Reduction of skin irritation and resistance during electrotransport
    1.
    发明授权
    Reduction of skin irritation and resistance during electrotransport 失效
    减少皮肤刺激和电传输期间的抵抗力

    公开(公告)号:US5624415A

    公开(公告)日:1997-04-29

    申请号:US427336

    申请日:1995-04-24

    IPC分类号: A61N1/30

    摘要: An electrotransport delivery device utilizing reservoir buffering at a select pH ranges in order to reduce skin irritation and skin resistance is provided. Cathodic reservoirs are buffered to a pH of less than about 4, preferably to a pH in the range of about 2 to 4, while anodic reservoirs are buffered to a pH above about 4, preferably to a pH in the range of about 4 to 10. Another electrotransport delivery device utilizes a potassium sensor to monitor potassium efflux from the skin. Potassium efflux above a certain predetermined level has been found to be a precursor to skin irritation/erythema. Operation of the device is modified (eg, terminated) when the predetermined potassium efflux level is sensed.

    摘要翻译: 提供了一种在选择的pH范围内利用储存器缓冲以便减少皮肤刺激和皮肤抵抗的电输送输送装置。 阴极储存器缓冲至小于约4的pH,优选至约2至4范围内的pH,而阳极储存器缓冲至高于约4,优选至约4至10范围内的pH 另一种电输送装置利用钾传感器来监测来自皮肤的钾流出。 已经发现高于某一预定水平的钾流出物是皮肤刺激/红斑的前体。 当检测到预定的钾流出水平时,装置的操作被修改(例如,终止)。

    Reduction or prevention of sensitization to drugs
    3.
    发明授权
    Reduction or prevention of sensitization to drugs 失效
    减少或预防对药物的敏感性

    公开(公告)号:US5149539A

    公开(公告)日:1992-09-22

    申请号:US793936

    申请日:1991-11-15

    IPC分类号: A61K9/70 A61K33/02

    CPC分类号: A61K9/7023 A61K33/02

    摘要: The present invention is directed to a method of reducing or preventing skin sensitization by inhibiting the immunological processing of a sensitizing drug as an antigen. The drug is sensitizing to humans, i.e., the drug is susceptible to inducing skin or mucosa sensitization in a human when the drug is transdermally administered to the human at a therapeutically effective rate. Skin sensitization reduction or prevention is induced by coadministering to the skin or mucosa of the human:(a) a therapeutically effective amount of a sensitizing drug, at a therapeutically effective rate over a predetermined period of time; and(b) an antigen processing-inhibiting agent in an amount effective to inhibit the antigen processing of the drug.The system of the invention comprises a matrix adapted to be placed in sensitizing drug and antigen processing-inhibiting agent transmitting relation to the selected skin or mucosa site. The matrix contains sufficient amounts of the drug and the agent to continuously coadminister to the skin or mucosa site the drug, at a therapeutically effective rate and over a predetermined delivery period, and the antigen processing-inhibiting agent, at a rate and for a period of time sufficient to inhibit the processing of the drug as an antigen.

    摘要翻译: 本发明涉及通过抑制作为抗原的敏化药物的免疫处理来减少或预防皮肤致敏的方法。 药物对人类敏感,即当药物以治疗有效的速率经皮给药时,药物易于引起人类皮肤或粘膜致敏。 通过向人的皮肤或粘膜共同诱导皮肤致敏减少或预防:(a)治疗有效量的敏化药物,以预定时间段的治疗有效速率; 和(b)有效抑制药物抗原加工的抗原加工抑制剂。 本发明的系统包括适于放置在致敏药物和抗原加工抑制剂中的基质,其与所选择的皮肤或粘膜部位传递关系。 基质含有足够量的药物和药剂,以治疗有效速率和超过预定的递送期间,以一定的速率和一段时间连续地连续地附着到皮肤或粘膜部位,药物,抗原加工抑制剂 的时间足以抑制作为抗原的药物的加工。

    Reduction or prevention of skin irritation by drugs
    5.
    发明授权
    Reduction or prevention of skin irritation by drugs 失效
    减少或预防药物引起的皮肤刺激

    公开(公告)号:US5130139A

    公开(公告)日:1992-07-14

    申请号:US549584

    申请日:1990-07-06

    摘要: The present invention provides a method of reducing or preventing skin irritation of a weak base drug by inhibiting the accumulation of the drug in the lysosomes. The drug is irritating to humans, i.e., the drug is susceptible to inducing skin or mucosa irritation in a human when the drug is transdermally administered to the human at a therapeutically effective rate. Irritation reduction or prevention is induced by coadministering to the skin or mucosa of the human:(a) a therapeutically effective amount of a weak base drug which is irritating to humans, at a therapeutically effective rate over a predetermined period of time; and(b) an effective amount of an agent capable of inhibiting the lysosomal uptake of the drug to reduce or prevent irritation to the skin or mucosa.

    摘要翻译: 本发明提供了通过抑制药物在溶酶体中的积累来减少或预防弱碱性药物的皮肤刺激的方法。 该药物对人类有刺激性,即当药物以治疗有效率透皮给药时,该药物易于引起人体皮肤或粘膜刺激。 通过向人的皮肤或粘膜共同诱导刺激减少或预防:(a)在预定时间段内以治疗有效速率治疗有效量的对人类有刺激性的弱碱性药物; 和(b)有效量的能够抑制药物的溶酶体摄取以减少或防止对皮肤或粘膜的刺激​​的药剂。

    Reduction or prevention of skin irritation by drugs
    8.
    发明授权
    Reduction or prevention of skin irritation by drugs 失效
    减少或预防药物对皮肤的刺激

    公开(公告)号:US5160741A

    公开(公告)日:1992-11-03

    申请号:US793932

    申请日:1991-11-13

    IPC分类号: A61K47/02 A61K47/18

    摘要: The present invention provides a method of reducing or preventing skin irritation of a weak base drug by inhibiting the accumulation of the drug in the lysosomes. The drug is irritating to humans, i.e., the drug is susceptible to inducing skin or mucosa irritation in a human when the drug is transdermally administered to the human at a therapeutically effective rate. Irritation reduction or prevention is induced by coadministering to the skin or mucosa of the human:(a) a therapeutically effective amount of a weak base drug which is irritating to humans, at a therapeutically effective rate over a predetermined period of time; and(b) an effective amount of an agent capable of inhibiting the lysosomal uptake of the drug to reduce or prevent irritation to the skin or mucosa.

    摘要翻译: 本发明提供了通过抑制药物在溶酶体中的积累来减少或预防弱碱性药物的皮肤刺激的方法。 该药物对人类有刺激性,即当药物以治疗有效率透皮给药时,该药物易于引起人体皮肤或粘膜刺激。 通过向人的皮肤或粘膜共同诱导刺激减少或预防:(a)在预定时间段内以治疗有效速率治疗有效量的对人类有刺激性的弱碱性药物; 和(b)有效量的能够抑制药物的溶酶体摄取以减少或防止对皮肤或粘膜的刺激​​的药剂。

    Reduction of skin irritation during electrotransport delivery
    9.
    发明授权
    Reduction of skin irritation during electrotransport delivery 失效
    电运输期间减少皮肤刺激

    公开(公告)号:US5865792A

    公开(公告)日:1999-02-02

    申请号:US895096

    申请日:1997-07-16

    IPC分类号: A61N1/30 A61N1/32

    摘要: The invention is directed to a composition and product for use in an electrotransport device. The composition includes an ionized drug, an anti-inflammatory agent and a solvent. Preferably, the anti-inflammatory agent is hydrocortisone or esters thereof, and the solvent is an alcohol, a glycol, a glycerol, a cyclodextrin, a nonionic surfactant or mixtures thereof. The composition preferably further includes a gel matrix that is a swellable, hydrophilic polymer, a water soluble hydrophilic polymer or a solid polymer. A hydrophobic polymer and/or additives may also be included.

    摘要翻译: 本发明涉及一种用于电输送装置的组合物和产品。 组合物包括电离药物,抗炎剂和溶剂。 优选地,抗炎剂是氢化可的松或其酯,溶剂是醇,二醇,甘油,环糊精,非离子表面活性剂或其混合物。 组合物优选还包括可溶胀亲水性聚合物,水溶性亲水聚合物或固体聚合物的凝胶基质。 还可以包括疏水性聚合物和/或添加剂。

    Reduction or prevention of skin irritation or sensitization during
transdermal administration of a irritating or sensitizing drug
    10.
    发明授权
    Reduction or prevention of skin irritation or sensitization during transdermal administration of a irritating or sensitizing drug 失效
    在透皮给药刺激性或致敏性药物时减少或预防皮肤刺激或致敏

    公开(公告)号:US5451407A

    公开(公告)日:1995-09-19

    申请号:US63176

    申请日:1993-06-21

    IPC分类号: A61K9/70 A61K47/22 A61F13/00

    摘要: The present invention is directed to the transdermal administration of methyl nicotinate and an irritating or sensitizing drug. The invention includes a transdermal drug delivery device comprising a matrix adapted to be placed in irritating/sensitizing drug- and methyl nicotinate-transmitting relation with the skin site. The matrix contains sufficient amounts of irritating/sensitizing drug and of methyl nicotinate, in combination, to continuously administer to the skin for a predetermined period of time the drug to provide an effective therapeutic result. The invention is also directed to a method for either 1) preventing or reducing the irritation caused by an irritating drug or 2) preventing or reducing sensitization from occurring, as well as reducing or eliminating pain and discomfort occurring during the elicitation phase after sensitization has already been induced.

    摘要翻译: 本发明涉及透明给药烟酸甲酯和刺激性或致敏药物。 本发明包括透皮药物递送装置,其包含适于与皮肤部位置于刺激/敏化药物和甲基烟酸酯传递关系中的基质。 基质含有足量的刺激性/致敏药物和烟酸甲酯组合,以持续给予皮肤预定的时间以提供有效的治疗结果。 本发明还涉及以下方法:1)预防或减少由刺激性药物引起的刺激或2)预防或减少致敏发生,以及减轻或消除致敏期间在引发阶段中发生的疼痛和不适 被诱导。