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1. 发明申请

US20090220580A1 Percutaneous Absorption Formulation 审中-公开
标题翻译：经皮吸收制剂
公开(公告)号：US20090220580A1
公开(公告)日：2009-09-03
申请号：US11918133
申请日：2005-04-20
申请人： Kouji Kawahara , Yasuhiko Aramomi , Noriko Shimada , Akira Ohtori , Akiharu Isowaki
发明人： Kouji Kawahara , Yasuhiko Aramomi , Noriko Shimada , Akira Ohtori , Akiharu Isowaki
IPC分类号： A61K9/70 , A61K31/4535 , A61P11/06 , A61P17/00 , A61P11/00
CPC分类号： A61K31/4535 , A61K9/7053 , A61K9/7076 , A61K47/14
摘要： The present invention provides a percutaneous absorption formulation including a patch having an adhesive layer disposed on a substrate and the adhesive layer contains ketotifen fumarate and tris(hydroxymethyl)aminomethane, and the patch is packaged in a hygroscopic packaging material. In the percutaneous absorption formulation, tris(hydroxymethyl)aminomethane particularly selected from various basic substances is incorporated, and by packaging the patch in a hygroscopic packaging material, the percutaneous absorptivity and content stability of a drug can be simultaneously improved and the yellowing of the drug can be suppressed. These effects can be further improved by the incorporation of propyl gallate, the use of an adhesive layer including an SIS-based adhesive base and a rosin ester-based adhesion imparting resin, and/or the removal of oxygen from the atmosphere in the inside of the packaging material.
摘要翻译：本发明提供一种经皮吸收制剂，其包括具有设置在基底上的粘合剂层的贴剂，并且所述粘合剂层含有富马酸酮替芬和三（羟甲基）氨基甲烷，并且将该贴剂包装在吸湿性包装材料中。在经皮吸收制剂中，加入特别选自各种碱性物质的三（羟甲基）氨基甲烷，通过将吸收包装材料包装在吸湿包装材料中，药物的经皮吸收性和含量稳定性可以同时改善，药物变黄可以抑制。通过加入没食子酸丙酯可以进一步改善这些效果，使用包含基于SIS的粘合剂基质和基于松香酯的粘合赋予树脂的粘合层，和/或从内部的大气中除去氧包装材料。

2. 发明申请

US20100150992A1 Methods for Treatment of Ophthalmic Disease of an External Ophthalmic Tissue 审中-公开
标题翻译：治疗外眼科眼科疾病的方法
公开(公告)号：US20100150992A1
公开(公告)日：2010-06-17
申请号：US12712459
申请日：2010-02-25
申请人： Kohji Kawahara , Yasuhiko Aramomi , Akira Ohtori , Akiharu Isowaki
发明人： Kohji Kawahara , Yasuhiko Aramomi , Akira Ohtori , Akiharu Isowaki
IPC分类号： A61K9/70 , A61P27/02 , A61K31/4535 , A61K31/196
CPC分类号： A61K9/7053 , A61K9/0048 , A61K9/7076
摘要： A transdermal drug delivery system for treatment of ophthalmic diseases comprising a structure that a plaster layer containing a remedy for ophthalmic diseases is provided on a support, wherein the system is applied to a skin surface including a front surface of an eyelid to administer the remedy for ophthalmic diseases in the plaster layer to an ophthalmic topical tissue by percutaneous permeation substantially without being administered through a systemic blood flow. Use of the transdermal drug delivery system for treatment of ophthalmic diseases, comprising applying the transdermal drug delivery system to a skin surface including a front surface of an eyelid to transfer the remedy for ophthalmic diseases in the plaster layer to an ophthalmic topical tissue by percutaneous permeation substantially without being administered through a systemic blood flow, and a method for transferring the remedy for ophthalmic diseases to the ophthalmic topical tissue.
摘要翻译：一种用于治疗眼科疾病的透皮药物递送系统，包括在载体上设置含有用于眼科疾病补救剂的膏药层的结构，其中将该系统施用于包括眼睑前表面的皮肤表面，石膏层中的眼科疾病通过经皮渗透到眼部局部组织，基本上不经由全身血流量施用。使用透皮药物递送系统来治疗眼科疾病，包括将透皮药物递送系统施用于包括眼睑前表面的皮肤表面，以通过经皮渗透将膏药层中的眼科疾病的药物转移至眼用局部组织基本上不经由全身血流量施用，以及用于将眼科疾病的药物转移到眼用局部组织的方法。

3. 发明申请

US20060036220A1 Percutaneous absorption preparation for treating ophthalmic disease, use thereof and method for migration of ophthalmic remedy into topical tissue in eye 审中-公开
标题翻译：用于治疗眼科疾病的经皮吸收制剂，其用途和眼科药物转移到眼睛局部组织中的方法
公开(公告)号：US20060036220A1
公开(公告)日：2006-02-16
申请号：US10540835
申请日：2004-01-22
申请人： Kohji Kawahara , Yasuhiko Aramomi , Akira Ohtori , Akiharu Isowaki
发明人： Kohji Kawahara , Yasuhiko Aramomi , Akira Ohtori , Akiharu Isowaki
IPC分类号： A61M35/00
CPC分类号： A61K9/7053 , A61K9/0048 , A61K9/7076
摘要： A transdermal drug delivery system for treatment of ophthalmic diseases comprising a structure that a plaster layer containing a remedy for ophthalmic diseases is provided on a support, wherein the system is applied to a skin surface including a front surface of an eyelid to administer the remedy for ophthalmic diseases in the plaster layer to an ophthalmic topical tissue by percutaneous permeation substantially without being administered through a systemic blood flow. Use of the transdermal drug delivery system for treatment of ophthalmic diseases, comprising applying the transdermal drug delivery system to a skin surface including a front surface of an eyelid to transfer the remedy for ophthalmic diseases in the plaster layer to an ophthalmic topical tissue by percutaneous permeation substantially without being administered through a systemic blood flow, and a method for transferring the remedy for ophthalmic diseases to the ophthalmic topical tissue.
摘要翻译：一种用于治疗眼科疾病的透皮药物递送系统，包括在载体上设置含有用于眼科疾病补救剂的膏药层的结构，其中将该系统施用于包括眼睑前表面的皮肤表面，石膏层中的眼科疾病通过经皮渗透到眼部局部组织，基本上不经由全身血流量施用。使用透皮药物递送系统来治疗眼科疾病，包括将透皮药物递送系统施用于包括眼睑前表面的皮肤表面，以通过经皮渗透将膏药层中的眼科疾病的药物转移至眼用局部组织基本上不经由全身血流量施用，以及用于将眼科疾病的药物转移到眼用局部组织的方法。

4. 发明申请

US20070053964A1 Ophthalmic percutaneously absorbed preparation containing muscarinic receptor agonist 审中-公开
标题翻译：含有毒蕈碱受体激动剂的眼科经皮吸收制剂
公开(公告)号：US20070053964A1
公开(公告)日：2007-03-08
申请号：US10569772
申请日：2005-05-20
申请人： Akiharu Isowaki , Akira Ohtori
发明人： Akiharu Isowaki , Akira Ohtori
IPC分类号： A61K31/4178 , A61F13/02
CPC分类号： A61K31/4178 , A61K9/0048 , A61K31/439
摘要： A percutaneous absorption type ophthalmic preparation comprising muscarinic receptor agonist is prepared, which can promote lacrimal fluid secretion by administration to the skin surface of the eyelid, and which causes fewer side effects such as miosis, thereby to provide a percutaneous absorption type ophthalmic preparation capable of maintaining a therapeutically effective concentration of a muscarinic receptor agonist for promoting lacrimal fluid secretion, which is associated with fewer side effects such as miosis, and a method of promoting lacrimal fluid secretion by administering a percutaneous absorption type ophthalmic preparation containing a muscarinic receptor agonist to the skin surface of the eyelid.
摘要翻译：制备包含毒蕈碱受体激动剂的经皮吸收型眼用制剂，其通过给予眼睑的皮肤表面而促进泪液分泌，并且引起较少的副作用如瞳孔缩小，由此提供能够维持用于促进泪液分泌的毒蕈碱受体激动剂的治疗有效浓度，其与较少的副作用如瞳孔缩小相关，以及通过将含有毒蕈碱受体激动剂的经皮吸收型眼用制剂给予皮肤表面的眼睑。

5. 发明申请

US20090209632A1 Percutaneously Absorptive Ophthalmic Preparation Comprising Olopatadine 有权
标题翻译：包含奥洛他定的经皮吸收性眼科制剂
公开(公告)号：US20090209632A1
公开(公告)日：2009-08-20
申请号：US11988377
申请日：2006-07-07
申请人： Akiharu Isowaki , Tomoko Nakajima , Akira Ohtori
发明人： Akiharu Isowaki , Tomoko Nakajima , Akira Ohtori
IPC分类号： A61K31/335 , A61P27/02
CPC分类号： A61K9/0014 , A61K9/0048
摘要： The present invention provides a percutaneously absorptive preparation for preventing or treating allergic eye disease, which comprises olopatadine or a salt thereof as an active ingredient. In addition, the present invention provides a method for preventing or treating allergic eye disease, which comprises applying a percutaneously absorptive preparation comprising olopatadine or a salt thereof to the skin surface including the skin surface of an eyelid, thereby casing transfer of a therapeutically effective amount of olopatadine or a salt thereof from the preparation to an anterior ocular segment through the skin of the eyelid rather than a systemic blood flow. The present preparation can exert a pharmacological effect over a prolonged period by a single application, as compared to conventional preparations such as eye drops.
摘要翻译：本发明提供一种用于预防或治疗过敏性眼病的经皮吸收制剂，其包含奥洛他定或其盐作为活性成分。此外，本发明提供了一种预防或治疗过敏性眼病的方法，其包括将包含奥洛他定或其盐的经皮吸收制剂施用于包括眼睑皮肤表面的皮肤表面，由此将治疗有效量的奥洛他定或其盐从制剂通过眼睑的皮肤而不是全身血液流过眼前段。与常规制剂如滴眼剂相比，本发明的制剂可以通过单次使用施用长时间的药理作用。

6. 发明申请

US20090143359A1 Percutaneously Absorptive Ophthalmic Preparation Comprising Epinastine 审中-公开
标题翻译：包含依诺斯汀的经皮吸收性眼科制剂
公开(公告)号：US20090143359A1
公开(公告)日：2009-06-04
申请号：US11988390
申请日：2006-07-07
申请人： Akiharu Isowaki , Tomoko Nakajima , Akira Ohtori
发明人： Akiharu Isowaki , Tomoko Nakajima , Akira Ohtori
IPC分类号： A61K31/55
CPC分类号： A61K9/7023 , A61K9/0048 , A61K9/06 , A61K9/107
摘要： The present invention provides a percutaneously absorptive preparation for preventing or treating allergic eye disease, which comprises epinastine or a salt thereof as an active ingredient. In addition, the present invention provides a method for preventing or treating allergic eye disease, which comprises applying a percutaneously absorptive preparation comprising epinastine or a salt thereof to the skin surface including the skin surface of an eyelid, thereby causing transfer of a therapeutically effective amount of epinastine or a salt thereof from the preparation to an anterior ocular segment through the skin of the eyelid rather than a systemic blood flow. The present preparation can exert a pharmacological effect over a prolonged period by a single application, as compared to conventional preparations such as eye drops.
摘要翻译：本发明提供一种用于预防或治疗过敏性眼病的经皮吸收制剂，其包含依波他汀或其盐作为活性成分。此外，本发明提供一种预防或治疗过敏性眼病的方法，其包括将包含依托斯汀或其盐的经皮吸收制剂施用于包括眼睑皮肤表面的皮肤表面，从而导致治疗有效量的转移的依帕斯他汀或其盐从制剂到眼前段，通过眼睑的皮肤而不是全身血流。与常规制剂如滴眼剂相比，本发明的制剂可以通过单次使用施用长时间的药理作用。

7. 发明申请

US20090082381A1 Percutaneously Absorbable Ophthalmic Preparation 审中-公开
标题翻译：经皮吸收眼科制剂
公开(公告)号：US20090082381A1
公开(公告)日：2009-03-26
申请号：US11989332
申请日：2006-07-26
申请人： Akiharu Isowaki , Akira Ohtori
发明人： Akiharu Isowaki , Akira Ohtori
IPC分类号： A61K31/438 , C07D221/20 , A61P27/02
CPC分类号： A61K9/0048 , A61K31/438 , A61K47/14 , A61K47/32 , C07D491/107
摘要： The present invention provides a percutaneously absorbable ophthalmic preparation that permits the retention of a therapeutically effective concentration of a heterocyclic spiro compound and a salt thereof for promoting lacrimation, and that produces less adverse reactions such as miosis. Specifically, the present invention provides a percutaneously absorbable ophthalmic preparation comprising as an active ingredient a heterocyclic spiro compound represented by the general formula (I): [wherein the symbols have the same definitions as those given in the description] or a pharmaceutically acceptable salt thereof.
摘要翻译：本发明提供了一种经皮吸收性眼用制剂，其允许保留治疗有效浓度的杂环螺环化合物及其盐以促进流泪，并且产生较少的不良反应，例如瞳孔缩小。具体地，本发明提供一种经皮吸收性眼用制剂，其包含作为活性成分的由通式（I）表示的杂环螺环化合物：[其中符号具有与说明书中给出的相同的定义]或其药学上可接受的盐。

8. 发明授权

US08101654B2 Percutaneously absorptive ophthalmic preparation comprising olopatadine 有权
标题翻译：包含奥洛他定的经皮吸收性眼用制剂
公开(公告)号：US08101654B2
公开(公告)日：2012-01-24
申请号：US11988377
申请日：2006-07-07
申请人： Akiharu Isowaki , Tomoko Nakajima , Akira Ohtori
发明人： Akiharu Isowaki , Tomoko Nakajima , Akira Ohtori
IPC分类号： A01N43/02 , A01N43/40
CPC分类号： A61K9/0014 , A61K9/0048
摘要： The present invention provides a percutaneously absorptive preparation for preventing or treating allergic eye disease, which comprises olopatadine or a salt thereof as an active ingredient. In addition, the present invention provides a method for preventing or treating allergic eye disease, which comprises applying a percutaneously absorptive preparation comprising olopatadine or a salt thereof to the skin surface including the skin surface of an eyelid, thereby casing transfer of a therapeutically effective amount of olopatadine or a salt thereof from the preparation to an anterior ocular segment through the skin of the eyelid rather than a systemic blood flow. The present preparation can exert a pharmacological effect over a prolonged period by a single application, as compared to conventional preparations such as eye drops.
摘要翻译：本发明提供一种用于预防或治疗过敏性眼病的经皮吸收制剂，其包含奥洛他定或其盐作为活性成分。此外，本发明提供了一种预防或治疗过敏性眼病的方法，其包括将包含奥洛他定或其盐的经皮吸收制剂施用于包括眼睑皮肤表面的皮肤表面，由此将治疗有效量的奥洛他定或其盐从制剂通过眼睑的皮肤而不是全身血液流过眼前段。与常规制剂如滴眼剂相比，本发明的制剂可以通过单次使用施用长时间的药理作用。

9. 发明申请

US20090318422A1 OPHTHALMIC PERCUTANEOUS ABSORPTION TYPE PREPARATION 审中-公开
标题翻译： OPHTHALMIC PERCUTANEOUS吸收式制备
公开(公告)号：US20090318422A1
公开(公告)日：2009-12-24
申请号：US12310281
申请日：2007-08-28
申请人： Akiharu Isowaki , Tomoko Nakajima , Akira Ohtori
发明人： Akiharu Isowaki , Tomoko Nakajima , Akira Ohtori
IPC分类号： A61K31/55 , A61K31/44 , A61K31/335
CPC分类号： A61K9/0048
摘要： The present invention provides an ophthalmic percutaneous absorption type preparation containing an ophthalmic drug and a vasoconstrictor, which can increase the amount of the ophthalmic drug transferred through the eyelid to a topical area in the eye, particularly the anterior segment of the eye such as conjunctiva, lacrimal fluid, aqueous humor, cornea and the like by administration to the skin surface of an eyelid.
摘要翻译：本发明提供一种含有眼用药物和血管收缩剂的眼用经皮吸收型制剂，其可以将通过眼睑转移的眼药物的量增加到眼睛中的局部区域，特别是眼睛前段，例如结膜，泪液，房水，角膜等，通过施用于眼睑的皮肤表面。

10. 发明授权

US5152758A Electroresponsive hydrogel and physiologically active substance release control system 失效
标题翻译：电生物氢化物和生理活性物质释放控制系统
公开(公告)号：US5152758A
公开(公告)日：1992-10-06
申请号：US556332
申请日：1990-07-23
申请人： Isao Kaetsu , Yasushi Morita , Akira Ohtori
发明人： Isao Kaetsu , Yasushi Morita , Akira Ohtori
IPC分类号： A61M37/00 , A61K9/00 , A61K9/20 , A61K9/22 , A61K38/28
CPC分类号： A61K38/28 , A61K9/0009 , A61K9/2027
摘要： An electroresponsive hydrogel produced by alkali hydrolysis of a copolymer comprising N-isopropylacrylamide, an ionic monomer and a crosslinking agent; and a physiologically active substance release control system comprising a biosensor, an amplifier and an electroresponsive hydrogel containing physiologically active substance are disclosed. The hydrogel of the present invention is capable of releasing a physiologically active substance alone in an amount corresponding to the applied voltage with excellent reproducibility by contracting and reswelling in good response to the loading and unloading of an external stimulation voltage, it can be advantageously used in a physiologically active substance release control system capable of releasing an essential physiologically active substance in a necessary amount according to changes in physiological conditions. Also, the physiologically active substance release control system of the present invention using this hydrogel is useful for the treatment of various diseases including diabetes mellitus.

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