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公开(公告)号：US10814002B2
公开(公告)日：2020-10-27
申请号：US16209084
申请日：2018-12-04
IPC分类号： A61K47/12 , A61K9/70 , A61K47/06 , A61K47/14 , A61K31/55 , A61M37/00 , A61K31/407 , A61K47/10 , A61F13/00 , A61F13/02
摘要： A method for producing a patch including a support layer, and an adhesive agent layer formed on the support layer and including sodium diacetate, a pressure-sensitive adhesive base agent, and asenapine and/or a pharmaceutically acceptable salt thereof. The sodium diacetate is generated from sodium acetate in the presence of the asenapine and/or salt thereof, a content of the asenapine and/or salt thereof in terms of free asenapine in the adhesive agent layer is in range of 3.0 to 20 mg, and when a content of the asenapine and/or salt thereof in terms of free asenapine in the adhesive agent layer is 6.4 mg and the patch is in contact with skin for 24 hours, Cmax of free asenapine is in range of 0.5 to 6.0 ng/mL and tmax of free asenapine is in range of 8 to 28 hr.
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公开(公告)号：US20180289631A1
公开(公告)日：2018-10-11
申请号：US16008704
申请日：2018-06-14
IPC分类号： A61K9/70 , A61K47/10 , A61K47/12 , A61K47/14 , A61K31/407
摘要： In a patch comprising a support layer and an adhesive agent layer, the adhesive agent layer comprises free asenapine, a maleic acid alkali salt, and a rubber-based adhesive agent.
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公开(公告)号：US20150164862A1
公开(公告)日：2015-06-18
申请号：US14417205
申请日：2013-07-25
IPC分类号： A61K31/407 , A61K47/12 , A61K47/14 , A61K9/70
CPC分类号： A61K47/12 , A61K9/7038 , A61K9/7046 , A61K9/7053 , A61K9/7061 , A61K9/7069 , A61K31/407 , A61K31/55 , A61K47/06 , A61K47/10 , A61K47/14 , A61M37/00
摘要： A method for producing a patch comprising a support layer and an adhesive agent layer comprises: a mixture preparation step of mixing asenapine or a pharmaceutically acceptable salt thereof with sodium acetate whose particle diameter D50 at a cumulative volume of 50% in a particle diameter distribution is 40 to 1000 μm, in such a manner that the sodium acetate and sodium diacetate generated from the sodium acetate have a particle diameter D50 of 10 μm or smaller, thereby obtaining a mixture containing the sodium diacetate and the asenapine or pharmaceutically acceptable salt; and an adhesive-agent-layer formation step of forming the adhesive agent layer comprising the sodium diacetate, the asenapine or pharmaceutically acceptable salt, and a pressure-sensitive adhesive base agent, by using an adhesive agent layer composition obtained by mixing the mixture with the pressure-sensitive adhesive base agent.
摘要翻译： 制备包含支持层和粘合剂层的贴剂的方法包括：混合制备步骤，其将粒径分布中累积体积为50％的粒径D50与甲酸钠的药学上可接受的盐混合， 40至1000μm，使得由乙酸钠生成的乙酸钠和二乙酸钠的粒径D50为10μm或更小，从而获得含有二乙酸钠和阿替平或其药学上可接受的盐的混合物; 以及通过使用通过将混合物与所述粘合剂层组合物混合而获得的粘合剂层组合物形成包含二乙酸钠，阿替平或其药学上可接受的盐的粘合剂层和粘合剂基剂的粘合剂层形成步骤 压敏胶基剂。
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公开(公告)号：US10080738B2
公开(公告)日：2018-09-25
申请号：US15331939
申请日：2016-10-24
CPC分类号： A61K47/12 , A61K9/7038 , A61K9/7046 , A61K9/7053 , A61K9/7061 , A61K9/7069 , A61K31/407 , A61K31/55 , A61K47/06 , A61K47/10 , A61K47/14 , A61M37/00
摘要： A method for producing a patch comprising a support layer and an adhesive agent layer comprises: a mixture preparation step of mixing asenapine or a pharmaceutically acceptable salt thereof with sodium acetate whose particle diameter D50 at a cumulative volume of 50% in a particle diameter distribution is 40 to 1000 μm, in such a manner that the sodium acetate and sodium diacetate generated from the sodium acetate have a particle diameter D50 of 10 μm or smaller, thereby obtaining a mixture containing the sodium diacetate and the asenapine or pharmaceutically acceptable salt; and an adhesive-agent-layer formation step of forming the adhesive agent layer comprising the sodium diacetate, the asenapine or pharmaceutically acceptable salt, and a pressure-sensitive adhesive base agent, by using an adhesive agent layer composition obtained by mixing the mixture with the pressure-sensitive adhesive base agent.
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公开(公告)号：US20150231250A1
公开(公告)日：2015-08-20
申请号：US14416983
申请日：2013-07-25
CPC分类号： A61K47/12 , A61K9/7038 , A61K9/7046 , A61K9/7053 , A61K9/7061 , A61K9/7069 , A61K31/407 , A61K31/55 , A61K47/06 , A61K47/10 , A61K47/14 , A61M37/00
摘要： In a patch comprising a support layer and an adhesive agent layer, the adhesive agent layer comprises free asenapine, a maleic acid alkali salt, and a rubber-based adhesive agent.
摘要翻译： 在包含支撑层和粘合剂层的贴剂中，粘合剂层包含游离的阿替那非，马来酸碱金属盐和橡胶基粘合剂。
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公开(公告)号：US11123305B2
公开(公告)日：2021-09-21
申请号：US16008704
申请日：2018-06-14
IPC分类号： A61K9/70 , A61K47/10 , A61K47/12 , A61K47/14 , A61K31/407
摘要： In a patch comprising a support layer and an adhesive agent layer, the adhesive agent layer comprises free asenapine, a maleic acid alkali salt, and a rubber-based adhesive agent.
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公开(公告)号：US10583121B2
公开(公告)日：2020-03-10
申请号：US15454066
申请日：2017-03-09
IPC分类号： A61K31/407 , A61K47/10 , A61K47/06 , A61K9/70 , A61K47/12 , A61K47/14 , A61M37/00 , A61K31/55
摘要： A patch for administering asenapine includes a support layer, and an adhesive agent layer formed on the support layer and including an adhesive base agent and asenapine and/or a pharmaceutically acceptable salt thereof. The adhesive base agent has a content in a range of 10 to 90% by mass in the adhesive agent layer and includes a natural rubber, polyisobutylene, an alkyl vinyl ether(co)polymer, polyisoprene, polybutadiene, a styrene-butadiene copolymer, a styrene-isoprene copolymer, a styrene-isoprene-styrene block copolymer, or a combination thereof. When a content of the asenapine and/or pharmaceutically acceptable salt thereof in terms of free asenapine in the adhesive agent layer is 3.4 mg, an AUC2-120 for a period starting from the time when the patch is brought into contact with a skin for 24 hours is 27,000 pg·hr/mL or more, and an AUC2-120 of an asenapine metabolite is 20% or less of the AUC2-120 of the free asenapine.
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公开(公告)号：US09969688B2
公开(公告)日：2018-05-15
申请号：US15502793
申请日：2015-10-21
发明人： Atsushi Sonobe , Takashi Yasukochi , Yasunori Takada , Kenji Atarashi , Motohiro Suzuki , Shinichi Yokota
IPC分类号： C07D213/75
CPC分类号： C07D213/75 , A61K31/44
摘要： The present invention provides a compound represented by the formula (I) or a pharmaceutically acceptable salt thereof: wherein R is a hydrogen atom, a C1-6 alkyl group optionally substituted with one or more hydroxyl groups, a C1-6 alkoxy group, or a cyano group.
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公开(公告)号：US09308187B2
公开(公告)日：2016-04-12
申请号：US14408482
申请日：2013-06-17
IPC分类号： A61K31/196 , A61K9/70 , A61K9/00 , A61K47/12 , A61K47/20
CPC分类号： A61K31/196 , A61K9/0014 , A61K9/7038 , A61K9/7053 , A61K9/7061 , A61K9/7069 , A61K47/12 , A61K47/20
摘要： A patch comprising a support layer and an adhesive layer,wherein the adhesive layer comprises diclofenac sodium, dimethyl sulfoxide, and citric acid; a mass ratio between the diclofenac sodium and the citric acid (mass of diclofenac sodium:mass of citric acid) is 1:0.15 to 1:0.45; and a mass ratio between the diclofenac sodium and the dimethyl sulfoxide (mass of diclofenac sodium:mass of dimethyl sulfoxide) is 1:0.75 to 1:3.
摘要翻译： 一种贴剂，其包括支持层和粘合剂层，其中所述粘合剂层包含双氯芬酸钠，二甲基亚砜和柠檬酸; 双氯芬酸钠和柠檬酸（双氯芬酸钠的质量：柠檬酸的质量）之间的质量比为1:0.15至1:0.45; 双氯芬酸钠与二甲基亚砜（二氯苯胺酸钠的质量：二甲基亚砜的质量）的质量比为1:0.75〜1:3。
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公开(公告)号：US10441551B2
公开(公告)日：2019-10-15
申请号：US15769393
申请日：2016-10-24
发明人： Atsushi Sonobe , Akio Takeuchi , Yasunori Takada
IPC分类号： A61K9/70 , A61K47/02 , A61K47/10 , A61K47/14 , A61K47/20 , A61K47/22 , A61K47/32 , A61K47/44 , A61K31/4468
摘要： A patch comprises a backing and an adhesive layer laminated on at least one surface of the backing, in which the adhesive layer contains at least one selected from the group consisting of fentanyl and salts thereof, and contains an adhesive base material and an antioxidant having a sulfur atom in its molecule.
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