Pharmaceutical composition

Abstract

A pharmaceutical composition for topical administration, including, as the pharmaceutically active component, at least 5% by weight, based on the total weight of the composition of a piperidinopyrimidine derivative or a pharmaceutically acceptable salt thereof; an acid in an amount to completely solubilise the piperidinopyrimidine derivative or a pharmaceutically acceptable salt thereof; a solvent composition including at least two of water, a lower alcohol and a co-solvent selected from one or more of the group consisting of aromatic and polyhydric alcohols; wherein when the co-solvent includes propylene glycol, it is present in an amount of less than approximately 10% by weight.

1 . A pharmaceutical composition for topical administration, including, as the pharmaceutically active component, 
 at least 5% by weight, based on the total weight of the composition of a piperidinopyrimidine derivative or a pharmaceutically acceptable salt thereof;    an acid in an amount to substantially completely solubilise the piperidinopyrimidine derivative or a pharmaceutically acceptable salt thereof    a solvent composition including a solvent selected from water and/or a lower alcohol and a co-solvent selected from one or more of the group consisting of aromatic and polyhydric alcohols; wherein when the co-solvent includes propylene glycol, it is present in an amount of less than approximately 10% by weight.    
     
     
         2 . A pharmaceutical composition according to  claim 1 , wherein the acid is added in an amount sufficient to provide an apparent pH to the composition of approximately 7.0 or less.  
     
     
         3 . A pharmaceutical composition according to  claim 1 , wherein the pharmaceutically active component is present in an amount of from approximately 5 to 25% by weight, based on the total weight of the pharmaceutical composition.  
     
     
         4 . A pharmaceutical composition according to  claim 3 , wherein the pharmaceutically active component is present in an amount of approximately 7.5 to 12% by weight, based on the total weight of the pharmaceutical composition.  
     
     
         5 . A pharmaceutical composition according to  claim 1 , wherein the pharmaceutically active component is minoxidil or a salt thereof.  
     
     
         6 . A pharmaceutical composition according to  claim 2 , wherein the acid provides to the composition an apparent pH in the range of approximately 5.0 to 7.0.  
     
     
         7 . A pharmaceutical composition according to  claim 2 , wherein the acid is a mineral or organic acid.  
     
     
         8 . A pharmaceutical composition according to  claim 7 , wherein the acid includes acetic or lactic acid.  
     
     
         9 . A pharmaceutical composition according to  claim 1 , wherein the solvent composition includes water and ethanol in a range of approximately 1:1 to 1:3 by volume.  
     
     
         10 . A pharmaceutical composition according to  claim 1 , wherein the co-solvent includes benzyl alcohol.  
     
     
         11 . A pharmaceutical composition according to  claim 1 , wherein the solvent composition system includes water and benzyl alcohol wherein the benzyl alcohol is in an amount of approximately 40 to 100% by weight based on the total weight of the co-solvent system.  
     
     
         12 . A pharmaceutical composition according to  claim 1 , wherein the water is present in an amount no greater than approximately 60% by weight based on the total weight of the co-solvent system.  
     
     
         13 . A pharmaceutical composition according to  claim 1 , wherein the co-solvent includes an alkylene glycol.  
     
     
         14 . A pharmaceutical composition according to  claim 13 , wherein the alkylene glycol is selected from one or more of the group consisting of glycerol, 1,3-butylene or propylene glycol.  
     
     
         15 . A pharmaceutical composition according to  claim 1 , wherein the acid is present at a level that provides at least 0.01 Normal acid.  
     
     
         16 . A pharmaceutical composition according to  claim 1 , wherein the acid is present in an amount equal to or greater than the amount of the piperidinopyrimidine derivative in Normal amounts.  
     
     
         17 . A pharmaceutical composition according to  claim 1 , wherein the solvent system includes water and ethanol in a range of approximately 9:1 to 1:9 by volume.  
     
     
         18 . A pharmaceutical composition according to  claim 5 , wherein the pharmaceutically active component is a minoxidil salt.  
     
     
         19 . A pharmaceutical composition according to  claim 18 , wherein the minoxidil salt is a minoxidil acetate or lactate salt.  
     
     
         20 . A pharmaceutical composition according to  claim 1 , including 
 approximately 5 to 12% by weight, based on the total weight of the composition, of a minoxidil or a minoxidil acid salt;    approximately 88 to 95% by weight of a solvent composition including 
 approximately 10 to 70% by weight of ethanol,  
 approximately 2.5 to 85% by weight of benzyl alcohol;  
   and less than 10% by weight, propylene glycol.    
     
     
         21 . A method for the treatment of hair loss and related indications in humans, which method includes 
 providing    a pharmaceutical composition for topical administration, including, as the pharmaceutically active component, 
 at least 5% by weight, based on the total weight of the composition of a piperidinopyrimidine derivative or a pharmaceutically acceptable salt thereof;  
   an acid in an amount to substantially completely solubilise the piperidinopyrimidine derivative or a pharmaceutically acceptable salt thereof;    a solvent composition including a solvent selected from water and/or a lower alcohol and a co-solvent selected from one or more of the group consisting of aromatic and polyhydric alcohols; wherein when the co-solvent includes propylene glycol, it is present in an amount of less than approximately 10% by weight; and    applying topically to the human scalp a therapeutically or prophylactically effective amount of the pharmaceutical composition.    
     
     
         22 . A method according to  claim 21 , wherein the pharmaceutically active component includes minoxidil or a minoxidil salt.  
     
     
         23 . A method according to  claim 22 , wherein the minoxidil salt is a minoxidil acetate or lactate salt.  
     
     
         24 . A method according to  claim 21 , wherein the pharmaceutical composition includes 
 approximately 5 to 12% by weight, based on the total weight of the composition, of a minoxidil or a minoxidil salt;    approximately 88 to 95% by weight of a solvent composition including 
 approximately 10 to 70% by weight of ethanol,  
 approximately 2.5 to 85% by weight of benzyl alcohol;  
   and less than 10% by weight, propylene glycol.    
     
     
         25 . A pharmaceutical composition according to  claim 1 , substantially as herein before described with reference to any one of the examples.