Compositions and methods for enhancing corticosteroid delivery
View Patent ↗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.
1. 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 0.90, and 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, and
wherein said composition does not include a monoglyceride of a C 6 -C 10 medium chain fatty acid.
2. The method of claim 1 wherein the corticosteroid comprises a fluorinated corticosteroid.
3. The method of claim 1 wherein the corticosteroid comprises fluocinonide.
4. The method of claim 1 wherein the corticosteroid comprises fluocinolone acetonide.
5. The method of claim 1 , 2 , 3 or 4 wherein the corticosteroid is present at about 0.10%.
6. The method of claim 1 , 2 , 3 or 4 wherein the corticosteroid is present at least about 0.50%.
7. The method of claim 1 , 2 , 3 or 4 wherein the corticosteroid is present at least about 0.25%.
8. The method 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.
9. The method of claim 1 wherein the composition further comprises one or more non-solvent/emulsifier ingredients.
10. The method of claim 9 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.
11. The method of claim 1 wherein the solvents and emulsifiers are present at about 4-5%.
12. The method of claim 10 wherein the non-solvent/emulsifier ingredients are present at about 11% to about 53%.
13. The method of claim 10 wherein the non-solvent/emulsifier ingredients are present at about 11% to about 27%.
14. 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 0.90, and wherein the first penetration enhancer is propylene glycol and the second penetration enhancer is selected from the group consisting of diisopropyl adipate, dimethyl isosorbide, 1,2,6 hexanetriol, and benzyl alcohol, and wherein the propylene glycol is at least 66.8% of the composition.
15. 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 0.90, and wherein the first penetration enhancer is propylene glycol and the second penetration enhancer is selected from the group consisting of diisopropyl adipate, dimethyl isosorbide, 1,2,6 hexanetriol, and benzyl alcohol, and wherein the propylene glycol is between 66.8% and 74.9% of the composition.
16. 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 0.90, and wherein the first penetration enhancer is dimethyl isosorbide and the second penetration enhancer is selected from the group consisting of propylene glycol, diisopropyl adipate, 1,2,6 hexanetriol, and benzyl alcohol.
17. The method of claim 16 wherein the corticosteroid comprises a fluorinated corticosteroid.
18. The method of claim 16 wherein the corticosteroid comprises fluocinonide.
19. The method of claim 16 wherein the corticosteroid comprises fluocinolone acetonide.
20. The method of claim 16 , 17 , 18 or 19 wherein the corticosteroid is present at about 0.10%.
21. The method of claim 16 , 17 , 18 or 19 wherein the corticosteroid is present at at least about 0.50%.
22. The method of claim 16 , 17 , 18 or 19 wherein the corticosteroid is present at at least about 0.25%.
23. The method of claim 16 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.
24. The method of claim 16 wherein the composition further comprises one or more non-solvent/emulsifier ingredients.
25. The method of claim 24 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.
26. The method of claim 16 wherein the solvents and emulsifiers are present at about 4-5%.
27. The method of claim 24 wherein the non-solvent/emulsifier ingredients are present at about 11% to about 53%.
28. The method of claim 24 wherein the non-solvent/emulsifier ingredients are present at about 11% to about 27%.
29. The method of claim 16 wherein the second penetration enhancer is propylene glycol and wherein the propylene glycol is at least 66.8% of the composition.
30. The method of claim 16 wherein the second penetration enhancer is propylene glycol and wherein the propylene glycol is between 66.8% and 74.9% of the composition.