US2004198709A1PendingUtilityA1

Compositions and methods for enhancing corticosteroid delivery

60
Priority: Dec 21, 2001Filed: Apr 16, 2004Published: Oct 7, 2004
Est. expiryDec 21, 2021(expired)· nominal 20-yr term from priority
Inventors:Eugene H. GansMitchell S. Wortzman
A61P 9/00A61P 29/00A61K 31/56A61K 31/58A61K 47/08A61K 47/10A61K 47/32A61K 47/14A61K 9/0014A61K 31/573A61K 47/20A61K 47/26A61P 17/00G11C 2216/10A61P 17/04A61K 47/22G11C 16/0433
60
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Claims

Abstract

The present invention comprises a composition, method of enhancing potency and method of delivering corticosteroids in a vehicle comprising at least two penetration enhancers, and solvents and emulsifiers. The propylene glycol and penetration enhancers are present in ratio to the total of the propylene glycol, penetration enhancers, and solvents and emulsifiers of at least about 0.70.

Claims

exact text as granted — not AI-modified
What is claimed is:  
     
         1 . A composition comprising 
 One or more corticosteroids;    Two or more penetration enhancers; and    One or more of the group consisting of solvents and emulsifiers, wherein the penetration enhancers are present in a ratio to a total of the penetration enhancers, and solvents and emulsifiers of at least about 0.70.    
     
     
         2 . The composition of  claim 1  wherein the corticosteroid comprises a fluorinated corticosteroid.  
     
     
         3 . The composition of  claim 1  wherein the corticosteroid comprises fluocinonide.  
     
     
         4 . The composition of  claim 1  wherein the corticosteroid comprises fluocinolone acetonide.  
     
     
         5 . The composition of  claim 1 ,  2 ,  3  or  4  wherein the corticosteroid is present at about 0.10%.  
     
     
         6 . The composition of  claim 1 ,  2 ,  3  or  4  wherein the corticosteroid is present at at least about 0.50%.  
     
     
         7 . The composition of  claim 1 ,  2 ,  3  or  4  wherein the corticosteroid is present at at least about 0.25%.  
     
     
         8 . The composition of  claim 1 ,  2 ,  3  or  4  wherein the penetration enhancers comprise two or more of the group consisting of propylene glycol, diisopropyl adipate, dimethyl isosorbide, 1,2,6 hexanetriol, and benzyl alcohol.  
     
     
         9 . The composition of  claim 1 ,  2 ,  3  or  4  wherein the penetration enhancers comprise two or more of the group consisting of propylene glycol, diisopropyl adipate and dimethyl isosorbide.  
     
     
         10 . The composition of  claim 1 ,  2 ,  3 , or  4  wherein one penetration enhancer comprises propylene glycol.  
     
     
         11 . The composition of  claim 1  wherein the ratio is at least about 0.80.  
     
     
         12 . The composition of  claim 1  wherein the ratio is at least about 0.90.  
     
     
         13 . The composition of  claim 1  wherein the ratio is at least about 0.95.  
     
     
         14 . The composition of  claim 1  wherein the solvents and emulsifiers comprise one or more of the group consisting of dehydrated alcohol, alcohol (95% v/v)USP, 3-Cyclohexene-1-Methanol, ∝4-Dimethyl-a-(4-Methyl-3-Pentenyl)-, Steareth-2, Steareth-21, citric acid, CPE-215, diisopropanolamine (1:9), DIPA/PG (1:9), ethoxydiglycol, Potassium hydroxide (10%), PEG-40 Stearate, PEG-7000, Polysorbate 60, potassium hydroxide (1%), propylene carbonate USP, propylethylene glycol 4, oleyl alcohol, sodium lauryl sulfate, sorbitan monostearate, sorbitan stearate, and 1,2,3-Propanetriyl Ester.  
     
     
         15 . The composition of  claim 1  further comprising one or more non-solvent/emulsifier ingredients.  
     
     
         16 . The composition of  claim 14  wherein the non-solvent/emulsifier ingredients comprise one or more of the group consisting of Glyceryl Stearate (and) PEG-100 Stearate, carbopol 980, cyclomethicone NF, glyceryl monostearate, hydroxyethyl cellulose, hydroxypropyl cellulose, isopropyl myristate, methyl paraben NF, mineral oil, oleic acid NF, PEG-100 Stearate, petrolatum, propyl paraben NF, purified water, stearyl alcohol, white petrolatum, and white wax.  
     
     
         17 . The composition of  claim 1  wherein the solvents and emulsifiers are present at about 4-5%.  
     
     
         18 . The composition of  claim 15  wherein the non-solvent/emulsifier ingredients are present at about 11% to about 53%.  
     
     
         19 . The composition of  claim 15  wherein the non-solvent/emulsifier ingredients are present at about 11% to about 27%.  
     
     
         20 . A composition comprising about 0.10% fluocinonide, about 74.9% propylene glycol, about 3.0% diisopropyl adipate, about 5.0% isopropyl myristate, about 2.5% 1,2,6 trihydroxyhexane, about 1.0% carbopol 980, about 1.0% diisopropanolamine 85%: propylene glycol (1:9), about 0.01% citric acid, about 2.49% purified water, about 2.5% glyceryl monostearate, and about 7.5% glyceryl monostearate & PEG stearate.  
     
     
         21 . A composition comprising about 0.10% fluocinonide, about 70.0% propylene glycol, about 15.0% dimethyl isosorbide, about 1.2% carbopol 980, about 1.2% diisopropanolamine 85%: propylene glycol (1:9), about 0.01% citric acid, about 2.49% purified water, about 2.5% glyceryl monostearate, and about 7.5% glyceryl monostearate & PEG stearate.  
     
     
         22 . A composition comprising about 0.10% fluocinonide, about 66.8% propylene glycol, about 5.0% dimethyl isosorbide, about 5.0% isopropyl myristate, about 0.5% carbopol 980, about 0.5% diisopropanolamine 85%: propylene glycol (1:9), about 5.0% white petrolatum USP, about 6.0% glyceryl monostearate, about 6.0% PEG 100 stearate, about 5.0% stearyl alcohol, and about 0.10% sodium lauryl sulfate.  
     
     
         23 . A composition comprising about 0.10% fluocinonide, about 69.9% propylene glycol, about 2.0% diisopropyl adipate, about 5.0% isopropyl myristate, about 0.5% carbopol 980, about 0.5% diisopropanolamine 85%: propylene glycol (1:9), about 5.0% white petrolatum USP, about 6.0% glyceryl monostearate, about 6.0% PEG 100 stearate, and about 5.0% stearyl alcohol.  
     
     
         24 . A method for enhancing potency of corticosteroids comprising 
 Combining one or more corticosteroids with two or more penetration enhancers, and one or more of the group consisting of solvents and emulsifiers, wherein the penetration enhancers are present in a ratio to a total of penetration enhancers, and solvents and emulsifiers of at least about 0.70.    
     
     
         25 . The method of  claim 24  wherein the corticosteroid comprises a fluorinated corticosteroid.  
     
     
         26 . The method of  claim 24  wherein the corticosteroid comprises fluocinonide.  
     
     
         27 . The method of  claim 24  wherein the corticosteroid comprises fluocinolone acetonide.  
     
     
         28 . The method of  claim 24 ,  25 ,  26  or  27  wherein the corticosteroid is present at about 0.10%.  
     
     
         29 . The method of  claim 24 ,  25 ,  26  or  27  wherein the corticosteroid is present at at least about 0.50%.  
     
     
         30 . The method of  claim 24 ,  25 ,  26  or  27  wherein the corticosteroid is present at at least about 0.25%.  
     
     
         31 . The method of  claim 24 ,  25 ,  26  or  27  wherein the penetration enhancers comprise two or more of the group consisting of propylene glycol, diisopropyl adipate, dimethyl isosorbide, 1,2,6 hexanetriol, and benzyl alcohol.  
     
     
         32 . The method of  claim 24 ,  25 ,  26  or  27  wherein the penetration enhancers comprise two or more of the group consisting of propylene glycol, diisopropyl adipate and dimethyl isosorbide.  
     
     
         33 . The method of  claim 24 ,  25 ,  26  or  27  wherein one penetration enhancer comprises propylene glycol.  
     
     
         34 . The method of  claim 24  wherein the ratio is at least about 0.80.  
     
     
         35 . The method of  claim 24  wherein the ratio is at least about 0.90.  
     
     
         36 . The method of  claim 24  wherein the ratio is at least about 0.95.  
     
     
         37 . The method of  claim 24  wherein the solvents and emulsifiers comprise one or more of the group consisting of dehydrated alcohol, alcohol (95% v/v) USP, 3-Cyclohexene-1-Methanol, ∝4-Dimethyl-a-(4-Methyl-3-Pentenyl)-, Steareth-2, Steareth-21, citric acid, CPE-215, diisopropanolamine (1:9), DIPA/PG (1:9), ethoxydiglycol, Potassium hydroxide (10%), PEG-40 Stearate, PEG-7000, Polysorbate 60, potassium hydroxide (1%), propylene carbonate USP, propylethylene glycol 4, oleyl alcohol, sodium lauryl sulfate, sorbitan monostearate, sorbitan stearate, and 1,2,3-Propanetriyl Ester.  
     
     
         38 . The method of  claim 24  wherein the composition further comprises one or more non-solvent/emulsifier ingredients.  
     
     
         39 . The method of  claim 38  wherein the non-solvent/emulsifier ingredients comprise one or more of the group consisting of Glyceryl Stearate (and) PEG-100 Stearate, carbopol 980, cyclomethicone NF, glyceryl monostearate, hydroxyethyl cellulose, hydroxypropyl cellulose, isopropyl myristate, methyl paraben NF, mineral oil, oleic acid NF, PEG-100 Stearate, petrolatum, propyl paraben NF, purified water, stearyl alcohol, white petrolatum, and white wax.  
     
     
         40 . The method of  claim 24  wherein the solvents and emulsifiers are present at about 4-5%.  
     
     
         41 . The method of  claim 39  wherein the non-solvent/emulsifier ingredients are present at about 11% to about 53%.  
     
     
         42 . The method of  claim 39  wherein the non-solvent/emulsifier ingredients are present at about 11% to about 27%.  
     
     
         43 . A method of delivering corticosteroids to skin comprising 
 Topically applying a composition comprising one or more corticosteroids with two or more penetration enhancers, and one or more of the group consisting of solvents and emulsifiers, wherein the penetration enhancers are present in ratio to a total of the penetration enhancers, and solvents and emulsifiers of at least about 0.70.    
     
     
         44 . The method of  claim 43  wherein the corticosteroid comprises a fluorinated corticosteroid.  
     
     
         45 . The method of  claim 43  wherein the corticosteroid comprises fluocinonide.  
     
     
         46 . The method of  claim 43  wherein the corticosteroid comprises fluocinolone acetonide.  
     
     
         47 . The method of  claim 43 ,  44 ,  45  or  46  wherein the corticosteroid is present at about 0.10%.  
     
     
         48 . The method of  claim 43 ,  44 ,  45  or  46  wherein the corticosteroid is present at at least about 0.50%.  
     
     
         49 . The method of  claim 43 ,  44 ,  45  or  46  wherein the corticosteroid is present at at least about 0.25%.  
     
     
         50 . The method of  claim 43 ,  44 ,  45  or  46  wherein the penetration enhancers comprise two or more of the group consisting of propylene glycol, diisopropyl adipate dimethyl isosorbide, 1,2,6 hexanetriol, and benzyl alcohol.  
     
     
         51 . The method of  claim 43 ,  44 ,  45  or  46  wherein the penetration enhancers comprise two or more of the group consisting of propylene glycol, diisopropyl adipate and dimethyl isosorbide.  
     
     
         52 . The method of  claim 43 ,  44 ,  45  or  46  wherein one penetration enhancer comprises propylene glycol.  
     
     
         53 . The method of  claim 43  wherein the ratio is at least about 0.85.  
     
     
         54 . The method of  claim 43  wherein the ratio is at least about 0.90.  
     
     
         55 . The method of  claim 43  wherein the solvents and emulsifiers comprise one or more of the group consisting of dehydrated alcohol, alcohol (95% v/v)USP, 3-Cyclohexene-1-Methanol, ∝4-Dimethyl-a-(4-Methyl-3-Pentenyl)-, Steareth-2, Steareth-21, citric acid, CPE-215, diisopropanolamine (1:9), DIPA/PG (1:9), ethoxydiglycol, Potassium hydroxide (10%), PEG-40 Stearate, PEG-7000, Polysorbate 60, potassium hydroxide (1%), propylene carbonate USP, propylethylene glycol 4, oleyl alcohol, sodium lauryl sulfate, sorbitan monostearate, sorbitan stearate, and 1,2,3-Propanetriyl Ester.  
     
     
         56 . The method of  claim 43  wherein the composition further comprises one or more non-solvent/emulsifier ingredients.  
     
     
         57 . The method of  claim 56  wherein the non-solvent/emulsifier ingredients comprise one or more of the group consisting of Glyceryl Stearate (and) PEG-100 Stearate, carbopol 980, cyclomethicone NF, glyceryl monostearate, hydroxyethyl cellulose, hydroxypropyl cellulose, isopropyl myristate, methyl paraben NF, mineral oil, oleic acid NF, PEG-100 Stearate, petrolatum, propyl paraben NF, purified water, stearyl alcohol, white petrolatum, and white wax.  
     
     
         58 . The method of  claim 43  wherein the solvents and emulsifiers are present at about 4-5%.  
     
     
         59 . The method of  claim 57  wherein the non-solvent/emulsifier ingredients are present at about 11% to about 53%.  
     
     
         60 . The method of  claim 57  wherein the non-solvent/emulsifier ingredients are present at about 11% to about 27%.

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