US2016175447A1PendingUtilityA1

Transdermal therapeutic system for administering the active substance buprenorphine

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Assignee: PURDUE PHARMA LPPriority: Nov 21, 2006Filed: Feb 25, 2016Published: Jun 23, 2016
Est. expiryNov 21, 2026(~0.3 yrs left)· nominal 20-yr term from priority
Inventors:Thomas HilleMichael HorstmannWalter Mueller
A61P 29/00A61P 25/36A61P 25/04A61P 25/00A61P 25/32A61K 31/485A61K 47/12A61K 9/7069A61K 9/7084A61M 37/00A61K 9/7053A61K 9/7092A61K 9/70
57
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Claims

Abstract

The invention relates to a transdermal therapeutic system for administering the active substance buprenorphine. Said system comprises at least one carboxylic acid that determines the solubility of buprenorphine in the matrix layer and that can likewise be absorbed. The transdermal therapeutic system according to the invention is used in the treatment of pain and characterized by a considerably increased utilization of the active substance.

Claims

exact text as granted — not AI-modified
What is claimed is: 
     
         1 . A transdermal therapeutic system for administering buprenorphine to the skin, comprising:
 an active-ingredient-impermeable backing layer;   at least one pressure-sensitive adhesive matrix layer comprising the active ingredient buprenorphine and at least one carboxylic acid;   wherein the matrix layer comprises a polymer selected from polysiloxanes or polyisobutylene;   wherein the buprenorphine is dissolved in the at least one carboxylic acid to form a solution and   wherein the solution is dispersed, in the form of droplets, in the matrix layer.   
     
     
         2 . The transdermal therapeutic system according to  claim 1 , wherein the matrix layer comprises polysiloxane. 
     
     
         3 . The transdermal therapeutic system according to  claim 1 , wherein the polysiloxane is an amine-resistant dimethylpolysiloxane. 
     
     
         4 . The transdermal therapeutic system according to  claim 1 , wherein the polysiloxane is a mixture of an amine-resistant and a non-amine-resistant dimethylpolysiloxane, in which the non-amine-resistant dimethylpolysiloxane is present at up to 40% by weight. 
     
     
         5 . The transdermal therapeutic system according to  claim 1 , wherein the matrix layer comprises polyisobutylene. 
     
     
         6 . The transdermal therapeutic system according to  claim 1 , wherein the at least one carboxylic acid diffuses into the skin more quickly than does the active ingredient buprenorphine. 
     
     
         7 . The transdermal therapeutic system according to  claim 1 , wherein the amount of the dispersed solution is up to 40% by weight. 
     
     
         8 . The transdermal therapeutic system according to  claim 1 , wherein the at least one carboxylic acid is liquid at skin temperature. 
     
     
         9 . The transdermal therapeutic system according to  claim 1 , wherein the at least one carboxylic acid is selected from the group consisting of oleic acid, linoleic acid, linolenic acid or mixtures thereof. 
     
     
         10 . The transdermal therapeutic system according to  claim 1 , wherein the buprenorphine and the at least one carboxylic acid are present in the same weight ratio. 
     
     
         11 . The transdermal therapeutic system according to  claim 2 ,
 wherein the polysiloxane is a mixture of an amine-resistant and a non-amine-resistant dimethylpolysiloxane, where the non-amine-resistant dimethylpolysiloxane is present in the mixture at up to 40% by weight;   wherein the at least one carboxylic acid diffuses into the skin more quickly than does the active ingredient buprenorphine and where the at least one carboxylic acid is liquid at skin temperature; and   wherein the amount of the dispersed solution in the matrix layer is up to 40% by weight.   
     
     
         12 . The transdermal therapeutic system according to  claim 1 , wherein the matrix layer is in diffusible contact with a layer based on polyacrylates. 
     
     
         13 . The transdermal therapeutic system according to  claim 12 , wherein the polyacrylate layer is embodied as a self-adhesive skin contact layer. 
     
     
         14 . The transdermal therapeutic system according to  claim 13 , wherein the polyacrylate adhesive possesses no free carboxyl groups. 
     
     
         15 . The transdermal therapeutic system according to  claim 1 , wherein active substance utilization under in vivo conditions of at least 30% is achieved. 
     
     
         16 . The transdermal therapeutic system according to  claim 1 , wherein active substance utilization under in vivo conditions of at least 40% is achieved. 
     
     
         17 . The transdermal therapeutic system according to  claim 1 , wherein active substance utilization under in vivo conditions of at least 50% is achieved. 
     
     
         18 . The transdermal therapeutic system according to  claim 1 , wherein the droplets in the matrix layer consist essentially of the buprenorphine and the at least one carboxylic acid. 
     
     
         19 . The transdermal therapeutic system according to  claim 1  further comprising a protective layer to be detached before use. 
     
     
         20 . The transdermal therapeutic system according to  claim 1 , wherein the buprenorphine and the at least one carboxylic acid are present in the different weight ratios. 
     
     
         21 . The transdermal therapeutic system according to  claim 1 , wherein the amount of the at least one carboxylic acid is from 7% to 9% by weight. 
     
     
         22 . A method of treating pain which comprises:
 administering to a patient, in need thereof, a transdermal therapeutic system for administering buprenorphine to the skin, wherein the transdermal therapeutic system comprises:   an active-ingredient-impermeable backing layer;   at least one pressure-sensitive adhesive matrix layer comprising a therapeutically effective amount of the active ingredient buprenorphine and at least one carboxylic acid;   wherein the matrix layer comprises a polymer selected from polysiloxanes or polyisobutylene;   wherein the buprenorphine is dissolved in the at least one carboxylic acid to form a solution; and   wherein the solution is dispersed, in the form of droplets, in the matrix layer.   
     
     
         23 . The method according to  claim 22 , wherein the matrix layer comprises polysiloxane. 
     
     
         24 . The method according to  claim 22 , wherein the buprenorphine and the at least one carboxylic acid are present in the different weight ratios. 
     
     
         25 . The method according to  claim 22 , wherein the amount of the at least one carboxylic acid is from 7% to 9% by weight. 
     
     
         26 . The method according to  claim 22 , wherein the matrix layer comprises polyisobutylene. 
     
     
         27 . The method according to  claim 22 , wherein the amount of the dispersed solution is up to 40% by weight. 
     
     
         28 . The method according to  claim 22 , wherein the at least one carboxylic acid is selected from the group consisting of oleic acid, linoleic acid, linolenic acid or mixtures thereof. 
     
     
         29 . The method according to  claim 22 , wherein active substance utilization under in vivo conditions of at least 30% is achieved. 
     
     
         30 . The method according to  claim 22 , wherein active substance utilization under in vivo conditions of at least 40% is achieved.

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