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公开(公告)号：US5662925A
公开(公告)日：1997-09-02
申请号：US638440
申请日：1996-04-26
CPC分类号： A61K9/703 , A61K9/7084
摘要： A device for administering an active agent to the skin or mucosa of an individual comprising a laminated composite of an adhesive overlay, a backing layer underlying the central portion of the adhesive overlay, an active agent-permeable membrane, the backing layer and membrane defining a reservoir that contains a formulation of the active agent, a peel seal disc underlying the active agent-permeable membrane, a heat seal about the periphery of the peel seal disc, the active agent-permeable membrane and the backing layer and a removable release liner underlying the exposed overlay and peel seal disc. The adhesive layer is above and peripheral to the path of the active agent to the skin or mucosa and is protected from degradation by the components of the reservoir by a multiplicity of heat seals. The peel seal disc protects against release of the active agent-containing reservoir and the release liner protects the adhesive from exposure to the environment prior to use.
摘要翻译： 一种用于向个体的皮肤或粘膜施用活性剂的装置，其包括粘合剂覆盖物，粘合剂覆盖物的中心部分下方的背衬层，活性剂渗透膜，背衬层和膜的层压复合材料 储存器，其包含活性剂的制剂，活性剂渗透膜下面的剥离密封盘，围绕剥离密封盘的周边的热密封，活性剂可渗透膜和背衬层以及可移除的释放衬垫 暴露的覆盖层和剥离密封盘。 粘合剂层位于活性剂到皮肤或粘膜的路径之上和周边，并通过多种热封保护储存器的部件免于降解。 剥离密封盘防止含活性剂的储存器的释放，并且释放衬垫在使用之前保护粘合剂免于暴露于环境中。
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公开(公告)号：US5626866A
公开(公告)日：1997-05-06
申请号：US544110
申请日：1995-10-17
IPC分类号： A61K9/70 , A61K31/465 , A61F13/00 , A61F13/02
CPC分类号： A61K9/703 , A61K9/7061
摘要： A method for making a transdermal drug delivery device for heat sensitive and volatile drugs is disclosed. The device contains a drug-containing adhesive composite layer having an impermeable backing material laminated to the distal surface thereof and a proximal peelable impermeable backing material adapted for removal for administering a drug to the skin or mucosa laminated to the proximal surface thereof. The method comprising the steps of providing first and second adhesive laminates each comprising a drug permeable adhesive layer having laminated to one surface one of said backing materials and having the opposing surface exposed. The drug, in gelled form and optionally containing additives such as enhancers and preservatives, is extruded onto at least one exposed surface of the first or second adhesive laminate followed by laminating together the exposed surfaces of the first and second adhesive laminate such that the adhesive layers and gelled drug are combined to form the drug-containing adhesive composite layer having the distal and proximal surfaces covered by the respective backing materials. The adhesives used in making up the laminates may be the same or different provided the drug is compatible with the adhesive. The process is particularly adaptable to the formulation of nicotine-containing patches. Drug delivery devices made according to the disclosed method and a method of using these drug delivery devices are also described.
摘要翻译： 公开了制备用于热敏和挥发性药物的透皮药物递送装置的方法。 该装置含有含有药物的粘合剂复合层，其具有层压到其远端表面的不可渗透的背衬材料和适于去除的药物的近侧可剥离的不渗透背衬材料，以将药物施用于层压到其近侧表面的皮肤或粘膜。 该方法包括以下步骤：提供第一和第二粘合剂层压体，每个粘合层压板包括药物可渗透的粘合剂层，该粘合剂层层压到所述背衬材料的一个表面并且具有暴露的相对表面。 将胶体形式的药物和任选地含有添加剂如增强剂和防腐剂的药物挤压到第一或第二粘合层压体的至少一个暴露表面上，然后将第一和第二粘合层压体的暴露表面层压在一起，使得粘合剂层 并且凝胶化药物组合以形成具有由各个背衬材料覆盖的远侧和近侧表面的含药物的粘合剂复合材料层。 用于组合层压体的粘合剂可以相同或不同，只要药物与粘合剂相容即可。 该方法特别适用于含尼古丁的贴剂的制剂。 还描述了根据所公开的方法制备的药物递送装置和使用这些药物递送装置的方法。
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公开(公告)号：US5780050A
公开(公告)日：1998-07-14
申请号：US504430
申请日：1995-07-20
IPC分类号： A61K9/70 , A61K31/565 , A61K31/57 , A61K47/04 , A61K47/10 , A61K47/14 , A61K47/16 , A61K47/20 , A61K47/30 , A61K47/32 , A61K47/44 , A61P5/24 , A61P5/38 , A61F13/00
CPC分类号： A61K9/7061 , A61K31/568 , A61K31/569 , A61K31/57 , A61K31/573 , A61K31/575
摘要： A stabilized patch device for transdermal drug delivery of steroid drugs containing a 3-keto-4-en functional group is described, wherein the patch comprises an effective amount of the steroid drug and a carrier that is free of acid functional groups. The device can further contain additives such as a penetration enhancer or excipient, so long as such additives are also free of acid functional groups. The device can be either a matrix patch or a liquid reservoir patch. In a matrix patch, the carrier is a biocompatible polymeric adhesive with which the steroid drug is intimately admixed. The adhesive is preferably an acrylic polymer or copolymer. In a liquid reservoir patch, the carrier is a controlled-viscosity composition containing a thinner or thickener. Preferred steroid drugs include certain corticosteroids and sex hormones, such as progestins and androgens. A method of stabilizing such steroid drugs during storage in transdermal patches is also disclosed.
摘要翻译： 描述了一种用于经皮药物递送含有3-酮-4-烯官能团的类固醇药物的稳定补片装置，其中补片包含有效量的类固醇药物和不含酸官能团的载体。 该装置可以进一步含有添加剂如渗透促进剂或赋形剂，只要这些添加剂也不含酸官能团。 该装置可以是矩阵补丁或液体储存器补丁。 在基质贴剂中，载体是与类固醇药物紧密混合的生物相容的聚合物粘合剂。 粘合剂优选为丙烯酸类聚合物或共聚物。 在液体储存贴片中，载体是含有较薄或增稠剂的受控粘度组合物。 优选的类固醇药物包括某些皮质类固醇和性激素，如孕激素和雄激素。 还公开了在透皮贴剂储存期间稳定这种类固醇药物的方法。
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4.发明授权Method of making pressure sensitive adhesive matrix patches for transdermal drug delivery using hydrophilic salts of drugs and hydrophobic pressure sensitive adhesive dispersions 有权使用药物的亲水盐和疏水性压敏粘合剂分散体制备用于透皮药物递送的压敏粘合剂基质贴剂的方法公开(公告)号：US06365178B1
公开(公告)日：2002-04-02
申请号：US09764040
申请日：2001-01-17
IPC分类号： A61K970
CPC分类号： A61K9/7053 , A61K9/7061
摘要： A method of making a pressure sensitive matrix patch for transdermal delivery of a drug is disclosed. The method includes the steps of dissolving a hydrophilic salt form of the drug in the water phase of an aqueous dispersion of a hydrophobic pressure sensitive adhesive, casting the resulting mixture as a thin film, and evaporating the water. The physical stability of the drug in the film is excellent, and crystallization of the drug is inhibited. A method of increasing the transdermal flux of an acidic drug is also disclosed.
摘要翻译： 公开了制备用于药物透皮递送的压敏基质贴片的方法。 该方法包括以下步骤：将亲水盐形式的药物溶解在疏水性压敏粘合剂的水分散体的水相中，将所得混合物浇铸成薄膜，并蒸发水。 药物在膜中的物理稳定性优异，药物的结晶被抑制。 还公开了增加酸性药物的经皮通量的方法。
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5.发明授权
公开(公告)号：US5985317A
公开(公告)日：1999-11-16
申请号：US706624
申请日：1996-09-06
CPC分类号： A61K9/703 , A61K9/7053 , A61K9/7061
摘要： A method of transdermally or transmucosally delivering a hydrophilic salt form of a drug with a water-based pressure sensitive hydrophobic adhesive matrix patch optionally containing a permeation enhancer is disclosed. A matrix patch comprising a water-based pressure sensitive hydrophobic adhesive, a hydrophilic salt form of a drug, and optionally a permeation enhancer for transdermal or transmucosal delivery of the hydrophilic salt form of the drug is also disclosed.
摘要翻译： 公开了一种透皮或透粘膜递送药物的亲水盐形式的方法，该方法是使用任选含有渗透促进剂的基于水的压敏疏水性粘合剂基质片剂。 还公开了一种基质贴剂，其包含水基压敏疏水性粘合剂，药物的亲水盐形式和任选的用于透皮或经粘膜递送亲水盐形式的药物的渗透促进剂。
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6.发明授权Transdermal delivery devices containing polydiorganosiloxane polymers to regulate adhesive properties 有权含有聚二有机硅氧烷聚合物以调节粘合剂性能的透皮递送装置公开(公告)号：US06730318B2
公开(公告)日：2004-05-04
申请号：US09924564
申请日：2001-08-08
IPC分类号： A61F1302
CPC分类号： A61K8/891 , A61F9/04 , A61F13/122 , A61F2013/00374 , A61F2013/00497 , A61F2013/00906 , A61K8/0208 , A61K8/676 , A61K8/678 , A61K9/7053 , A61K9/7061 , A61Q19/00 , A61Q19/08
摘要： The adhesive capability of matrix-type transdermal devices for the delivery of drugs, cosmetics, emollients and the like is altered by incorporating into the pressure-sensitive adhesive an effective amount of a polydiorganosiloxane polymer fluid adhesion adjusting agent. The properties of the pressure-sensitive adhesive are modified to enable a matrix-type patch to adhere temporarily to the skin for a period sufficient to accomplish its desired delivery purpose and then be removed without causing skin damage or irritation and without leaving substantial adhesive residue on the skin. Polydimethylsiloxanes (dimethicones) are preferred adhesion adjusting agents and acrylic-based polymers are preferred pressure-sensitive adhesives. Matrix-type patches containing anti-wrinkle agents formulated with dimethicones in the adhesive for application to areas on the face and particularly around the eyes are especially useful.
摘要翻译： 用于递送药物，化妆品，润肤剂等的基质型透皮装置的粘合能力通过将有效量的聚二有机硅氧烷聚合物流体粘附调节剂并入压敏粘合剂而改变。 修改压敏粘合剂的性能以使基质型贴片能够临时粘附到皮肤上足够长的时间以实现其期望的递送目的，然后在不引起皮肤损伤或刺激的情况下被除去并且不会留下大量的粘合剂残留物 皮。 聚二甲基硅氧烷（二甲基硅氧烷）是优选的粘合调节剂，丙烯酸类聚合物是优选的压敏粘合剂。 在粘合剂中用二甲硅油配制的抗皱剂的基质型贴剂适用于脸部和特别是眼睛周围的区域是特别有用的。
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7.发明授权
公开(公告)号：US5601839A
公开(公告)日：1997-02-11
申请号：US429757
申请日：1995-04-26
IPC分类号： A61K9/00 , A61K9/70 , A61K31/137 , A61K31/138 , A61K31/167 , A61K31/216 , A61K31/404 , A61K31/4458 , A61K31/46 , A61K31/485 , A61K31/5415 , A61K31/55 , A61K47/10 , A61K47/14 , A61K47/30 , A61K47/32 , A61P9/00 , A61P9/06 , A61P21/02 , A61P23/02 , A61P25/04 , A61P25/24 , A61P25/26 , A61P27/02 , A61F13/02
CPC分类号： A61K9/7053 , A61K47/14 , A61K9/0014 , A61K9/7061 , A61K9/7069 , Y10S514/946
摘要： A composition and method for enhancing transdermal penetration of a basic drug are described. The composition comprises a matrix patch comprising an effective amount of a basic drug, preferably having a pK.sub.a of about 8.0 or greater, an effective amount of penetration enhancer consisting essentially of triacetin, and a polymer later preferably comprising a pressure-sensitive adhesive. A preferred basic drug is oxybutynin and acid addition salts thereof. The method for enhancing transdermal penetration comprises applying the matrix patch to a selected area of skin.
摘要翻译： 描述了用于增强基础药物透皮渗透的组合物和方法。 所述组合物包含基质贴片，其包含有效量的碱性药物，优选具有约8.0或更大的pKa，有效量的基本上由三醋精组成的渗透促进剂，以及稍后优选包含压敏粘合剂的聚合物。 优选的碱性药物是奥昔布宁及其酸加成盐。 用于增强透皮渗透的方法包括将基质片施加到选定的皮肤区域。
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8.发明授权Methods for providing testosterone and optionally estrogen replacement therapy to women 失效为女性提供睾酮和任选的雌激素替代疗法的方法
公开(公告)号：US5460820A
公开(公告)日：1995-10-24
申请号：US99923
申请日：1993-08-03
IPC分类号： A61K9/70 , A61K31/565 , A61K31/566 , A61K31/568 , A61P3/02 , A61P5/24 , A61P5/30 , A61P9/00 , A61P19/10 , A61P43/00 , A61F13/00
CPC分类号： A61K9/7061 , A61K31/565 , A61K31/568
摘要： A method of providing testosterone replacement therapy to a woman in need of such therapy comprising applying a testosterone-delivering patch to the skin of said woman which patch transdermally delivers 50 to 500 .mu.g/day of testosterone to the woman.
摘要翻译： 向需要这种治疗的女性提供睾酮替代疗法的方法包括向所述女性的皮肤施用睾丸激素递送贴片，所述补片透皮地向女性递送50-500μg/天的睾丸激素。
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9.发明授权Antioxidant composition for topical/transdermal prevention and treatment of wrinkles 有权用于局部/透皮预防和治疗皱纹的抗氧化组合物公开(公告)号：US06180133B2
公开(公告)日：2001-01-30
申请号：US09198734
申请日：1998-11-24
IPC分类号： A61K970
CPC分类号： A61Q19/08 , A61F9/04 , A61F13/122 , A61F2013/00374 , A61F2013/00497 , A61F2013/00906 , A61K8/0208 , A61K8/676 , A61K8/678 , A61K2800/522 , Y10S514/844 , Y10S514/848 , Y10S514/975
摘要： An anti-wrinkle skin treating composition comprises a pressure sensitive matrix patch having dissolved in the adhesive a mixture of antioxidants in the form of a Vitamins C ester and Vitamin E. Also preferably dissolved in the adhesive are glycerine and a polydiorganosiloxane adhesion-adjusting agent. Optionally dissolved in the adhesive is also one or more members selected from the group consisting of moisturizing agents, skin collagen synthesis promoting agents and exfoliating agents. When applied to a wrinkled skin area the composition acts to diminish fine wrinkles and improves the overall thickness, elasticity, firmness and smoothness of the skin. The modified adhesive properties of the patch are sufficient to maintain the patch in place on the skin for the recommended treatment period while allowing the patch to be readily removed without causing skin irritation or leaving adhesive residue on the skin.
摘要翻译： 抗皱皮肤处理组合物包含在维生素C酯和维生素E形式的溶解在粘合剂中的抗氧化剂混合物的压敏基质贴片。还优选溶解在粘合剂中的是甘油和聚二有机硅氧烷粘合调节剂。 任选地溶解在粘合剂中也是选自保湿剂，皮肤胶原合成促进剂和去角质剂的一种或多种。 当应用于起皱的皮肤区域时，组合物起减少细小皱纹的作用，并提高皮肤的整体厚度，弹性，坚固度和平滑度。 贴剂的改性粘合剂性能足以将贴片保持在皮肤上适合推荐的治疗期，同时允许容易地去除贴片而不引起皮肤刺激或在皮肤上留下粘合剂残留物。
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10.发明授权Transdermal drug delivery matrix for coadministering estradiol and another steroid 失效用于联合雌二醇和另一种类固醇的透皮药物递送基质
公开(公告)号：US5783208A
公开(公告)日：1998-07-21
申请号：US683892
申请日：1996-07-19
IPC分类号： A61K9/70 , A61K31/565 , A61L15/58 , C07J1/00 , A61F13/02
CPC分类号： A61K9/7061 , A61K31/565
摘要： A matrix type transdermal patch for coadministering estradiol and another steroid wherein the matrix is composed of a N-vinyl-2-pyrrolidone-containing acrylic copolymer pressure sensitive adhesive, estradiol, the other steroid, and optionally a permeation enhancer, and the respective fluxes of estradiol and the other steroid from the matrix are independent of the respective concentrations of the other steroid and estradiol in the matrix.
摘要翻译： 用于共混雌二醇和另一种类固醇的基质型透皮贴剂，其中基质由含N-乙烯基-2-吡咯烷酮的丙烯酸共聚物压敏粘合剂，雌二醇，另一种类固醇和任选的渗透促进剂组成， 雌二醇和基质中的其他类固醇与基质中其他类固醇和雌二醇的各自浓度无关。
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