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    • 1. 发明申请
    • CHOLINESTERASE INHIBITORS IN LIPOSOMES AND THEIR PRODUCTION AND USE
    • 在脂质体胆碱酯酶抑制剂及其制备方法和用途
    • WO2005102268A3
    • 2006-04-06
    • PCT/AT2005000138
    • 2005-04-21
    • SANOCHEMIA PHARMAZEUTIKA AGBODENTEICH ANGELIKABOECKMANN JOSEFFRANTSITS WERNERPIRICH EBERHARD
    • BODENTEICH ANGELIKABOECKMANN JOSEFFRANTSITS WERNERPIRICH EBERHARD
    • A61K9/127A61K9/00
    • A61K9/127
    • The invention relates to a pharmaceutical composition based on an active ingredient that is enclosed in liposomes for topical, transdermal application. The interior of said liposomes comprises an acidic, aqueous medium containing at least one cholinesterase inhibitor, preferably from the group containing donepezil, rivastigmine, galantamine, physostigmine, heptylphysostigmine, phenserine, tolserine, cymserine, thiatolserine, thiacymserine, neostigmine, huperzine, tacrine, metrifonate and dichlorvos, or an enantiomer or derivative of at least one of said compounds. In addition, the invention relates to a method for producing said composition, optionally in a sterile form and also to the use of the liposomes charged with the active ingredient in various galenic formulations for topical, transdermal application with a depot effect in the epidermis, for the prophylaxis and/or treatment of cutaneous neuropathic pain or the loss of cutaneous sensory function as a result of neuropathy.
    • 本发明涉及一种用于局部,经皮应用的脂质体包埋的剂的基础上的药物组合物,其中所述脂质体具有在其内部的酸性含水环境和在至少一种胆碱酯酶抑制剂,优选选自多奈哌齐,利凡斯的明 ,加兰他敏,毒扁豆碱,heptylphysostigmine,phenserine,Tolserin,cymserine,Thiatolserin,Thiacymserin,新斯的明,石杉碱甲,他克林,美曲膦酯和敌敌畏,或其对映体或其衍生物,这些化合物中的至少一种。 本发明还涉及一种方法,用于制备该组合物,任选以无菌形式,以及利用在用于与在表皮贮库效应局部透皮应用的各种盖伦制剂装载药物的脂质体,用于预防和/或治疗的皮肤神经性疼痛或 皮肤感觉功能的neurophatiebedingten损失。