Subsaturated transdermal drug delivery device exhibiting enhanced drug
flux
    21.
    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

    CPC classification number: A61K9/7061

    Abstract: 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.

    Abstract translation: 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。

    Sorbitan esters as skin permeation enhancers
    22.
    发明授权
    Sorbitan esters as skin permeation enhancers 失效
    山梨糖醇酯作为皮肤渗透促进剂

    公开(公告)号:US5122383A

    公开(公告)日:1992-06-16

    申请号:US702043

    申请日:1991-05-17

    CPC classification number: A61K9/703 A61K47/26 A61K9/0014 A61K9/7061

    Abstract: 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.

    Abstract translation: 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。

    Unoccluded topical oxybutynin gel composition and methods for transdermal oxybutynin therapy
    23.
    发明授权
    Unoccluded topical oxybutynin gel composition and methods for transdermal oxybutynin therapy 有权
    未包括的局部奥昔布宁凝胶组合物和透皮奥昔布宁治疗方法

    公开(公告)号:US08241662B2

    公开(公告)日:2012-08-14

    申请号:US11645076

    申请日:2006-12-21

    Abstract: 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.

    Abstract translation: 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。

    Compositions and Methods for Transdermal Oxybutynin Therapy
    24.
    发明申请
    Compositions and Methods for Transdermal Oxybutynin Therapy 审中-公开
    经皮奥昔布宁治疗的组合和方法

    公开(公告)号:US20090018190A1

    公开(公告)日:2009-01-15

    申请号:US12236585

    申请日:2008-09-24

    Abstract: 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.

    Abstract translation: 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。

    Device for administering an active agent to the skin or mucosa
    26.
    发明授权
    Device for administering an active agent to the skin or mucosa 失效
    用于向皮肤或粘膜施用活性剂的装置

    公开(公告)号:US4983395A

    公开(公告)日:1991-01-08

    申请号:US326536

    申请日:1989-03-21

    CPC classification number: A61K9/703 A61K9/7084

    Abstract: 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.

    Abstract translation: 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。

    Transdermal administration of a systemic active agent to a premature
neonatal infant
    29.
    发明授权
    Transdermal administration of a systemic active agent to a premature neonatal infant 失效
    将全身活性剂透皮给药给早产新生儿

    公开(公告)号:US4853227A

    公开(公告)日:1989-08-01

    申请号:US112917

    申请日:1987-10-23

    CPC classification number: A61M35/00 A61K9/7023

    Abstract: A method of treating a premature neonatal infant of a gestational age between about 24 and about 35 weeks with a pharmaceutically acceptable, systemically active, substantially skin compatible, water-soluble neonatal therapeutic agent having a molecular weight below about 5000, and which agent is substantially non-transmissable through normal mature intact human skin, comprising:(a) applying to the intact neonatal skin of said infant a transdermal device comprising (i) a backing member, (ii) a substantially shape retaining hydrogel reservoir having a water content of between about 5 percent and about 95 percent preferably between 10 percent and 80 percent by weight of said reservoir and containing an effective amount of said agent, (iii) a skin contacting surface of predetermined area, and (iv) means for maintaining said reservoir in material transmitting relationship to said skin;(b) maintaining said skin contacting surface of said device in material transmitting relationship to said intact neonatal skin of the infant for an extended period of time; and(c) delivering said agent through the intact neonatal skin in a controlled continuous manner such that the blood plasma level of said agent is substantially within the therapeutic index of said agent for a majority of said extended period of time.

    Abstract translation: 一种在约24至约35周之间用具有分子量低于约5000的药学上可接受的,系统活性的,基本上与皮肤相容的水溶性新生儿治疗剂来治疗胎龄较早的新生儿婴儿的方法, 包括:(a)向所述婴儿的完整的新生儿皮肤施用透皮装置,其包括(i)背衬构件,(ii)基本上保持形状的水凝胶储存器,其水含量介于 约5%至约95%,优选10%至80%,并含有有效量的所述试剂,(iii)预定面积的皮肤接触表面,和(iv)用于将所述储存器保持在材料中的装置 传递与所述皮肤的关系; (b)将所述装置的所述皮肤接触表面与所述婴儿的所述完整的新生儿皮肤的材料传播关系延长一段时间; 和(c)以受控的连续方式将所述药剂输送穿过完整的新生儿皮肤,使得所述药剂的血浆水平基本上在所述药剂的治疗指数中大部分所述延长的一段时间。

    Device for administering an active agent to the skin or mucosa
    30.
    发明授权
    Device for administering an active agent to the skin or mucosa 失效
    用于向皮肤或粘膜施用活性剂的装置

    公开(公告)号:US4849224A

    公开(公告)日:1989-07-18

    申请号:US119617

    申请日:1987-11-12

    CPC classification number: A61K9/703 A61K9/7084

    Abstract: 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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