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公开(公告)号：EP0268222A2
公开(公告)日：1988-05-25
申请号：EP87116757.3
申请日：1987-11-13
IPC分类号： A61K47/00
CPC分类号： A01N25/02 , A01N37/18 , A01N43/60 , A61K9/0014 , A61K47/22 , C07D295/185 , D06M16/00 , D06P1/6426 , Y10S514/946 , Y10S514/947
摘要： This invention relates to a method for administering systemically active agents including therapeutic agents through the skin or mucosal membranes of humans and animals in a transdermal device or formulation comprising topically administering with said systemic agent an effective amount of a membrane penetration enhancer having the structural formula
wherein X may represent sulfur, oxygen or nitrogen; a and b may be 0 or 1, c may be 0, 1 or 2, except that when X is oxygen, a, b and c are 0, when X is nitrogen c is 0 and only one of a or b is 1, and when X is sulfur a and b are0; A is a branched or a straight chain, divalent aliphatic radical having from 0 to 2 double bonds; Rʹ is selected from the group consisting of H, a lower alkyl group having from 1 to 4 carbon atoms, phenyl, lower alkyl or halogen substituted phenyl, acetamido, halogen, piperidinyl, lower alkyl or halogen substituted piperidinyl, carbalkoxy, carboxamide, and alkanoyl; and R is hydrogen or a lower alkyl group having from 1 to 4 carbon atoms,
wherein Rʺ is H or halogen, and salts, e.g. acid or quaternary derivatives, thereof. These compositions are useful in topical or transdermal applications of the physiologically-active agent.摘要翻译： 本发明涉及一种在透皮装置或制剂中通过人和动物的皮肤或粘膜给予全身活性剂包括治疗剂的方法，所述方法包括向所述全身剂局部给药有效量的具有下列结构式的膜渗透促进剂：其中 X可以代表硫，氧或氮; a和b可以是0或1，c可以是0,1或2，除了当X是氧时，a，b和c是0时，当X是氮时，c是0且a或b中只有一个是1， 当X是硫时，a和b是0; A是具有0至2个双键的支链或直链二价脂族基团; R'选自H，具有1至4个碳原子的低级烷基，苯基，低级烷基或卤素取代的苯基，乙酰氨基，卤素，哌啶基，低级烷基或卤素取代的哌啶基，烷氧羰基，羧酰胺和烷酰基 ; 并且R是氢或具有1至4个碳原子的低级烷基，其中R“是H或卤素，和盐， 酸或季铵衍生物。 这些组合物可用于生理活性剂的局部或透皮应用。
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公开(公告)号：EP0268222B1
公开(公告)日：1996-03-27
申请号：EP87116757.3
申请日：1987-11-13
IPC分类号： A61K47/00
CPC分类号： A01N25/02 , A01N37/18 , A01N43/60 , A61K9/0014 , A61K47/22 , C07D295/185 , D06M16/00 , D06P1/6426 , Y10S514/946 , Y10S514/947
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