Transdermal Compositions Comprising an Active Agent Layer and An Active Agent Conversion Layer

Abstract

Transdermal compositions are provided. Aspects of the transdermal compositions include: an active agent layer and a conversion layer, where the conversion layer includes a weak base and, optionally, a carboxylated component. Also provided are methods of using the transdermal compositions and kits containing the transdermal compositions.

What is claimed is: 
     
         1 . A transdermal composition comprising:
 an active agent layer comprising an active agent in a matrix; and   a conversion layer comprising a weak base in a matrix.   
     
     
         2 . The transdermal composition according to  claim 1 , wherein the conversion layer comprises a carboxylated component. 
     
     
         3 . The transdermal composition according to  claim 1 , wherein the active agent is present as a salt. 
     
     
         4 . The transdermal composition according to  claim 3 , wherein the active agent is a propynylaminoindan. 
     
     
         5 . The transdermal composition according to  claim 4 , wherein the propynylaminoindan is N-propargyl-1-aminoindan. 
     
     
         6 . The transdermal composition according to  claim 1 , wherein the carboxylated component of the conversion layer is an acrylic carboxylated polymer. 
     
     
         7 . The transdermal composition according to  claim 6 , wherein the acrylic carboxylate polymer is the acrylic carboxylate polymer present in DuroTak® 87-2100 pressure-sensitive adhesive. 
     
     
         8 . The transdermal composition according to  claim 1 , wherein the carboxylated component of the conversion layer is a low molecular weight organic acid. 
     
     
         9 . The transdermal composition according to  claim 8 , wherein the low molecular weight organic acid is acetic acid. 
     
     
         10 . The transdermal composition according to  claim 1 , wherein the weak base of the conversion layer is a cationic acrylic copolymer. 
     
     
         11 . The transdermal composition according to  claim 10 , wherein the cationic acrylic copolymer is an aminated methacrylate copolymer. 
     
     
         12 . The transdermal composition according to  claim 11 , wherein the aminated methacrylate copolymer is a copolymer of diethylaminoethyl methacrylate, butyl methacrylate and methyl methacrylate. 
     
     
         13 . The transdermal composition according to  claim 12 , wherein the aminated methacrylate copolymer is Eudragit® E100 aminated methacrylate copolymer. 
     
     
         14 . The transdermal composition according to  claim 1 , wherein the matrix of the active agent layer comprises a carboxylated polymer. 
     
     
         15 . The transdermal composition according to  claim 1 , wherein the transdermal composition comprises a pressure sensitive adhesive. 
     
     
         16 . The transdermal composition according to  claim 1 , wherein the transdermal composition comprises a permeation enhancer. 
     
     
         17 . The transdermal composition according to  claim 1 , wherein the transdermal composition comprises a rate-controlling layer between the active agent layer and the active agent conversion layer. 
     
     
         18 . The transdermal composition according to  claim 1 , wherein the composition comprises at least one additional layer. 
     
     
         19 . The transdermal composition according to  claim 1 , wherein the transdermal composition exhibits a constant flux of the active agent over an extended period of time. 
     
     
         20 . A method comprising:
 applying to a skin surface of a subject a transdermal composition comprising:
 an active agent layer comprising an active agent in a matrix; and 
 a conversion layer comprising a weak base in a matrix; 
   in a manner sufficient to achieve a constant flux of the active agent over an extended period of time.   
     
     
         21 . The method according to  claim 20 , wherein the extended period of time is 72 hours or longer. 
     
     
         22 . The method according to  claim 20 , wherein the conversion layer comprises a carboxylated component. 
     
     
         23 . The method according to  claim 20 , wherein the active agent is a propynylaminoindan. 
     
     
         24 . The method according to  claim 23 , wherein the propynylaminoindan is N-propargyl-1-aminoindan. 
     
     
         25 . A kit comprising:
 two or more transdermal compositions, wherein each transdermal composition comprises:   an active agent layer comprising an active agent in a matrix; and   a conversion layer comprising a weak base in a matrix.   
     
     
         26 . The kit according to  claim 25 , wherein the conversion layer comprises a carboxylated component.