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公开(公告)号：US4983395A
公开(公告)日：1991-01-08
申请号：US326536
申请日：1989-03-21
申请人： Yunik Chang , Dinesh C. Patel , Charles D. Ebert
发明人： Yunik Chang , Dinesh C. Patel , Charles D. Ebert
CPC分类号： A61K9/703 , A61K9/7084
摘要： A transdermal drug delivery device comprising a drug formulation-containing reservoir defined by a backing layer and a drug-permeable membrane layer, a peelable inner liner that underlies the reservoir and a portion of the backing/membrane outwardly of the reservoir periphery, an adhesive layer that underlies the inner liner and outwardly extending portions of the membrane/backing layers, and a peelable release liner layer that underlies the adhesive layer with a first permanent heat seal between the backing and the membrane about the perimeter of the reservoir and another concentric peelable (impermanent) heat seal between the membrane and the inner liner positioned underlying and at a radius not less than the first permanent heat seal, the heat seals and peelable barrier layer providing barriers that isolate the drug formulation from the adhesive.
摘要翻译： 一种透皮药物递送装置，其包括由背衬层和药物可渗透膜层限定的含药物制剂储存器，位于储存器下方的可剥离内衬层和位于储存器周边外部的背衬/膜的一部分，粘合剂层 位于膜/背衬层的内衬层和向外延伸部分之下的可剥离剥离衬垫层，以及位于粘合剂层下面的可剥离衬垫层，其中衬垫和膜周围围绕储存器的第一永久热密封，另一个同心可剥离（ 膜和内衬之间的热密封，其位于下方并且半径不小于第一永久热封，热密封和可剥离阻挡层提供将药物制剂与粘合剂隔离的障碍物。
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公开(公告)号：US4849224A
公开(公告)日：1989-07-18
申请号：US119617
申请日：1987-11-12
申请人： Yunik Chang , Dinesh C. Patel , Charles D. Ebert
发明人： Yunik Chang , Dinesh C. Patel , Charles D. Ebert
CPC分类号： A61K9/703 , A61K9/7084
摘要： A transdermal drug delivery device comprising a drug formulation-containing reservoir defined by a backing layer and a drug-permeable membrane layer, a ring-shaped layer made of an adhesive that is incompatible with one or more components of the drug formulation that is peripheral to the reservoir outwardly of the membrane layer and a peelable liner layer that underlies at least the membrane layer with a first heat seal between the backing and the membrane about the perimeter of the reservoir and another concentric heat seal between the backing and the release liner positioned outwardly of the first heat seal, the heat seals providing barriers that isolate the drug formulation from the adhesive.
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3.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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4.发明授权Subsaturated transdermal drug delivery device exhibiting enhanced drug flux 失效表现出增强的药物通量的亚饱和透皮药物递送装置
公开(公告)号：US5164190A
公开(公告)日：1992-11-17
申请号：US626685
申请日：1990-12-11
申请人： Dinesh C. Patel , Charles D. Ebert
发明人： Dinesh C. Patel , Charles D. Ebert
IPC分类号： A61K9/70
CPC分类号： A61K9/7061
摘要： Transdermal administration of hydrophobic drugs via a diffusion mechanism in which the drug is dissolved in a carrier at concentrations that are 20% to 80% of the saturation concentration. The flux of drug from the device is non-Fickian and is substantially greater than the flux observed when the drug is at saturation.
摘要翻译： 通过扩散机制透析给药疏水性药物，其中药物以浓度为饱和浓度的20％至80％的浓度溶解在载体中。 来自该装置的药物流量是非Fickian，并且显着大于当药物饱和时观察到的通量。
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5.发明授权Method for reducing skin irritation associated with drug/penetration enhancer compositions 失效减少与药物/渗透增强剂组合物相关的皮肤刺激的方法
公开(公告)号：US4855294A
公开(公告)日：1989-08-08
申请号：US240688
申请日：1988-09-06
申请人： Dinesh C. Patel , Charles D. Ebert
发明人： Dinesh C. Patel , Charles D. Ebert
CPC分类号： A61K47/12 , A61K31/047 , A61K47/10 , A61K47/14 , A61K47/20 , A61K47/22 , A61K9/0014 , Y10S514/947
摘要： A composition and method for reducing the skin irritation properties of a transdermal drug/enhancer composition which comprises incorporating into said composition, either prior to or at the time of application the skin, an effective amount of glycerin. When incorporated into the drug/enhancer composition prior to application to the skin the glycerin content will be between about 0.1 and 70 wt. %, preferably between about 1.0 and 50 wt. % and most preferably between about 5.0 and 20 wt. % of the composition.
摘要翻译： 一种用于降低透皮药物/增强剂组合物的皮肤刺激性质的组合物和方法，其包括在皮肤施用之前或施用时将所述组合物加入到所述组合物中，有效量的甘油。 当在施用于皮肤之前将其并入药物/增强剂组合物中时，甘油含量为约0.1-70重量％。 ％，优选约1.0至50wt。 ％，最优选约5.0至20wt。 ％的组成。
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6.发明授权公开(公告)号：US07081251B2
公开(公告)日：2006-07-25
申请号：US10731041
申请日：2003-12-08
IPC分类号： A61F13/00
CPC分类号： A61K9/0024 , A61K9/0014 , A61K9/0019 , A61K9/1647 , A61K9/7061 , A61K31/216 , A61K47/10 , A61K47/14 , A61K47/38 , A61K2300/00
摘要： The present invention provides compositions and methods for administering oxybutynin while minimizing the incidence and or severity of adverse drug experiences associated with oxybutynin therapy. In one aspect, these compositions and methods provide a lower plasma concentration of oxybutynin metabolites, such as N-desethyloxybutynin, which is presumed to be contributing at least in part to some of the adverse drug experiences, while maintaining sufficient oxybutynin plasma concentration to benefit a subject with oxybutynin therapy. The invention also provides isomers of oxybutynin and its metabolites that meet these characteristics of minimized incidence and/or severity of adverse drug experiences, and maintenance of beneficial and effective therapy for overactive bladder.
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7.发明授权公开(公告)号：US07081250B2
公开(公告)日：2006-07-25
申请号：US10731040
申请日：2003-12-08
IPC分类号： A61F13/00
CPC分类号： A61K9/0024 , A61K9/0014 , A61K9/0019 , A61K9/1647 , A61K9/7061 , A61K31/216 , A61K47/10 , A61K47/14 , A61K47/38 , A61K2300/00
摘要： The present invention provides compositions and methods for administering oxybutynin while minimizing the incidence and or severity of adverse drug experiences associated with oxybutynin therapy. In one aspect, these compositions and methods provide a lower plasma concentration of oxybutynin metabolites, such as N-desethyloxybutynin, which is presumed to be contributing at least in part to some of the adverse drug experiences, while maintaining sufficient oxybutynin plasma concentration to benefit a subject with oxybutynin therapy. The invention also provides isomers of oxybutynin and its metabolites that meet these characteristics of minimized incidence and/or severity of adverse drug experiences, and maintenance of beneficial and effective therapy for overactive bladder.
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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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公开(公告)号：US5212199A
公开(公告)日：1993-05-18
申请号：US871643
申请日：1992-04-21
申请人： Sonia Heiber , Dinesh Patel , Charles D. Ebert
发明人： Sonia Heiber , Dinesh Patel , Charles D. Ebert
CPC分类号： A61K9/703 , A61K47/26 , A61K9/0014 , A61K9/7061 , Y10S514/946 , Y10S514/947
摘要： Skin permeation enhancer compositions are provided which increase the permeability of skin to transdermally administered pharmacologically active agents. The compositions contain a sorbitan ester in addition to the selected pharmacologically active agent, and may also contain a C.sub.1 -C.sub.4 aliphatic alcohol. Methods and transdermal drug delivery systems for using the compositions are also provided.
摘要翻译： 提供了皮肤渗透增强剂组合物，其增加皮肤对透皮给药的药理学活性剂的渗透性。 该组合物除了所选择的药理学活性剂外还含有脱水山梨醇酯，并且还可以含有C 1 -C 4脂族醇。 还提供了用于使用组合物的方法和透皮药物递送系统。
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公开(公告)号：US07179483B2
公开(公告)日：2007-02-20
申请号：US10913019
申请日：2004-08-06
CPC分类号： A61K31/216 , A61F2013/00646 , A61K9/0014 , A61K9/0019 , A61K9/0024 , A61K9/06 , A61K9/1647 , A61K9/7061 , A61K47/10 , A61K47/14 , A61K47/38 , A61K2300/00
摘要： The present invention provides compositions and methods for administering oxybutynin while minimizing the incidence and or severity of adverse drug experiences associated with oxybutynin therapy. In one aspect, these compositions and methods provide a lower plasma concentration of oxybutynin metabolites, such as N-desethyloxybutynin, which is presumed to be contributing at least in part to some of the adverse drug experiences, while maintaining sufficient oxybutynin plasma concentration to benefit a subject with oxybutynin therapy. The invention also provides isomers of oxybutynin and its metabolites that meet these characteristics of minimized incidence and/or severity of adverse drug experiences, and maintenance of beneficial and effective therapy for overactive bladder. In some aspects, the composition may be presented in the form of an unoccluded or free form topically administered gel.
摘要翻译： 本发明提供了用于奥昔布宁的组合物和方法，同时最小化与奥昔布宁治疗相关的不良药物经历的发生率和/或严重程度。 在一个方面，这些组合物和方法提供了较低的奥昔布宁代谢物的血浆浓度，例如N-去乙氧基丁啶，其被推定为至少部分地促成一些不良药物经历，同时保持足够的奥昔布宁血浆浓度以有益于 奥昔布宁治疗。 本发明还提供了符合以下特征的奥昔布宁及其代谢物的异构体，这些特征使不良药物经历的发生率和/或严重程度最小化，以及维持膀胱过度活动症的有益和有效治疗。 在一些方面，组合物可以呈局部施用凝胶的未被包裹或游离形式存在。
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