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Method and composition for promoting skin penetration of a drug using a penetration promoting agent when the drug and / or penetration promoting agent is unstable during long-term compound storage

机译:当药物和/或渗透促进剂在长期化合物贮存期间不稳定时,使用渗透促进剂促进皮肤渗透的方法和组合物

摘要

The present invention relates to a method for promoting epidermal, transdermal and dermal penetration of a topical pharmaceutical active agent (such as a drug or a medicament) which causes poor skin permeability in the absence of a penetration enhancer and causes decomposition due to instability during long-term storage with a specific penetration promoter, /RTI Also provided according to the present invention are methods and means for increasing the penetration of a pharmacologically active agent that destabilizes and degrades the penetration enhancer when the skin penetration rate is low and is compounded with a long-term skin penetrant. According to the present invention, one or more second compositions comprising at least one first composition containing a drug, a pharmaceutically acceptable salt thereof, a chemical derivative or combination thereof, and a penetration enhancer in an acceptable carrier, among the dermatologically acceptable carriers, . These compositions are physically isolated from each other until they are applied locally, simultaneously or in a short period of time to the body or skin surface, and are mixed and preferably formed into the final active composition on the skin. In addition, a premix of these compositions may be made according to the invention and applied to the skin. According to the present invention, the drug can be delivered in a therapeutically effective amount to the skin and systemic circulation system, and the penetration rate of the drug, which usually has poor skin penetration rate, can be remarkably increased by the action of the penetration promoter in the active composition.
机译:本发明涉及促进局部药物活性剂(例如药物或药物)的表皮,透皮和真皮渗透的方法,该药物活性剂在缺乏渗透促进剂的情况下导致皮肤渗透性差并且由于长期的不稳定性而引起分解。根据特定的渗透促进剂的长期储存,根据本发明还提供了用于增加药理学活性剂的渗透的方法和手段,当皮肤渗透率低并且复合时,该药理活性剂会破坏并降低渗透促进剂。具有长期的皮肤渗透性。根据本发明,在皮肤病学上可接受的载体中,一种或多种第二组合物包括至少一种包含药物,其药学上可接受的盐,其化学衍生物或它们的组合,以及渗透增强剂的第一组合物。这些组合物彼此物理隔离,直到将它们局部,同时或在短时间内施用于身体或皮肤表面,然后混合并优选在皮肤上形成最终的活性组合物。另外,可以根据本发明制备这些组合物的预混合物并将其施加到皮肤上。根据本发明,可以以治疗有效量将药物递送至皮肤和全身循环系统,并且通常通过皮肤的渗透率较差的药物的渗透率可以通过渗透的作用而显着提高。活性组合物中的启动子。

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