Compositions and methods for enhancing corticosteroid delivery
DCFirst Claim
Patent Images
1. A composition consisting essentially ofOne or more corticosteroids;
- Two or more penetration enhancers selected from the group consisting of diisopropyl adipate, dimethyl isosorbide, propylene glycol, 1,2,6-hexanetriol, and benzyl alcohol; and
One or more of the group consisting of solvents and emulsifiers, wherein the solvents and emulsifiers are selected from the group consisting of dehydrated alcohol, alcohol (95% v/v) USP, 3-Cyclohexene-1-Methanol, .α
.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%), PEG40 Stearate, PEG-7000, Polysorbate 60, potassium hydroxide (1%), propylene carbonate USP, propylethylene glycol4, oleyl alcohol, sodium lauryl sulfate, sorbitan monostearate, sorbitan stearate, and 1,2,3-Propanetriol Ester, and wherein the penetration enhancers are present in a ratio to a total of the penetration enhancers, and solvents and emulsifiers of at least about 0.9.
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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.
17 Citations
56 Claims
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1. A composition consisting essentially of
One or more corticosteroids; -
Two or more penetration enhancers selected from the group consisting of diisopropyl adipate, dimethyl isosorbide, propylene glycol, 1,2,6-hexanetriol, and benzyl alcohol; and One or more of the group consisting of solvents and emulsifiers, wherein the solvents and emulsifiers are selected from the group consisting of dehydrated alcohol, alcohol (95% v/v) USP, 3-Cyclohexene-1-Methanol, .α
.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%), PEG40 Stearate, PEG-7000, Polysorbate 60, potassium hydroxide (1%), propylene carbonate USP, propylethylene glycol4, oleyl alcohol, sodium lauryl sulfate, sorbitan monostearate, sorbitan stearate, and 1,2,3-Propanetriol Ester, and wherein the penetration enhancers are present in a ratio to a total of the penetration enhancers, and solvents and emulsifiers of at least about 0.9. - View Dependent Claims (2, 3, 4, 5, 6, 7, 8, 9, 10, 11, 12, 13, 14)
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15. A composition consisting essentially of
one or more corticosteroids; -
two or more penetration enhancers selected from the group consisting of diisopropyl adipate, dimethyl isosorbide, propylene glycol, 1,2,6-hexanetriol, and benzyl alcohol; one or more solvents/emulsifiers, wherein the solvents and emulsifiers are selected from the group consisting of dehydrated alcohol, alcohol (95% v/v) USP, 3-Cyclohexene-1-Methanol, .α
.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%), PEG40 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-Propanetriol Ester; andone or more non-solvent/emulsifier ingredients, 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, and wherein the one or more non-solvent/emulsifier ingredients include purified water, and wherein the penetration enhancers are present in a ratio to a total of the penetration enhancers, and solvents/emulsifiers of at least about 0.90. - View Dependent Claims (16, 17, 18, 19, 20, 21, 22, 23, 24, 25, 26)
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27. A composition consisting essentially of
one or more corticosteroids; -
two or more penetration enhancers, 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; one or more solvents/emulsifiers, wherein the solvents and emulsifiers are selected from the group consisting of dehydrated alcohol, alcohol (95% v/v) USP, 3-Cyclohexene-1-Methanol, .α
.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%), PEG40 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-Propanetriol Ester; andone or more non-solvent/emulsifier ingredients, wherein the non-solvent/emulsifier ingredients comprise one or more of the group consisting of Glyceryl Stearate (and) PEG-100Stearate, 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, and wherein the one or more non-solvent/emulsifier ingredients include purified water and wherein the penetration enhancers are present in a ratio to a total of the penetration enhancers, and solvents/emulsifiers of at least about 0.90 wherein the propylene glycol is at least 66.8% of the composition. - View Dependent Claims (28)
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29. A composition comprising
One or more corticosteroids; -
Two or more penetration enhancers wherein the first penetration enhancer is dimethyl isosorbide and the second penetration enhancer is selected from the group consisting of diisopropyl adipate, propylene glycol, 1,2,6-hexanetriol, and benzyl alcohol; and One or more of the group consisting of solvents and emulsifiers , wherein the solvents and emulsifiers are selected from the group consisting of dehydrated alcohol, alcohol (95% v/v) USP, 3-Cyclohexene-1-Methanol, .α
.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%), PEG40 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-Propanetriol Ester, wherein the penetration enhancers are present in a ratio to a total of the penetration enhancers, and solvents and emulsifiers of at least about 0.90. - View Dependent Claims (30, 31, 32, 33, 34, 35, 36, 37, 38, 39, 40, 41, 42)
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43. A composition consisting essentially of
one or more corticosteroids; -
two or more penetration enhancers wherein the first penetration enhancer is dimethyl isosorbide and the second penetration enhancer is selected from the group consisting of diisopropyl adipate, propylene glycol, 1,2,6-hexanetriol, and benzyl alcohol; one or more solvents/emulsifiers, wherein the solvents and emulsifiers are selected from the group consisting of dehydrated alcohol, alcohol (95% v/v) USP, 3-Cyclohexene-1-Methanol, .α
.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%), PEG40 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-Propanetriol Ester; andone or more non-solvent/emulsifier ingredients, 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, and wherein the one or more non-solvent/emulsifier ingredients include purified water, and wherein the penetration enhancers are present in a ratio to a total of the penetration enhancers, and solvents/emulsifiers of at least about 0.90. - View Dependent Claims (44, 45, 46, 47, 48, 49, 50, 51, 52, 53, 54, 55, 56)
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Specification