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1. 发明申请

US20050187212A1 Pharmaceutical composition for topical delivery of meloxicam 审中-公开
公开(公告)号：US20050187212A1
公开(公告)日：2005-08-25
申请号：US11045233
申请日：2005-01-27
申请人： Toshimitsu Ohki , Noritaka Seko , Naohisa Kawamura , Ken-Ichi Noguchi , Junji Kawakami
发明人： Toshimitsu Ohki , Noritaka Seko , Naohisa Kawamura , Ken-Ichi Noguchi , Junji Kawakami
IPC分类号： A61K9/70 , A61K31/5415 , A61K47/18 , A61P29/00
CPC分类号： A61K9/7053 , A61K9/7076 , A61K31/5415 , A61K47/18
摘要： A pharmaceutical composition comprising: (a) a pharmaceutically effective amount of meloxicam, or a pharmaceutically acceptable salt thereof; (b) a skin permeation enhancing agent selected from the group consisting of: (i) an amine of formula I wherein: R1, R2, and R3 are each independently an alkanolyl group with 1 to 24 C-atoms, in which one or more H-atoms are optionally substituted by —OH and/or one or more —CH2— groups are optionally substituted by —O—, or a polyoxyethylene group with 2 to 30 ethylene oxide units, and R2 and R3 are additionally independently H or a linear, branched, or cyclic alkyl group with 1 to 24 C-atoms, in which one or more —CH2— groups are optionally substituted by —CH═CH— and/or —O— and/or in which one or more H-atoms are optionally substituted by —OH, and (ii) an amide of formula II wherein: R4 and R5 are each independently a linear, branched, or cyclic alkyl group with 1 to 24 C-atoms, in which one or more —CH2— groups are optionally substituted by —CH═CH—and/or —O— and/or in which one or more H-atoms are optionally substituted by —OH, and R6 is H or a linear, branched, or cyclic alkyl group with 1 to 24 C-atoms, in which one or more —CH2— groups are optionally substituted by —CH═CH— and/or —O— and/or in which one or more H-atoms are optionally substituted by —OH; and (c) at least one inert carrier. Furthermore this invention relates to a transdermal delivery system and a method for treating, preventing and/or relieving the signs and/or symptoms of rheumatoid arthritis, cervico-omo-brachial syndrome, low back pain, osteoarthritis, periarthritis scapulohumeralis, tendovaginitis, peritendinitis, humerus epicondylitis, including tennis elbow, myalgia, post-traumatic tumor and pain.

2. 发明授权

US08128946B2 Medical tape preparation 有权
标题翻译：医用胶带准备
公开(公告)号：US08128946B2
公开(公告)日：2012-03-06
申请号：US13154151
申请日：2011-06-06
申请人： Naohisa Kawamura , Hidenori Sawada , Takayuki Kobayashi
发明人： Naohisa Kawamura , Hidenori Sawada , Takayuki Kobayashi
IPC分类号： A61K9/70 , C08L15/00
CPC分类号： A61L15/225 , A61K9/7061 , A61L15/585 , C08L33/08 , C08L33/14 , C08L2666/04 , C09J7/385 , C09J133/08 , C09J133/14
摘要： A medical tape preparation which comprises a support and, superposed on one side thereof in the following order, a pressure-sensitive adhesive layer and a release liner. The pressure-sensitive adhesive layer can contain a large amount of an oleophilic oily matter. The tape preparation is excellent in adhesion, cohesiveness, and stability even when no crosslinking agent is used. The pressure-sensitive adhesive layer in the medical tape preparation comprises a blend of two tacky polymers, which are a tacky polymer (A) comprising a copolymer obtained from 2-acetoacetoxyethyl methacrylate and other vinyl monomer(s) as constituent ingredients and a tacky polymer (B) comprising a copolymer which is obtained from a C4-10-alkyl(meth)acrylate and other vinyl monomer(s) as constituent ingredients and is different from the tacky polymer (A).
摘要翻译：一种医用胶带制剂，其包含支撑体，并且按照以下顺序叠置在其一侧上的压敏粘合剂层和剥离衬垫。压敏粘合剂层可以含有大量的亲油性油性物质。即使没有使用交联剂，胶带制剂的粘合性，内聚性和稳定性也优异。医用胶带制剂中的压敏粘合剂层包括两种粘性聚合物的共混物，它们是包含由甲基丙烯酸2-乙酰乙酰氧基乙酯和其它乙烯基单体作为组分成分得到的共聚物的粘性聚合物（A）和粘性聚合物（B）包含由（甲基）丙烯酸C 4-10烷基酯和其它乙烯基单体作为构成成分得到的并且与粘性聚合物（A）不同的共聚物。

3. 发明申请

US20120178788A1 METHOD FOR SUPPRESSING ESTERIFICATION OF PHARMACEUTICAL COMPOSITION 审中-公开
标题翻译：抑制药物组合物鉴定的方法
公开(公告)号：US20120178788A1
公开(公告)日：2012-07-12
申请号：US13420991
申请日：2012-03-15
申请人： Naohisa Kawamura , Takashi Saitoh , Junko Tsuchiya , Chie Sugaya
发明人： Naohisa Kawamura , Takashi Saitoh , Junko Tsuchiya , Chie Sugaya
IPC分类号： A61K31/405 , A61K31/196 , A61K31/137 , A61K31/192
CPC分类号： A61K9/7053 , A61K9/7076 , A61K31/137 , A61K31/192 , A61K31/195 , A61K31/405
摘要： Disclosed are a pharmaceutical composition for external application, an adhesive skin patch and others which are improved in a drug release property, transdermal absorbability and stability of a pharmacologically active ingredient contained therein and can reduce the aggravation of irritation to the skin. Specifically disclosed is an adhesive skin patch comprising a support and an adhesive layer laminated on the support, wherein the adhesive layer contains a pharmaceutical composition for external application. The pharmaceutical composition for external application comprises a pharmacologically active ingredient, an auxiliary component and a pyrrolidone compound, wherein one of the pharmacologically active ingredient and the auxiliary component has a carboxylate group in the molecule and the other has a hydroxy group in the molecule. Preferably, the adhesive layer further comprises a hydrogenated oil.
摘要翻译：本发明公开了一种外用药物组合物，粘合性皮肤贴剂等，其药物释放性能，经皮吸收性和其中所含的药理活性成分的稳定性得到改善，并且可以减轻刺激对皮肤的加重。具体公开了一种粘合性皮肤贴剂，其包含层压在载体上的载体和粘合剂层，其中粘合剂层含有用于外用的药物组合物。用于外用的药物组合物包含药理活性成分，辅助成分和吡咯烷酮化合物，其中药理活性成分和辅助成分之一在分子中具有羧酸酯基，另一个在分子中具有羟基。优选地，粘合剂层还包含氢化油。

4. 发明申请

US20110236440A1 MEDICAL TAPE PREPARATION 有权
标题翻译：医用胶带制剂
公开(公告)号：US20110236440A1
公开(公告)日：2011-09-29
申请号：US13154151
申请日：2011-06-06
申请人： Naohisa Kawamura , Hidenori Sawada , Takayuki Kobayashi
发明人： Naohisa Kawamura , Hidenori Sawada , Takayuki Kobayashi
IPC分类号： A61K9/70 , C08L33/10 , C08L33/26 , A61P17/00
CPC分类号： A61L15/225 , A61K9/7061 , A61L15/585 , C08L33/08 , C08L33/14 , C08L2666/04 , C09J7/385 , C09J133/08 , C09J133/14
摘要： A medical tape preparation which comprises a support and, superposed on one side thereof in the following order, a pressure-sensitive adhesive layer and a release liner. The pressure-sensitive adhesive layer can contain a large amount of an oleophilic oily matter. The tape preparation is excellent in adhesion, cohesiveness, and stability even when no crosslinking agent is used. The pressure-sensitive adhesive layer in the medical tape preparation comprises a blend of two tacky polymers, which are a tacky polymer (A) comprising a copolymer obtained from 2-acetoacetoxyethyl methacrylate and other vinyl monomer(s) as constituent ingredients and a tacky polymer (B) comprising a copolymer which is obtained from a C4-10-alkyl (meth)acrylate and other vinyl monomer(s) as constituent ingredients and is different from the tacky polymer (A).
摘要翻译：一种医用胶带制剂，其包含支撑体，并且按照以下顺序叠置在其一侧上的压敏粘合剂层和剥离衬垫。压敏粘合剂层可以含有大量的亲油性油性物质。即使没有使用交联剂，胶带制剂的粘合性，内聚性和稳定性也优异。医用胶带制剂中的压敏粘合剂层包括两种粘性聚合物的共混物，它们是包含由甲基丙烯酸2-乙酰乙酰氧基乙酯和其它乙烯基单体作为组分成分得到的共聚物的粘性聚合物（A）和粘性聚合物（B）包含由（甲基）丙烯酸C 4-10烷基酯和其它乙烯基单体作为构成成分得到的并且与粘性聚合物（A）不同的共聚物。

5. 发明申请

US20090274748A1 Nonaqueous pressure-sensitive adhesive for medicinal tape preparation for percutaneous absorption, medicinal tape preparation for percutaneous absorption, and process for producing the same 审中-公开
公开(公告)号：US20090274748A1
公开(公告)日：2009-11-05
申请号：US12460146
申请日：2009-07-14
申请人： Naohisa Kawamura , Hidenori Sawada , Takayuki Kobayashi
发明人： Naohisa Kawamura , Hidenori Sawada , Takayuki Kobayashi
IPC分类号： A61K9/70 , A61K47/32
CPC分类号： A61L24/046 , A61F2013/00663 , A61K9/7061 , A61K47/32 , Y10T156/1052
摘要： A nonaqueous pressure-sensitive adhesive for a medicinal tape preparation for percutaneous absorption comprising (a) a support, (b) a pressure-sensitive adhesive layer containing a drug and a nonaqueous pressure-sensitive adhesive and (c) a release film laminated in that order, and a medicinal tape preparation for percutaneous absorption comprising the adhesive. The nonaqueous pressure-sensitive adhesive may comprise a copolymer obtained by copolymerization of a (meth)acrylic monomer having an acetoacetyl group in the molecule and one or more monomers from among other (meth)acrylic monomers without acetoacetyl groups and copolymerizable vinyl monomers, in a nonaqueous solvent. Suitable (meth)acrylic monomers having an acetoacetyl group in the molecule are acetoacetoxyalkyl methacrylates, and especially 2-acetoacetoxyethyl methacrylate. The copolymer nonaqueous pressure-sensitive adhesive of the invention, comprising a (meth)acrylic monomer having an acetoacetyl group as a constituent monomer, is capable of containing large amounts of lipophilic oily substances in the pressure-sensitive adhesive layer, and during heat drying, the acetoacetyl groups undergo self-crosslinking to form a network structure as the solvent evaporates off, so that large amounts of oily substances such as the plasticizer can be included in the network structure. The pressure-sensitive adhesive of the invention uses no polyamine derivatives, isocyanate compounds, polyvalent metal chelate compounds, etc., as crosslinking agents, and therefore toxicity is not a concern and skin is not irritated. A medicinal tape preparation for percutaneous absorption of the invention has superior adhesive strength and cohesive strength, and is highly safe with low skin irritation. It also has excellent drug release and percutaneous absorption properties.

6. 发明授权

US6039971A Composition for skin patch preparation and process for preparing the same 失效
标题翻译：皮肤贴剂制剂组合物及其制备方法
公开(公告)号：US6039971A
公开(公告)日：2000-03-21
申请号：US25191
申请日：1998-02-18
申请人： Akihiko Kusunoki , Naohisa Kawamura , Yoshiki Sugizaki , Akio Kuwahara
发明人： Akihiko Kusunoki , Naohisa Kawamura , Yoshiki Sugizaki , Akio Kuwahara
IPC分类号： A61K9/70 , A61L15/60 , A61L26/00 , A61L5/60
CPC分类号： A61L26/008 , A61K9/7023 , A61L15/60
摘要： A composition for a skin patch including a synthetic polymer gel prepared by reacting a water-soluble polymer of an aliphatic carboxylic acid or a salt thereof with a sparingly soluble aluminum compound, an organic acid containing a hydroxyl group in its molecule as a reaction accelerator, and an ethylenediamine compound as a reaction inhibitor in the presence of water at a pH of 4.0 to 6.1. The composition can homogeneously gel at any crosslinking rate and does not cause any change in quality with the lapse of time.
摘要翻译：一种皮肤贴剂用组合物，其含有将脂肪族羧酸或其盐的水溶性聚合物与微溶铝化合物，分子中含有羟基的有机酸作为反应促进剂反应而制备的合成聚合物凝胶，和乙二胺化合物作为反应抑制剂，在pH为4.0至6.1的水存在下进行。该组合物可以任何交联速率均匀地凝胶化，并且随着时间的推移不会导致质量的任何改变。

7. 发明授权

US09168232B2 Transdermally absorbable preparation 有权
标题翻译：经皮吸收制剂
公开(公告)号：US09168232B2
公开(公告)日：2015-10-27
申请号：US13394656
申请日：2010-09-01
申请人： Naohisa Kawamura , Chie Sugaya
发明人： Naohisa Kawamura , Chie Sugaya
IPC分类号： A61M35/00 , A61K9/70 , A61K31/167 , A61K31/465 , A61F13/02
CPC分类号： A61K9/7061 , A61F13/02 , A61F13/023 , A61F13/0246 , A61F13/0253 , A61K9/7069 , A61K31/167 , A61K31/465 , A61M35/00
摘要： Disclosed is a transdermally absorbable preparation, in which an adhesive agent produced by crosslinking at least one copolymer is contained in an adhesive layer and the aging period in the production of the adhesive layer can be shortened. The transdermally absorbable preparation comprises a support and an adhesive layer arranged on the support and containing an adhesive agent and a medicinal component. The transdermally absorbable preparation is characterized in that the adhesive agent comprises a resin mixture comprising 100 parts by mass of a specific acrylic copolymer (A) and 0.1 to 30 parts by mass of a specific acrylic copolymer (B) or 0.05 to 2 part(s) by mass of a polyamine compound, and the adhesive layer additionally contains an organic acid.
摘要翻译：公开了一种透皮吸收制剂，其中通过交联至少一种共聚物制备的粘合剂包含在粘合剂层中，并且可以缩短粘合剂层的制备中的老化时间。经皮吸收制剂包括载体和布置在载体上并含有粘合剂和药物组分的粘合剂层。经皮吸收制剂的特征在于，粘合剂包含含有100质量份特定丙烯酸共聚物（A）和0.1〜30质量份特定丙烯酸类共聚物（B）或0.05〜2份（s）的树脂混合物），并且粘合剂层另外含有有机酸。

8. 发明申请

US20100022614A1 PHARMACEUTICAL COMPOSITION FOR EXTERNAL APPLICATION AND ADHESIVE SKIN PATCH 审中-公开
标题翻译：用于外用和胶粘皮肤的药物组合物
公开(公告)号：US20100022614A1
公开(公告)日：2010-01-28
申请号：US12448072
申请日：2007-12-06
申请人： Naohisa Kawamura , Takashi Saitoh , Junko Tsuchiya , Chie Sugaya
发明人： Naohisa Kawamura , Takashi Saitoh , Junko Tsuchiya , Chie Sugaya
IPC分类号： A61K31/405 , A61K31/192 , A61K31/196 , A61P25/00 , A61P29/00
CPC分类号： A61K9/7053 , A61K9/7076 , A61K31/137 , A61K31/192 , A61K31/195 , A61K31/405
摘要： Disclosed are a pharmaceutical composition for external application, an adhesive skin patch and others which are improved in a drug release property, transdermal absorbability and stability of a pharmacologically active ingredient contained therein and can reduce the aggravation of irritation to the skin. Specifically disclosed is an adhesive skin patch comprising a support and an adhesive layer laminated on the support, wherein the adhesive layer contains a pharmaceutical composition for external application. The pharmaceutical composition for external application comprises a pharmacologically active ingredient, an auxiliary component and a pyrrolidone compound, wherein one of the pharmacologically active ingredient and the auxiliary component has a carboxylate group in the molecule and the other has a hydroxy group in the molecule. Preferably, the adhesive layer further comprises a hydrogenated oil.
摘要翻译：本发明公开了一种外用药物组合物，粘合性皮肤贴剂等，其药物释放性能，经皮吸收性和其中所含的药理活性成分的稳定性得到改善，并且可以减轻刺激对皮肤的加重。具体公开了一种粘合性皮肤贴剂，其包含层压在载体上的载体和粘合剂层，其中粘合剂层含有用于外用的药物组合物。用于外用的药物组合物包含药理活性成分，辅助成分和吡咯烷酮化合物，其中药理活性成分和辅助成分之一在分子中具有羧酸酯基，另一个在分子中具有羟基。优选地，粘合剂层还包含氢化油。

9. 发明申请

US20090043236A1 Skin patch 审中-公开
标题翻译：皮肤补丁
公开(公告)号：US20090043236A1
公开(公告)日：2009-02-12
申请号：US11921289
申请日：2006-06-01
申请人： Naohisa Kawamura , Hidenori Sawada , Takashi Saitoh , Chihiro Takizawa , Junko Tsuchiya
发明人： Naohisa Kawamura , Hidenori Sawada , Takashi Saitoh , Chihiro Takizawa , Junko Tsuchiya
IPC分类号： A61F13/02
CPC分类号： A61K9/7053 , A61K9/7076 , C08K5/0016 , C08K5/01 , C08K5/3415 , C08L53/02 , C08L2201/00 , C08L2203/02 , C09J7/21 , C09J7/30 , C09J153/02 , C09J2201/60 , C09J2205/102 , C09J2453/00 , Y10T428/2883 , C08F236/08 , C08F236/10
摘要： A skin patch that can enhance the water resistance and handling easiness and can alleviate any irritation on the user. There is provided a skin patch having a flexible backing and, superimposed thereon, a plaster containing a styrene-isoprene-styrene block copolymer and having a glass transition temperature (Tg) of −45° to −35° C. and tan δ (lag angle) value, determined at dynamic viscoelasticity measurement (frequency 6.2832 rad/s) at 45° C., of 0.25 or less.
摘要翻译：皮肤贴剂可以增强耐水性和处理容易性，并可减轻使用者的任何刺激。提供了一种具有柔性背衬并且叠加在其上的含有苯乙烯 - 异戊二烯 - 苯乙烯嵌段共聚物并且具有-45°至-35℃的玻璃化转变温度（Tg）和tanδ（滞后）的石膏的皮肤贴剂角度）值，在45℃的动态粘弹性测量（频率6.2832rad / s）下测定为0.25或更小。

10. 发明申请

US20140302118A1 HYDROUS ADHESIVE SKIN PATCH 审中-公开
标题翻译： HYDROUS粘性皮肤护理
公开(公告)号：US20140302118A1
公开(公告)日：2014-10-09
申请号：US14240980
申请日：2012-08-24
申请人： Naohisa Kawamura , Je Phil Ryoo
发明人： Naohisa Kawamura , Je Phil Ryoo
IPC分类号： A61K31/167 , A61K47/10 , A61K9/70
CPC分类号： A61K47/10 , A61K9/7061 , A61K31/167
摘要： The purpose of the present invention is to provide a hydrous adhesive skin patch which contains lidocaine and can be applied in a uniform thickness easily. This hydrous adhesive skin patch comprises a support and an adhesive agent layer arranged on the support, wherein lidocaine or a pharmacologically acceptable salt thereof, a hydrophilic adhesive agent, and diethylene glycol or a diethylene glycol monoalkyl ether are contained in the adhesive agent layer. The diethylene glycol monoalkyl ether is preferably at least one compound selected from the group consisting of diethylene glycol monomethyl ether, diethylene glycol monoethyl ether and diethylene glycol monobutyl ether.
摘要翻译：本发明的目的是提供含有利多卡因的含水粘合剂皮肤贴片，并且可以容易地以均匀的厚度涂敷。这种含水粘合剂皮肤贴剂包括载体和布置在载体上的粘合剂层，其中在粘合剂层中包含利多卡因或其药理学上可接受的盐，亲水性粘合剂和二甘醇或二甘醇单烷基醚。二甘醇单烷基醚优选为选自二甘醇单甲醚，二甘醇单乙醚和二甘醇单丁醚中的至少一种化合物。

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