Matrix for transdermal drug delivery

Abstract

A transdermal drug delivery device involving a macromonomer-containing acrylate or methacrylate copolymer, a softener, and a drug. Also a pressure sensitive skin adhesive involving a macromonomer containing acrylate or methacrylate copolymer and a softener.

1 . A transdermal drug delivery device, comprising: 
 (1) a backing;    (2) a matrix adhered to one side of the backing and comprising 
 (a) a copolymer comprising 
 (i) an alkyl acrylate containing 4 to 10 carbon atoms in the alkyl group;  
 (ii) hydroxyethyl acrylate; and  
 (iii) a substantially linear macromonomer copolymerizable with the alkyl acrylate and hydroxyethyl acrylate and having a molecular weight in the range 500-500,000;  
 
 (b) a softener dissolved in the copolymer; and,  
 (c) if the softener is not therapeutically effective, a therapeutically effective amount of a drug.  
   
     
     
         2 . A transdermal drug delivery device according to  claim 1 , wherein the alkyl acrylate is present in an amount of about 40 to about 95 percent by weight, based on the total weight of all monomers in the copolymer.  
     
     
         3 . A transdermal drug delivery device according to  claim 2 , wherein the alkyl acrylate is isooctyl acrylate.  
     
     
         4 . A transdermal drug delivery device according to  claim 2 , wherein the alkyl acrylate is 2-ethylhexyl acrylate.  
     
     
         5 . A transdermal drug delivery device according to  claim 3 , wherein the hydroxyethyl acrylate is present in an amount of less than 60 percent by weight based on the total weight of the copolymer.  
     
     
         6 . A transdermal drug delivery device according to  claim 3 , wherein the hydroxyethyl acrylate is present in an amount of greater than 25 percent by weight based on the total weight of the copolymer, to about 50 percent by weight based on the total weight of the copolymer.  
     
     
         7 . A transdermal drug delivery device according to  claim 5 , wherein the macromonomer has a molecular weight in the range 2,000-100,000.  
     
     
         8 . A transdermal drug delivery device according to  claim 5 , wherein the macromonomer has a molecular weight in the range 5,000-30,000.  
     
     
         9 . A transdermal drug delivery device according to  claim 7 , wherein the macromonomer is present in an amount of not more than about 30% by weight based on the total weight of all monomers in the copolymer.  
     
     
         10 . A transdermal drug delivery device according to  claim 7 , wherein the macromonomer is present in an amount of not more than about 20% by weight based on the total weight of all monomers in the copolymer.  
     
     
         11 . A transdermal drug delivery device according to  claim 7 , wherein the macromonomer is present in an amount of not more than about 10% by weight based on the total weight of all monomers in the copolymer.  
     
     
         12 . A transdermal drug delivery device according to  claim 11 , wherein the macromonomer is selected from the group consisting of polymethylmethacrylate macromonomer, styrene/acrylonitrile macromonomer, and polystyrene macromonomer.  
     
     
         13 . A transdermal drug delivery device according to  claim 11 , wherein the macromonomer is a polymethylmethacrylate macromonomer.  
     
     
         14 . A transdermal drug delivery device according to  claim 13 , wherein the softener is present in an amount in excess of 20% based on the total weight of the matrix.  
     
     
         15 . A transdermal drug delivery device according to  claim 13 , wherein the softener is present in an amount not in excess of 60% based on the total weight of the matrix.  
     
     
         16 . A transdermal drug delivery device according to  claim 13 , wherein the softener is present in an amount in excess of 20% and less than about 45% by weight based on the total weight of the matrix.  
     
     
         17 . A transdermal drug delivery device according to  claim 15 , wherein the softener is selected from the group consisting of C 8 -C 22  fatty acids, C 8 -C 22  fatty alcohols, lower alkyl esters of C 8 -C 22  fatty acids, monoglycerides of C 8 -C 22  fatty acids, di(lower)alkyl esters of C 6 -C 8  diacids, tetrahydrofurfuryl alcohol polyethylene glycol ether, polyethylene glycol, propylene glycol, ethoxyethoxy ethanol, diethylene glycol monomethyl ether, N,N-dimethyl dodecylamine-N-oxide, 2-(2-ethoxyethoxy)ethanol, and combinations of the foregoing.  
     
     
         18 . A transdermal drug delivery device according to  claim 15 , wherein the softener is selected from the group consisting of glyceryl monolaurate, diethylene glycol monomethyl ether, tetrahydrofurfuryl alcohol polyethylene glycol ether, propylene glycol, isopropyl myristate, ethyl oleate, diisopropyl adipate, oleyl alcohol, 2-(2-ethoxyethoxy)ethanol, and methyl laurate.  
     
     
         19 . A transdermal drug delivery device according to  claim 15 , wherein the softener is methyl laurate.  
     
     
         20 . A pressure sensitive skin adhesive comprising: 
 (1) a copolymer comprising 
 (i) an alkyl acrylate containing 4 to 10 carbon atoms in the alkyl group;  
 (ii) hydroxyethyl acrylate; and  
 (iii) a substantially linear macromonomer copolymerizable with the alkyl acrylate and hydroxyethyl acrylate and having a molecular weight in the range 500-500,000;  
   (2) a softener dissolved in the copolymer; and    (3) if the softener is not therapeutically effective, a therapeutically effective amount of a drug.