Reduction of skin reactions caused by transdermal drug delivery
    8.
    发明授权
    Reduction of skin reactions caused by transdermal drug delivery 失效
    减少透皮给药引起的皮肤反应

    公开(公告)号:US06203817B1

    公开(公告)日:2001-03-20

    申请号:US09092606

    申请日:1998-06-05

    IPC分类号: A61F1302

    CPC分类号: A61K9/7053 A61K9/7084

    摘要: Transdermal compositions, devices, and methods for the administration of a drug at reduced skin irritation levels are disclosed. More particularly, this invention relates to novel methods, compositions, and devices for the reduction or elimination of irritation or sensitization caused by an irritating or sensitizing drug when it is delivered transdermally. According to a preferred embodiment, transdermal administration of a drug salt of a non-zwitterionic drug is disclosed wherein the drug salt comprises a combination of surface activity and a low octanol-water partition coefficient. Such drug salts have been found to reduce irritation or sensitization to the drug being delivered while achieving therapeutically effective transdermal fluxes.

    摘要翻译: 公开了用于在皮肤刺激水平降低的药物给药的透皮组合物,装置和方法。 更具体地说,本发明涉及当通过皮肤递送时由刺激性或致敏性药物引起的刺激或致敏的减少或消除的新方法,组合物和装置。 根据优选的实施方案,公开了非两性离子药物的药物盐的透皮给药,其中所述药物盐包含表面活性和低辛醇 - 水分配系数的组合。 已经发现,这些药物盐可以减少对所递送药物的刺激或致敏,同时实现治疗有效的经皮通气。

    Reduction of skin irritation and resistance during electrotransport
    9.
    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 skin irritation by drugs
    10.
    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。