Pharmaceutical composition in the form of a gel or a solution based on dihydrotestosterone, process for preparing it and uses thereof

Abstract

The present invention relates to a pharmaceutical composition in the form of a hydro-alcoholic gel or a solution for transdermal application, comprising: from about 0.2% to about 1.5% of dihydrotestosterone; and from about 0.2 to about 3% of isopropyl myristate.

What we claim is:  
     
         1 . Pharmaceutical composition in the form of a hydro-alcoholic gel or a solution for transdermal application, comprising: 
 from about 0.2% to about 1.5% of dihydrotestosterone;    and from about 0.2% to about 3% of isopropyl myristate;    these percentages being expressed by weight relative to 100 g of the pharmaceutical composition.    
     
     
         2 . Pharmaceutical composition according to  claim 1 , having a dihydrotestosterone content of about 0.7%, these percentages being expressed by weight relative to 100 g of the pharmaceutical composition.  
     
     
         3 . Pharmaceutical composition of  claim 1 , having a content of isopropyl myristate from about 0.45 to about 2%, these percentages being expressed by weight relative to 100 g of the pharmaceutical composition.  
     
     
         4 . Pharmaceutical composition of  claim 2 , having a content of isopropyl myristate of about 0.7%, these percentages being expressed by weight relative to 100 g of the pharmaceutical composition.  
     
     
         5 . Pharmaceutical composition according to  claim 1 , wherein the alcoholic solvent is selected from the group consisting of ethanol, isopropanol and mixtures thereof.  
     
     
         6 . Pharmaceutical composition according to  claim 1 , having a content of from about 50 to about 75% of absolute ethanol, these percentages being expressed by weight relative to 100 g of formulation.  
     
     
         7 . Pharmaceutical composition according to  claim 6 , having a content of about 66% of absolute ethanol, these percentages being expressed by weight relative to 100 g of formulation.  
     
     
         8 . Pharmaceutical composition according to  claim 1 , having a content of from about 0.2 and about 2% of a gelling agent, these percentages being expressed by weight relative to 100 g of formulation.  
     
     
         9 . Pharmaceutical composition according to  claim 1 , having a content of about 0.5% of a gelling agent, these percentages being expressed by weight relative to 100 g of formulation.  
     
     
         10 . Pharmaceutical composition according to  claim 8 , wherein the gelling agent is selected from the group consisting of carbomers, cellulose derivatives and mixtures thereof.  
     
     
         11 . Pharmaceutical composition according to  claim 8 , wherein the gelling agent is a carbomer.  
     
     
         12 . Pharmaceutical composition according to  claim 8 , wherein the gelling agent is Carbopol® 980 (carboxyvinyl polymer grade 980, polymerized in an ethyl acetate/cyclohexane system).  
     
     
         13 . Pharmaceutical composition according to  claim 8 , further comprising a neutralizing agent.  
     
     
         14 . Pharmaceutical composition according to  claim 13 , wherein the neutralizing agent is selected from the group consisting of triethanolamine, sodium hydroxide, ammonium hydroxide, potassium hydroxide, arginine, aminomethylpropanol and tromethamine, and mixtures thereof.  
     
     
         15 . Pharmaceutical composition according to  claim 13 , wherein the neutralizing agent/gelling agent ratio is from about 3/1 to about 0.5/1.  
     
     
         16 . Pharmaceutical composition according to  claim 14 , wherein the neutralizing agent is triethanolamine.  
     
     
         17 . Pharmaceutical composition according to  claim 15 , wherein the neutralizing agent/gelling agent ratio is about 1/1.  
     
     
         18 . Process for preparing a pharmaceutical composition according to  claim 1 , comprising the following steps: 
 a mixture comprising DHT, isopropyl myristate and an alcoholic solvent is prepared;    a gelling agent is optionally added to this mixture, and mixing is again carried out;    a neutralizer is optionally added, and mixing is then again carried out;    the pharmaceutical composition containing DHT is recovered.    
     
     
         19 . Process according to  claim 18 , wherein the alcoholic solvent is selected from the group consisting of ethanol, isopropanol or mixtures thereof.  
     
     
         20 . Method for the treatment of physiological conditions associated with insufficiency of dihydrotestosterone, comprising the step of administering a pharmaceutical composition according to  claim 1  to a subject.  
     
     
         21 . Method according to  claim 21 , wherein the physiological conditions are selected from the group consisting of permanent hypogonadism, functional hypogonadism, hyperplasia of the prostate, gynaecomasty, balano-preputial sclero-atrophic lichen in men and vulval sclero-atrophic lichen in women, or micropenis in children.