of melting and then solidification of this saccharide with a low melting point. Moreover, the present invention relates to a method of manufacturing a quick-disintegrating tablet in the buccal cavity comprising a drug, a diluent and a saccharide with a relatively lower melting point than the drug and the diluent, which comprises (a) the process whereby tablet starting materials including a drug, a diluent, and a saccharide with a relatively lower melting point than the drug and the diluent are molded under the low pressure necessary for retaining the shape of a tablet, (b) the process whereby the molded product obtained in process (a) is heated to at least the temperature at which this saccharide with a low melting point will melt, and (c) the process whereby the molded product obtained in process (b) is cooled to at least the temperature at which the molten saccharide with a low melting point solidifies. The present invention presents a quick-disintegrating tablet in the buccal cavity that can be used for practical purposes in that it has almost the same properties as conventional oral pharmaceutical tablets, that is, it has sufficient tablet strength that it can be used with automatic unit dosing machines, and it is produced by conventional tableting machines, and a manufacturing method thereof. Moreover, the present invention presents a quick-disintegrating tablet in the buccal cavity which, in comparison to conventional quick-disintegrating tablets in the buccal cavity, has increased tablet strength and an improved friability without prolonging the disintegration time in the buccal cavity, and a manufacturing method thereof.

9. 发明授权

US08877214B2 Pharmaceutical composition for modified release 有权
标题翻译：用于改性释放的药物组合物
公开(公告)号：US08877214B2
公开(公告)日：2014-11-04
申请号：US13073677
申请日：2011-03-28
申请人： Yuuki Takaishi , Soichiro Nakamura
发明人： Yuuki Takaishi , Soichiro Nakamura
IPC分类号： A61K31/426 , A61P13/10 , A61P1/00 , A61P3/04 , A61P3/06 , A61P3/00 , A61P13/00 , A61K9/00 , A61P3/10 , A61K9/20 , A61K9/28
CPC分类号： A61K9/2031 , A61K9/0004 , A61K9/205 , A61K9/2054 , A61K9/2086 , A61K9/2846 , A61K31/426
摘要： A pharmaceutical composition for modified release comprising (R)-2-(2-aminothiazol-4-yl)-4′-[2-[(2-hydroxy-2-phenylethyl)amino]ethyl]acetic acid anilide or a pharmaceutically acceptable salt thereof, and a carrier for a sustained release pharmaceutical composition, wherein a dissolution rate of the drug from the composition is less than 85% after 30 minutes from the beginning of a dissolution test, is disclosed.
摘要翻译：包含（R）-2-（2-氨基噻唑-4-基）-4' - [2 - [（2-羟基-2-苯基乙基）氨基]乙基]乙酸酰苯胺或其药学上可接受的盐，以及缓释药物组合物用载体，其中，从溶出试验开始30分钟后，药物从组合物中的溶出速度小于85％。

10. 发明申请

US20120070465A1 PHARMACEUTICAL COMPOSITION FOR MODIFIED RELEASE 审中-公开
标题翻译：用于改性释放的药物组合物
公开(公告)号：US20120070465A1
公开(公告)日：2012-03-22
申请号：US13073721
申请日：2011-03-28
申请人： Yuuki Takaishi , Soichiro Nakamura , Yutaka Takahashi
发明人： Yuuki Takaishi , Soichiro Nakamura , Yutaka Takahashi
IPC分类号： A61K9/00 , A61K31/426
CPC分类号： A61K31/426 , A61K9/0004 , A61K9/1652 , A61K9/2031 , A61K9/205 , A61K9/2054 , A61K9/2072 , A61K9/2086 , A61K9/2846 , A61K9/2866 , A61K47/36
摘要： A pharmaceutical composition for modified release comprising (R)-2-(2-aminothiazol-4-yl)-4′-[2-[(2-hydroxy-2-phenylethyl)amino]ethyl]acetic acid anilide or a pharmaceutically acceptable salt thereof, and a carrier for a sustained release pharmaceutical composition, wherein a maximum blood drug concentration (Cmax) when administered in a fasted state is 400 ng/mL or less, is disclosed.
摘要翻译：包含（R）-2-（2-氨基噻唑-4-基）-4' - [2 - [（2-羟基-2-苯基乙基）氨基]乙基]乙酸酰苯胺或其药学上可接受的盐，以及缓释药物组合物的载体，其中以禁食状态施用时的最大血药浓度（C max）为400ng / mL以下。

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