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    • 1. 发明申请
    • Transdermal absorption preparation
    • 透皮吸收制剂
    • US20060188554A1
    • 2006-08-24
    • US10566502
    • 2004-08-03
    • Katashi NakashimaSatoshi OhmoriNorihiro KanayamaYoshiki Sakai
    • Katashi NakashimaSatoshi OhmoriNorihiro KanayamaYoshiki Sakai
    • A61K31/445A61K31/4164A61F13/02
    • A61K9/7053A61K9/7076A61K31/4174
    • (Object) A transdermal preparation is provided, which ensures stable and effective absorption of 4-(2-methyl-1-imidazolyl)-2,2-diphenylbutylamide (KRP-197) which has a low skin absorption and is a bladder-selective muscarinic M3 and M1 receptor antagonist, into body through the skin while causing little side effects and providing sustained pharmacological effect with less skin irritancy. (Solving means) A composition comprising KRP-197 and an external preparation base is deposited and dried onto a structural body or a small pool of the composition is deposited on the structural body to obtain a single adhesive layer-type transdermal preparation or a reservoir-type transdermal preparation. These preparations can ensure high permeation of KRP-197 through the skin and sustained absorption of KRP-197 into body while causing decreased skin irritancy.
    • (对象)提供透皮制剂,其确保具有低皮肤吸收性并且是膀胱选择性的4-(2-甲基-1-咪唑基)-2,2-二苯基丁基酰胺(KRP-197)的稳定和有效的吸收 毒蕈碱M3和M1受体拮抗剂通过皮肤进入体内,同时引起少量副作用,并提供持久的药理作用,皮肤刺激性较小。 (解决方法)将包含KRP-197和外部制剂基质的组合物沉积并干燥到结构体上,或将组合物的小池沉积在结构体上,以获得单一粘合剂层型透皮制剂或储液器 - 型透皮制剂。 这些制剂可以确保KRP-197通过皮肤的高渗透和KRP-197持续吸收到体内,同时引起皮肤刺激性降低。