Pharmaceutical composition in the form of a hydrogel for transdermal administration of active ingredients

Abstract

The invention relates to a pharmaceutical composition in the form of a hydrogel that comprises a carboxylic acid diester, a C 2 -C 4 alkyl alcohol, an active ingredient and a polymer matrix. The invention also relates to the use of a carboxylic acid diester as a transdermal permeation enhancer for an active ingredient in a pharmaceutical composition in the form of a hydrogel, whereby the composition comprises a polymer matrix and a C 2 -C 4 alkyl alcohol. The invention also relates to a sweat-resistant composition in the form of a hydrogel, which comprises an acrylic polymer in combination with a cellulose derivative.

1 .- 20 . (canceled) 
     
     
         21 . A pharmaceutical composition in the form of a hydrogel that contains a
 (i) carbonic acid diester of the general formula (II)   
       
         
           
           
               
               
           
         
         in which index m is a number from 1 to 3, and R 3  is hydrogen or C 1 -C 4 -alkyl 
         (ii) a C 2 -C 4  alkyl alcohol, 
         (iii) at least one active ingredient of the general formula (V) 
       
       
         
           
           
               
               
           
         
         in which R 4  is fluorine or hydrogen, and X is a hydroxyl group or its acetate and (iv) a polymer matrix. 
       
     
     
         22 . A composition according to  claim 21 , wherein m is 1 and R 3  is methyl. 
     
     
         23 . A composition according to  claim 21 , wherein the C 2 -C 4  alkyl alcohol is ethanol. 
     
     
         24 . A composition according to  claim 21 , wherein X is a hydroxyl group. 
     
     
         25 . A composition according to  claim 21 , wherein the polymer matrix is an acrylic polymer. 
     
     
         26 . A composition according to  claim 25 , wherein the acrylic polymer comprises an acrylate/C 10-30  alkyl acrylate crosspolymer. 
     
     
         27 . A composition according to  claim 21 , wherein the polymer matrix comprises a cellulose derivative. 
     
     
         28 . A method for treating steroid deficiency symptoms comprising administering a hydrogel according to  claims 21  to a patient in need thereof. 
     
     
         29 . A method for treatment of primary or secondary hypogonadism comprising administering to a patient in need thereof a hydrogel according to  claim 21 . 
     
     
         30 . A composition according to  claim 21 , wherein said compound of formula II wherein R 3  is hydrogen. 
     
     
         31 . A composition according to  claim 21 , wherein said compound of formula II is from 7.5-12.5% by weight of propylene carbonate. 
     
     
         32 . A composition according to  claim 25 , comprising 0.005-10% by weight of at least one acrylic gel former. 
     
     
         33 . A composition according to  claim 21 , wherein said polymer matrix comprises 0.005-10% by weight of at least one acrylic gel former and 0.01-2.5% by weight of a cellulose derivative. 
     
     
         34 . A composition according to  claim 26 , comprising 0.1-1.5% by weight of acrylate/C10-30 alkyl acrylate crosspolymer.