Corticosteroid-containing pharmaceutical composition

Abstract

The present invention provides a foamable pharmaceutical composition comprising a corticosteroid active substance, a quick-break foaming agent, a propellant and a buffering agent. The quick-break foaming agent typically comprises an aliphatic alcohol, water, a fatty alcohol and surface active agent. The compositions of the invention can be used to treat various skin disease, and in particular scalp psoriasis.

1 . A foamable pharmaceutical composition adapted for topical administration, the composition comprising a corticosteroid, a quick-break foaming agent, a propellant and an amount of a buffering agent, wherein the composition has a pH within the range of 3.0 to 6.0.  
   
   
       2 . The foamable pharmaceutical composition according to  claim 1  having a pH within the range of 4.0 to 5.0.  
   
   
       3 . The foamable pharmaceutical composition according to  claim 1 , wherein the buffering agent is present in an amount from 0.01 to 1.0% w/w.  
   
   
       4 . The foamable pharmaceutical composition according to  claim 3 , wherein the buffering agent is present in an amount in the range of 0.05 to 0.2% w/w.  
   
   
       5 . A foamable pharmaceutical composition adapted for topical administration, the composition comprising a corticosteroid, a quick-break foaming agent, a propellant and an amount of a buffering agent, selected from the group consisting of a citrate buffer, an acetic acid/sodium acetate buffer and a phosphoric acid/sodium phosphate buffer, wherein the composition has a pH within the range of 3.0 to 6.0.  
   
   
       6 . The foamable pharmaceutical composition according to  claim 5 , wherein said citrate buffering agent is a citric acid/sodium citrate buffer.  
   
   
       7 . The foamable pharmaceutical composition according to  claim 5 , wherein said citrate buffering agent is an anhydrous citric acid/potassium citrate buffer.  
   
   
       8 . The foamable pharmaceutical composition according to  claim 1 , wherein the corticosteroid is a topically effective corticosteroid selected from the group consisting of alclometasone dipropionate, amcinonide, beclomethasone dipropionate, betamethasone benzoate, betamethasone dipropionate, betamethasone valerate, budesonide, clobetasol propionate, clobetasone butyrate, desonide, desoxymethasone, diflorasone diacetate, diflucortolone valerate, flumethasone pivalate, fluclorolone acetonide, fluocinolone acetonide, fluocinonide, fluocortin butyl, fluocortolone, fluprednidene acetate, flurandrenolone, halcinonide, hydrocortisone, hydrocortisone acetate, hydrocortisone butyrate, methylprednisolone acetate, mometasone furoate, triamcinolone acetonide, and pharmacologically effective mixtures thereof.  
   
   
       9 . The foamable pharmaceutical composition according to  claim 1 , wherein the corticosteroid is betamethasone or a pharmacologically effective ester or salt thereof.  
   
   
       10 . The foamable pharmaceutical composition according to  claim 7 , wherein the corticosteroid is selected from betamethasone benzoate, betamethasone dipropionate and betamethasone valerate.  
   
   
       11 . The foamable pharmaceutical composition according to  claim 8 , wherein the corticosteroid is betamethasone valerate.  
   
   
       12 . The foamable pharmaceutical composition according to  claim 1 , wherein the corticosteroid is present in an amount from 0.01 to 1.0% w/w.  
   
   
       13 . The foamable pharmaceutical composition according to  claim 12 , wherein the corticosteroid is present in an amount from 0.05 to 0.2% w/w.  
   
   
       14 . The foamable pharmaceutical composition according to  claim 1 , wherein the quick-break foaming agent comprises an aliphatic alcohol, water, a fatty alcohol and a surface active agent.  
   
   
       15 . The foamable pharmaceutical composition according to  claim 14 , wherein the aliphatic alcohol is present in an amount corresponding to 7 to 90% by weight of the total weight of the composition.  
   
   
       16 . The foamable pharmaceutical composition according to  claim 15 , wherein the aliphatic alcohol is present in an amount corresponding to 55 to 70% by weight of the composition.  
   
   
       17 . The foamable pharmaceutical composition according to  claim 19 , wherein the aliphatic alcohol is present in an amount corresponding to 57 to 59% by weight of the composition.  
   
   
       18 . The foamable pharmaceutical composition according to  claim 14 , wherein the aliphatic alcohol is selected from the group consisting of methanol, ethanol, isopropyl alcohol, butyl alcohol, and mixtures thereof.  
   
   
       19 . The foamable pharmaceutical composition according to  claim 18 , wherein the aliphatic alcohol is ethanol.  
   
   
       20 . The foamable pharmaceutical composition according to  claim 14 , wherein the water is present in an amount in the range of 10 to 40% by weight of the composition.  
   
   
       21 . The foamable pharmaceutical composition according to  claim 14 , wherein the fatty alcohol is present in an amount corresponding to 0.5 to 10% by weight of the composition.  
   
   
       22 . The foamable pharmaceutical composition according to  claim 14 , wherein the fatty alcohol is selected from the group consisting of cetyl, stearyl, lauryl, myristyl, and palmityl alcohols, and mixtures thereof.  
   
   
       23 . The foamable pharmaceutical composition according to  claim 22 , wherein the fatty alcohol component is a mixture of cetyl alcohol and a stearyl alcohol.  
   
   
       24 . The foamable pharmaceutical composition according to  claim 14 , wherein the surface active agent is present in an amount from 0.1 to 15% w/w of the composition.  
   
   
       25 . The foamable pharmaceutical composition according to  claim 14 , wherein the surface active agent is selected from the group consisting of ethoxylated sorbitan stearate, ethoxylated sorbitan palmitate, ethoxylated sorbitan oleate, nonyl phenol ethoxylates, fatty alcohol ethoxylates, and mixtures thereof.  
   
   
       26 . The foamable pharmaceutical composition according to  claim 25 , wherein the surface active agent is a mixture of partial stearic esters of sorbitol and its anhydrides, copolymerized with approximately 20 moles of ethylene oxide for each mole of sorbitol and its anhydrides.  
   
   
       27 . A pharmaceutical product comprising the foamable pharmaceutical composition of  claim 1  contained within a container capable of withstanding the pressure of the propellant and having a valve or nozzle for dispensing the foamable composition as a foam under pressure.  
   
   
       28 . A foamable pharmaceutical composition adapted for topical administration having the following composition:  
     
       
         
               
               
               
             
                   
                   
               
                   
                   
               
                   
                   
                 % w/w 
               
                   
                   
               
                   
               
               
               
               
             
                   
                 Betamethasone Valerate 
                 0.120 
               
                   
                 Cetyl Alcohol BP 
                 1.100 
               
                   
                 Octadecan-1-ol BP 
                 0.500 
               
                   
                 Polysorbate 60 BP 
                 0.400 
               
                   
                 Ethanol 
                 57.790 
               
                   
                 Purified Water 
                 33.690 
               
                   
                 Propylene Glycol BP 
                 2.000 
               
                   
                 Citric Acid Anhydrous BP 
                 0.073 
               
                   
                 Potassium Citrate 
                 0.027 
               
                   
                 Butane/Propane 
                 4.300 
               
                   
                   
                 100.000.