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    • 1. 发明申请
    • TRANSDERMAL THERAPEUTIC SYSTEM WITH TWO-PHASE RELEASING PROFILE
    • 透皮治疗系统两相释放曲线
    • WO2008043601A3
    • 2008-06-12
    • PCT/EP2007058867
    • 2007-08-27
    • AXXONIS PHARMA AGTACK JOHANNESSCHURAD BJOERNMUELLER-SCHUBERT ANTJEHOROWSKI REINHARD
    • TACK JOHANNESSCHURAD BJOERNMUELLER-SCHUBERT ANTJEHOROWSKI REINHARD
    • A61K9/70A61K47/06A61K47/10A61K47/16A61K47/32A61K47/44C07D457/00
    • A61K9/7061A61K31/48
    • The present invention relates to a transdermal therapeutic system (TTS) comprising an impermeable covering layer, a matrix containing an ergolin compound of formula (I) or the physiologically compatible salt or derivative thereof, wherein R 1 represents an H atom or a halogen atom and R 2 an alkyl group with 1 to 4 carbon atoms and ------ a single or double bond, and a removable protective layer, the ergolin compound or the physiologically compatible salt or derivative thereof being stabilized by an antioxidant and a basic polymer. The TTS is characterized in that the matrix contains at least one hydrocarbon having 8 to 18 carbon atoms in a linear or branched chain and carrying a functional group at the end of the alkyl chain, and/or aloe vera oil so that, in a first phase (0-5 hours after application), only 0 to 20 % of the therapeutically desired steady state plasma concentration of the ergolin compound is achieved and, in a second phase (5-20 hours after application), the therapeutically desired steady state plasma concentration of the ergolin compound is achieved.
    • 本发明涉及一种经皮治疗系统(TTS)由不可渗透的覆盖层的湿润剂,式(I)或其生理上可接受的盐或衍生物矩阵,其中R 1 是一个氢原子或一个麦角灵 一个卤原子,R 2 是具有碳原子数1〜4的烷基,以及-----是单键或双键,和一个可去除的保护层,其中所述麦角灵化合物或生理学上可接受的盐或衍生物的抗氧化剂 和碱性聚合物是稳定的。 的TTS的特征在于,在基体中,都包括从在烷基链和/或芦荟油的端部携带的官能团在直链或支链8-18个碳原子的具有至少一个烃,使得在第一阶段中 只有0-20%的麦角灵化合物的治疗所需的稳态血浆浓度的实现(应用0-5小时后),且仅在一个第二阶段(给药后5-20小时),麦角灵化合物的治疗期望的稳态血浆浓度达到 ,