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1. 发明授权

US5154929A Percutaneous absorption type preparation and process for preparing the same 失效
标题翻译：经皮吸收型制剂及其制备方法
公开(公告)号：US5154929A
公开(公告)日：1992-10-13
申请号：US740662
申请日：1991-08-02
申请人： Keisuke Shibata , Yuusuke Ito , Saburo Otsuka , Shoichi Tokuda , Takashi Kinoshita
发明人： Keisuke Shibata , Yuusuke Ito , Saburo Otsuka , Shoichi Tokuda , Takashi Kinoshita
IPC分类号： A61K9/70
CPC分类号： A61K9/7061
摘要： A percutaneous absorption type preparation and a process for preparing the same are disclosed. The preparation comprises a substantially drug-impermeable backing having provided thereon an adhesive layer comprising a pressure-sensitive adhesive containing therein a percutaneous absorption type drug (solid at room temperature) in an amount greater than the saturated solubility in the adhesive, wherein the excess amount of the drug greater than the saturated solubility is present in the adhesive in a continuous recrystallized state and a substantially network state.
摘要翻译：公开了一种经皮吸收型制剂及其制备方法。该制剂包括基本上不透液的背衬，其上设置有粘合剂层，所述粘合剂层包含其中含有大于在粘合剂中的饱和溶解度的量的经皮吸收型药物（室温下为固体）的压敏粘合剂，其中过量大于饱和溶解度的药物以连续重结晶状态和基本上网络状态存在于粘合剂中。

2. 发明授权

US4765974A Preparation for percutaneous administration 失效
标题翻译：经皮给药制剂
公开(公告)号：US4765974A
公开(公告)日：1988-08-23
申请号：US48977
申请日：1987-05-13
申请人： Shoichi Tokuda , Yuusuke Ito , Saburo Otsuka , Takashi Kinoshita
发明人： Shoichi Tokuda , Yuusuke Ito , Saburo Otsuka , Takashi Kinoshita
IPC分类号： A61K9/00 , A61K31/415 , A61K47/32 , A61K9/70 , A61F13/02 , A61L15/03
CPC分类号： A61K31/415 , A61K47/32 , A61K9/0014
摘要： A clonidine preparation for percutaneous administration comprising a support having provided thereon an active ingredient-containing layer is disclosed. The active ingredient-containing layer contains an acrylic polymer having a glass transition temperature of from -70.degree. C. to -10.degree. C. and pressure-sensitive adhesion at room temperature as a base, at least one of clonidine and clonidine hydrochloride as an active ingredient, and a decomposition inhibitor. The active ingredient can be stably maintained within the preparation without being decomposed, and, therefore, can be effectively released over a prolonged period of time.
摘要翻译：公开了一种用于经皮给药的可乐定制剂，其包含其上提供有活性成分的层的载体。活性成分含有层含有玻璃化转变温度为-70℃〜-10℃的丙烯酸类聚合物，作为碱的室温下的压敏粘合剂，可乐定和可乐定盐酸盐中的至少一种作为活性成分和分解抑制剂。活性成分可以稳定地保持在制剂中而不被分解，因此可以在更长的时间内有效释放。

3. 发明授权

US4719226A Percutaneous absorption type preparation and process for preparing the same 失效
标题翻译：经皮吸收型制剂及其制备方法
公开(公告)号：US4719226A
公开(公告)日：1988-01-12
申请号：US687898
申请日：1984-12-31
申请人： Saburo Otsuka , Yuusuke Ito , Shoichi Tokuda , Takashi Kinoshita , Keisuke Shibata
发明人： Saburo Otsuka , Yuusuke Ito , Shoichi Tokuda , Takashi Kinoshita , Keisuke Shibata
IPC分类号： A61K9/22 , A61K9/32 , A61K9/70 , A61F13/00 , A61F13/02
CPC分类号： A61K9/7061 , A61K9/7069
摘要： A percutaneous absorption type preparation and a process for preparing the same, where the preparation comprises a backing readily conformable to the skin or mucosa and substantially impermeable to a drug absorbed through the skin or mucosa, and an adhesive layer provided on a backing, where the adhesive layer comprises a polymer which is pressure-adhesive at room temperature and the drug present in the polymer, wherein the amount of the drug present in the adhesive layer is greater than its saturated solubility in the polymer is dispersed in the polymer in the form of recrystallized fine particles. The excess portion is again dissolved in the polymer when the drug is consumed as the result of absorption through the skin or mucosa. The drug is released continuously over a long period of time.
摘要翻译：经皮吸收型制剂及其制备方法，其中所述制剂包含易于与皮肤或粘膜相适应并且对通过皮肤或粘膜吸收的药物基本上不可渗透的背衬以及设置在背衬上的粘合剂层，其中粘合剂层包括在室温下是压敏粘合剂和存在于聚合物中的药物的聚合物，其中存在于粘合剂层中的药物的量大于其在聚合物中的饱和溶解度，以聚合物的形式分散在聚合物中再结晶的细颗粒。当药物被吸收通过皮肤或粘膜消耗时，过量部分再次溶解在聚合物中。药物长期不间断地释放。

4. 发明授权

US5175052A Adhesive tape preparation of clonidine 失效
标题翻译：可乐定胶带的制备
公开(公告)号：US5175052A
公开(公告)日：1992-12-29
申请号：US790081
申请日：1991-11-13
申请人： Shoichi Tokuda , Saburo Otsuka , Yuusuke Ito
发明人： Shoichi Tokuda , Saburo Otsuka , Yuusuke Ito
IPC分类号： A61K9/70 , A61K31/415 , A61L15/24 , A61L15/58
CPC分类号： A61K9/7053 , A61K31/415 , A61K9/7061 , A61L15/24 , A61L15/58 , Y10T428/28 , Y10T428/2891 , Y10T428/31544
摘要： An adhesive tape preparation of clonidine is disclosed, comprising a polytetrafluoroethylene porous sheet having an air permeability of from 10 to 500 seconds having thereon an active ingredient-containing layer comprising a pressure-sensitive adhesive obtained by copolymerizing a monomer mixture comprising from 40 to 80% by weight of 2-ethylhexyl acrylate, from 20 to 60% by weight of 2-methoxyethyl acrylate, and 0 to 40% by weight of vinyl acetate, the pressure-sensitive adhesive containing clonidine as an active ingredient. The preparation achieves sustained release of clonidine and exhibits long-term preservability while minimizing skin irritation and maintaining sufficient adhesion to the skin.
摘要翻译：公开了可乐定的胶带制剂，其包含具有10至500秒的透气性的聚四氟乙烯多孔片，其上含有含活性成分的层，所述活性成分含有层包含通过共聚单体混合物获得的压敏粘合剂，所述单体混合物包含40至80％的丙烯酸2-乙基己酯，20〜60重量％的丙烯酸2-甲氧基乙酯和0〜40重量％的乙酸乙烯酯，该压敏粘合剂含有可乐定作为活性成分。该制剂可持续释放可乐定，并显示出长期保存性，同时最大限度地减少皮肤刺激并保持与皮肤的充分粘附。

5. 发明授权

US4608249A Hydrophilic therapeutic material 失效
标题翻译：亲水治疗材料
公开(公告)号：US4608249A
公开(公告)日：1986-08-26
申请号：US438422
申请日：1982-11-02
申请人： Saburo Otsuka , Toshiyuki Yoshikawa , Shoichi Tokuda , Yuusuke Ito
发明人： Saburo Otsuka , Toshiyuki Yoshikawa , Shoichi Tokuda , Yuusuke Ito
IPC分类号： A61K9/70 , A61L15/03 , A61K31/79 , C08F220/12
CPC分类号： A61K9/7053 , A61K9/7061
摘要： A hydrophilic therapeutic material comprising a carrier and a drug-containing patching layer formed thereon directly or indirectly, wherein said patching layer comprises a copolymer of 5 to 75% by weight of an acrylic or methacrylic ester having an ether group in the molecule, 85 to 15% by weight of an alkyl acrylate or alkyl methacrylate and 10 to 50% by weight of a polar monomer copolymerizable therewith.
摘要翻译：一种亲水治疗材料，其包含直接或间接形成于其上的载体和含药剂的修补层，其中所述修补层包含5至75重量％的在分子中具有醚基的丙烯酸或甲基丙烯酸酯的共聚物，85至 15重量％的丙烯酸烷基酯或甲基丙烯酸烷基酯和10〜50重量％的与其共聚的极性单体。

6. 发明授权

US5151271A Pressure-sensitively adhering composite medicinal preparation 失效
标题翻译：压力敏感的复合药物制剂
公开(公告)号：US5151271A
公开(公告)日：1992-09-29
申请号：US426526
申请日：1989-10-24
申请人： Saburo Otsuka , Yuusuke Ito , Toshiyuki Yoshikawa , Shoichi Tokuda
发明人： Saburo Otsuka , Yuusuke Ito , Toshiyuki Yoshikawa , Shoichi Tokuda
IPC分类号： A61K9/70
CPC分类号： A61K9/7053 , A61K9/7061 , A61K9/7076 , A61K9/7084
摘要： A pressure-sensitively adhering multilayer medicinal preparation comprises a pressure-sensitively adhering macromolecular substance layer and a polymer layer adjacent thereto and the drug and adjuvant incorporated in said preparation each can migrate from the layer of its original incorporation into the other, said adjuvant being capable of increasing absorption of the drug. In such preparation, the drug amount per unit volume can be increased.
摘要翻译：压力敏感粘合性多层药物制剂包括压力敏感地粘附的大分子物质层和与其相邻的聚合物层，并且所述制剂中掺入的药物和佐剂各自可以从其原始掺入层迁移到另一个中，所述佐剂能够增加药物的吸收。在这样的制备中，可以增加每单位体积的药物量。

7. 发明授权

US4485087A Process for obtaining composite pharmaceutical preparation 失效
标题翻译：获得复合药物制剂的方法
公开(公告)号：US4485087A
公开(公告)日：1984-11-27
申请号：US357540
申请日：1982-03-12
申请人： Saburo Otsuka , Yuusuke Ito , Toshiyuki Yoshikawa , Shoichi Tokuda
发明人： Saburo Otsuka , Yuusuke Ito , Toshiyuki Yoshikawa , Shoichi Tokuda
IPC分类号： A61K9/70 , A61L15/03 , A61F13/00
CPC分类号： A61K9/7061
摘要： A process for obtaining a composite pharmaceutical preparation which comprises coating or laminating a composition comprising(a) an adhesive substance having a pressure-sensitive adhesive property at room temperature, and(b) a percutaneous absorption type medicine which is solid at 0.degree. C.onto a polymer film capable of allowing the medicine in contact therewith to migrate through the polymer film, the composition being prepared by adding the medicine to the adhesive substance in a higher concentration than the solubility thereof in the adhesive substance.
摘要翻译：一种获得复合药物制剂的方法，其包括涂覆或层压组合物，所述组合物包含（a）在室温下具有压敏粘合性质的粘合剂物质和（b）在0℃下为固体的经皮吸收型药物。能够使与其接触的药物通过聚合物膜迁移的聚合物膜，该组合物通过以高于其在粘合物质中的溶解度的浓度将该药物添加到粘合剂物质中来制备。

8. 发明授权

US4420470A Percutaneous absorption type pharmaceutical preparation of isosorbide dinitrate or pentaerythritol tetranitrate in pressure-sensitive laminate 失效
标题翻译：硝酸异山梨酯或季戊四醇四硝酸酯在压敏层压板中的经皮吸收型药物制剂
公开(公告)号：US4420470A
公开(公告)日：1983-12-13
申请号：US338190
申请日：1982-01-08
申请人： Saburo Otsuka , Toshiyuki Yoshikawa , Shoichi Tokuda , Yuuseke Ito
发明人： Saburo Otsuka , Toshiyuki Yoshikawa , Shoichi Tokuda , Yuuseke Ito
IPC分类号： A61K9/70 , A61K31/21 , A61P9/08 , A61P9/10 , A61L15/03 , A61F13/00
CPC分类号： A61K9/7053 , A61K9/7061 , A61K9/7076
摘要： A pharmaceutical preparation comprising a flexible backing and a base material provided thereon is described wherein the base material consists essentially of a polymer having a glass transition temperature of from -70.degree. C. to -10.degree. C. and exhibiting pressure-sensitivity at room temperature, and isosorbide dinitrate or pentaerythritol tetranitrate. This pharmaceutical preparation is applied to the skin, and permits the active ingredient to be absorbed through the skin into the body at a constant rate, and gradually over a long period of time.
摘要翻译：描述了一种包含柔性背衬和其上提供的基材的药物制剂，其中所述基材主要由玻璃化转变温度为-70℃至-10℃的聚合物组成，并且在室温下表现出压敏性，硝酸异山梨酯或季戊四醇四硝酸酯。这种药物制剂适用于皮肤，并且允许活性成分以恒定的速率通过皮肤吸收到体内，并且逐渐地长时间地吸收。

9. 发明授权

US5882675A Percutaneous absorption preparation 失效
标题翻译：经皮吸收制剂
公开(公告)号：US5882675A
公开(公告)日：1999-03-16
申请号：US812545
申请日：1997-03-07
申请人： Kazuhisa Ninomiya , Shoichi Tokuda , Yasuhiro Fukushima
发明人： Kazuhisa Ninomiya , Shoichi Tokuda , Yasuhiro Fukushima
IPC分类号： A61K9/00 , A61K9/70 , A61K47/14 , A61L15/44 , A61L15/58 , A61F13/02
CPC分类号： A61K9/7061 , A61K9/0014 , A61L15/58 , A61K47/14
摘要： The present invention provides a percutaneous absorption preparation which has excellent pressure-sensitive adhesive characteristics and exerts excellent percutaneous absorption property. A crosslinking agent is added to a solution of an acrylic copolymer prepared by copolymerizing a (meth)acrylic acid alkyl ester with a functional monomer, and the acrylic copolymer is partially crosslinked. A composition containing the crosslinked acrylic copolymer is pulverized to prepare a pressure-sensitive adhesive solution comprised of the acrylic copolymer containing crosslinked acrylic copolymer particles. Thereafter, a drug for percutaneous absorption use, a percutaneous penetration enhancer are added to the pressure-sensitive adhesive solution, thereby producing the percutaneous absorption preparation.
摘要翻译：本发明提供一种经皮吸收制剂，其具有优异的压敏粘合剂特性并且具有优异的经皮吸收性能。将交联剂加入通过使（甲基）丙烯酸烷基酯与官能单体共聚制备的丙烯酸共聚物的溶液中，并且丙烯酸共聚物部分交联。将含有交联的丙烯酸共聚物的组合物粉碎以制备由包含交联的丙烯酸共聚物颗粒的丙烯酸共聚物组成的压敏粘合剂溶液。此后，将经皮吸收用药物，经皮渗透促进剂加入到压敏粘合剂溶液中，从而制备经皮吸收制剂。

10. 发明授权

US5618555A Percutaneous absorption preparation 失效
标题翻译：经皮吸收制剂
公开(公告)号：US5618555A
公开(公告)日：1997-04-08
申请号：US430384
申请日：1995-04-28
申请人： Shoichi Tokuda , Kazuhisa Ninomiya , Yasuhiro Fukushima , Shigeyuki Watanabe , Mitsuru Ochiai , Mutsuo Okumura , Yuko Hosokawa
发明人： Shoichi Tokuda , Kazuhisa Ninomiya , Yasuhiro Fukushima , Shigeyuki Watanabe , Mitsuru Ochiai , Mutsuo Okumura , Yuko Hosokawa
IPC分类号： A61K9/00 , A61K9/70 , A61K31/485 , A61K47/14 , A61P25/04 , A61F13/00
CPC分类号： A61K9/7061 , A61K31/485 , A61K47/14 , A61K9/0014 , Y10S514/946
摘要： A percutaneous absorption preparation which is excellent in the skin penetration of a non-narcotic analgesic buprenorphine and can sustain a high blood level in a stable state over a long period of time is provided. The percutaneous absorption preparation for administrating buprenorphine hydrochloride and/or buprenorphine, which comprises a support having on one surface thereof a plaster layer containing a pressure-sensitive adhesive, buprenorphine hydrochloride and/or buprenorphine, and a penetration enhancer, wherein the penetration enhancer comprises a combination of a monoglyceride of a fatty acid having 6 to 8 carbon atoms and isopropyl myristate, and the plaster layer contains at least 10% by weight of a monoglyceride off fatty acid having 6 to 8 carbon atoms and at least 5% by weight off isopropyl myristate, with the proviso that the content of the whole penetration enhancer ranges from 25 to 50% by weight. The combined use of the fatty acid monoglyceride and isopropyl myristate as a penetration enhancer synergistically elevates skin penetration of buprenorphine hydrochloride and/or buprenorphine.
摘要翻译：提供了一种在非麻醉性止痛丁丙诺啡的皮肤渗透性优异并能够长期稳定地维持高血液水平的经皮吸收制剂。用于施用盐酸丁丙诺非和/或丁丙诺啡的经皮吸收制剂，其包含在其一个表面上具有含有压敏粘合剂，盐酸丁丙诺非和/或丁丙诺啡的膏药的支持物和渗透促进剂，其中所述渗透促进剂包含具有6至8个碳原子的脂肪酸的单酸甘油酯和肉豆蔻酸异丙酯的组合，所述膏药层含有至少10重量％的具有6至8个碳原子的单酸甘油酯脱脂肪酸和至少5重量％的异丙基肉豆蔻酸酯，条件是全部渗透促进剂的含量为25至50重量％。将脂肪酸单甘油酯和肉豆蔻酸异丙酯作为渗透促进剂的组合使用协同地提高了丁丙诺啡盐酸盐和/或丁丙诺啡的皮肤渗透。

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