Topically applicable anti-inflammatory O/W emulsions comprising pro-penetrating glycols

Abstract

Stable, topically applicable, non-greasy and non-tacky oil-in-water (O/W) anti-inflammatory emulsions, useful, e.g., for the treatment of psoriasis, contain: a. a therapeutically effective amount of at least one steroidal anti-inflammatory agent, notably clobetasol propionate; b. a pro-penetrating system which includes at least one pro-penetrating glycol and at least one other pro-penetrating agent; c. at least one gelling agent; and d. at least one non-polymeric emulsifier, formulated into a topically applicable, pharmaceutically acceptable vehicle therefor, such emulsions being characteristically devoid of any polymeric emulsifier.

1 . A stable, topically applicable, non-greasy and non-tacky oil-in-water (O/W) anti-inflammatory emulsion, comprising: 
 a. a therapeutically effective amount of at least one steroidal anti-inflammatory agent;    b. a pro-penetrating system which comprises at least one pro-penetrating glycol and at least one other pro-penetrating agent;    c. at least one gelling agent; and    d. at least one non-polymeric emulsifier, formulated into a topically applicable, pharmaceutically acceptable vehicle therefor, with the proviso that said emulsion is devoid of any polymeric emulsifier.    
   
   
       2 . The topically applicable O/W anti-inflammatory emulsion as defined by  claim 1 , said at least one steroidal anti-inflammatory agent comprising clobetasol propionate.  
   
   
       3 . The topically applicable O/W anti-inflammatory emulsion as defined by  claim 1 , said at least one pro-penetrating glycol being selected from the group consisting of propylene glycol, ethylene glycol, butylene glycol, pentylene glycol, hexylene glycol, diethylene glycol monoethyl ether, dipropylene glycol, propylene glycol dipelargonate, propylene glycol laurate, ethoxydiglycol and propylene glycol dicaprate/dicaprylate.  
   
   
       4 . The topically applicable O/W anti-inflammatory emulsion as defined by  claim 1 , said at least one other pro-penetrating agent being selected from the group consisting of propylene glycol, dipropylene glycol, propylene glycol dipelargonate, propylene glycol laurate, ethoxydiglycol, propylene glycol dicaprate-dicaprylate, ethanol, dimethyl isosorbide, methylpyrrolidone, oleic acid, PEG-8 capric/caprylic glycerides and oleyl alcohol.  
   
   
       5 . The topically applicable O/W anti-inflammatory emulsion as defined by  claim 1 , said at least one gelling agent being selected from the group consisting of xanthan gum, carob gum, guar gum, alginates, hydroxyethylcellulose, methylcellulose, hydroxypropylcellulose, hydroxypropylmethylcellulose, carboxymethylcellulose, carbomers and starch derivatives, and mixtures thereof.  
   
   
       6 . The topically applicable O/W anti-inflammatory emulsion as defined by  claim 1 , said at least one non-polymeric emulsifier being selected from the group consisting of polyglycerol esters of isostearic acid, sorbitan isostearate, sorbitan sesquioleate, sorbitan laurate, glycol esters of isostearic acid, sorbitol esters of oleic acid, glycol esters of oleyl alcohol, oxyethylenated sorbitan monostearate, stearyl alcohol and cetyl alcohol.  
   
   
       7 . The topically applicable O/W anti-inflammatory emulsion as defined by  claim 1 , said pro-penetrating system comprising a combination of pro-penetrating glycols/agents selected from the group consisting of: 
 1. propylene glycol and dimethyl isosorbide,    2. propylene glycol and ethanol,    3. propylene glycol, diethylene glycol monoethyl ether and propylene glycol laurate,    4. propylene glycol and methylpyrrolidone,    5. propylene glycol, dimethyl isosorbide and ethanol,    6. propylene glycol, methylpyrrolidone and oleyl alcohol.    
   
   
       8 . The topically applicable O/W anti-inflammatory emulsion as defined by  claim 1 , comprising: 
 a. 0.0025% to 0.5% of clobetasol propionate,    b. 30% to 50% of a pro-penetrating glycol,    c. 1% to 20% of at least one other pro-penetrating agent,    d. 0.1% to 5% of at least one gelling agent,    e. 0.1% to 5% of non-polymeric emulsifier.    
   
   
       9 . The topically applicable O/W anti-inflammatory emulsion as defined by  claim 8 , comprising: 
 a. 0.0025% to 0.5% of clobetasol propionate,    b. 30% to 50% of a pro-penetrating glycol selected from the group consisting of propylene glycol, dipropylene glycol, propylene glycol dipelargonate, propylene glycol laurate, ethoxydiglycol and propylene glycol dicaprate-dicaprylate,    c. 1% to 20% of at least one other pro-penetrating agent selected from the group consisting of propylene glycol, dipropylene glycol, propylene glycol dipelargonate, propylene glycol laurate, ethoxydiglycol, propylene glycol dicaprate-dicaprylate, ethanol, dimethyl isosorbide, methylpyrrolidone, oleic acid, PEG-8 capric/caprylic glycerides, and oleyl alcohol,    d. 0.1% to 5% of at least one gelling agent selected from the group consisting of xanthan gum, carob gum, guar gum, alginates, hydroxyethylcellulose, methylcellulose, hydroxypropylcellulose, hydroxypropylmethylcellulose, carboxymethylcellulose, carbomers and starch derivatives, and mixtures thereof, and    e. 0.1% to 5% of at least one non-polymeric emulsifier selected from the group consisting of polyglyceryl esters of isostearic acid, sorbitan isostearate, sorbitan sesquioleate, sorbitan laurate, glycol esters of isostearic acid, sorbitol esters of oleic acid, glycol esters of oleyl alcohol, oxyethylenated sorbitan monostearate, stearyl alcohol and cetyl alcohol.    
   
   
       10 . A stable, topically applicable, non-greasy and non-tacky oil-in-water (O/W) anti-inflammatory emulsion, consisting essentially of: 
 a. a therapeutically effective amount of at least one steroidal anti-inflammatory agent;    b. a pro-penetrating system which comprises at least one pro-penetrating glycol and at least one other pro-penetrating agent;    c. at least one gelling agent; and    d. at least one non-polymeric emulsifier, formulated into a topically applicable, pharmaceutically acceptable vehicle therefor.    
   
   
       11 . The topically applicable O/W anti-inflammatory emulsion as defined by  claim 1 , comprising from 35% to 47% by weight of said at least one pro-penetrating glycol.  
   
   
       12 . The topically applicable O/W anti-inflammatory emulsion as defined by  claim 11 , comprising from 1% to 20% by weight of said at least one other pro-penetrating agent.  
   
   
       13 . The topically applicable O/W anti-inflammatory emulsion as defined by  claim 1 , having a pH ranging from 5 to 7.5.  
   
   
       14 . The topically applicable O/W anti-inflammatory emulsion as defined by  claim 13 , having a pH ranging from 5.5 to 6.5.  
   
   
       15 . A regime or regimen for treating psoriasis, which comprises topically applying onto the affected skin area of an individual in need of such treatment, a thus effective amount of a stable, non-greasy and non-tacky oil-in-water (O/W) anti-inflammatory emulsion, comprising: 
 a. a therapeutically effective amount of at least one steroidal anti-inflammatory agent;    b. a pro-penetrating system which comprises at least one pro-penetrating glycol and at least one other pro-penetrating agent;    c. at least one gelling agent; and    d. at least one non-polymeric emulsifier, formulated into a topically applicable, pharmaceutically acceptable vehicle therefor, with the proviso that said emulsion is devoid of any polymeric emulsifier.