申请人:——
公开号:US05162315A1
公开(公告)日:1992-11-10
Pharmaceutical compositions for enhancing absorption of a topically administered formulation through dermal or mucosal membrane, for local or systemic application, comprising one or more agents of formula I: ##STR1## where: R is a saturated or unsaturated, straight or branched, cyclic or acyclic hydrocarbon group with from 1 to 19 carbon atoms or an alkoxyalkyl group; n is 2-20; X is selected from H, OR.sub.2 or NR.sub.2 R.sub.3 ; wherein R.sub.1, R.sub.2 and R.sub.3 are independently selected from H, alkyl, haloalkyl, acyl, carbalkoxy, carbalkoxyalkyl, hydroyalkyl, acyloxyalkyl, alkoxyalkyl, aminoalkyl- and acylaminoalkyl; i) with the proviso that when n is 2, X is OR.sub.2 and R.sub.2 is H, then R.sub.1 is not hydroxyalkyl, specifically, 2-hydroxyethyl; and ii) with the proviso that when n is 2 and X is NR.sub.2 R.sub.3, then R.sub.1 and R.sub.2 may combine to form a heterocyclic ring and R.sub.3 is not acyl; and iii) with the proviso that when X is NR.sub.2 R.sub.3, then R.sub.2 and R.sub.3 may combine to form a heterocyclic ring; iv) with the proviso that when R is an alkoxyalkyl group then X may be hydrogen and when X is not hydrogen, and v) with the proviso that when X is H, R is not alkyl and R.sub.1 is not H and alkyl then R.sub.1 and X may combine to form heterocyclic ring and methods of using the same are disclosed.
用于增强经皮或粘膜膜局部或全身应用的局部制剂吸收的药物组合物,包括一个或多个式I的药剂:##STR1## 其中:R是具有1至19个碳原子的饱和或不饱和,直链或支链,环状或非环状的碳氢基团或烷氧基烷基团;n为2-20;X选自H,OR.sub.2或NR.sub.2 R.sub.3;其中R.sub.1,R.sub.2和R.sub.3独立地选自H,烷基,卤代烷基,酰基,羧烷氧基,羧烷氧基烷基,羟基烷基,酰氧基烷基,烷氧基烷基,氨基烷基和酰胺基烷基;i)当n为2,X为OR.sub.2且R.sub.2为H时,R.sub.1不是羟基烷基,特别是2-羟基乙基;ii)当n为2且X为NR.sub.2 R.sub.3时,R.sub.1和R.sub.2可以结合形成杂环环,并且R.sub.3不是酰基;iii)当X为NR.sub.2 R.sub.3时,R.sub.2和R.sub.3可以结合形成杂环环;iv)当R为烷氧基烷基团时,X可以是氢,当X不是氢时;v)当X为H时,R不是烷基且R.sub.1不是H和烷基,则R.sub.1和X可以结合形成杂环环。公开了使用该组合物的方法。