Topical formulations comprising a steroid
View Patent ↗The application provides formulations for the topical administration of an active agent comprising at least one steroid, in the form of topical sprays that are propellant-free, and/or substantially non-foaming, and/or alcohol-free. The present application also provides processes for preparing such compositions and methods of using them in management of skin diseases or disorders such as psoriasis, dermatoses, and other associated skin diseases or disorders.
1. A sprayable topical pharmaceutical composition, comprising:
an active agent consisting of at least one steroid;
a non-polymeric emulsifying agent comprising sorbitan stearate;
a polymer selected from the group consisting of a cellulose, a gum, an alginate, and a phthalate;
water; and
a water-immiscible substance;
wherein said composition is substantially free of a propellant and propylene glycol; and
wherein the topical pharmaceutical composition is substantially non-occlusive to the skin.
2. The composition according to claim 1 , wherein the steroid is selected from the group comprising alclometasone dipropionate, beclomethasone dipropionate, betamethasone dipropionate, betamethasone valerate, fluocinolone acetonide, halobetasol propionate, hydrocortisone aceponate, hydrocortisone acetate, hydrocortisone valerate, hydrocortisone butyrate, mometasone furoate, triamcinolone acetonide, clocortolone pivalate, clobetasol propionate, desoximetasone, and fluticasone propionate.
3. The composition according to claim 1 , wherein the polymer is selected from the group consisting of ethyl cellulose, methyl cellulose, hydroxyethyl cellulose, hydroxypropylcellulose, hydroxypropyl methylcellulose, hydroxybutyl methyl cellulose, xanthan gum, tragacanth, guar gum, locust bean gum, acacia, alginate, cellulose acetate phthalate, cellulose acetate butyrate, hydroxypropyl methylcellulose phthalate, and any combination thereof.
4. The composition according to claim 1 , wherein the water-immiscible substance is selected from the group consisting of vegetable oil, saturated paraffin oil, mineral oil, fatty acid, fatty ester of a natural fatty acid, triglyceride of animal or vegetable origin, medium chain triglyceride, mixture of mono-, di- and/or tri-glycerides, wax, hydrogenated vegetable oil, and any combination thereof.
5. The composition according to claim 1 , and further comprising a penetration enhancer.
6. The composition according to claim 5 , wherein the penetration enhancer is in amounts of about 0.001 percent to about 15 percent by weight.
7. The composition according to claim 6 , wherein the penetration enhancer is selected from the group comprising a polyol and esters, ethers, sulfoxides, fatty acids, fatty acid esters, or any combination thereof.
8. The composition according to claim 1 , wherein
the steroid is selected from the group comprising alclometasone dipropionate, beclomethasone dipropionate, betamethasone dipropionate, betamethasone valerate, fluocinolone acetonide, halobetasol propionate, hydrocortisone aceponate, hydrocortisone acetate, hydrocortisone valerate, hydrocortisone butyrate, mometasone furoate, triamcinolone acetonide, clocortolone pivalate, clobetasol propionate, desoximetasone, or fluticasone propionate;
the polymer is selected from the group consisting of ethyl cellulose, methyl cellulose, hydroxyethyl cellulose, hydroxypropyl cellulose, hydroxypropyl methylcellulose, hydroxybutyl methyl cellulose, xanthan gum, tragacanth, guar gum, locust bean gum, acacia, alginate, cellulose acetate phthalate, cellulose acetate butyrate, hydroxypropyl methylcellulose phthalate, and any combination thereof; and
the water-immiscible substance is selected from the group consisting of vegetable oil, saturated paraffin oil, mineral oil, fatty acid, fatty ester of a natural fatty acid, triglyceride of animal or vegetable origin, medium chain triglyceride, mixture of mono-, di- and/or tri-glycerides, wax, hydrogenated vegetable oil, and any combination thereof.
9. The composition according to claim 1 , wherein
the steroid is selected from the group comprising betamethasone dipropionate and betamethasone valerate; and
the polymer is selected from the group consisting of ethyl cellulose, methyl cellulose, hydroxyethyl cellulose, hydroxypropyl cellulose, hydroxypropyl methylcellulose, hydroxybutyl methyl cellulose, and any combination thereof.
10. The composition according to claim 1 , wherein the steroid is betamethasone dipropionate.
11. The composition according to claim 1 , wherein the viscosity of the composition is in the range of about 10 to about 15,000 centipoise.
12. The composition according to claim 1 , wherein the composition is substantially non-foaming.
13. A sprayable topical pharmaceutical composition, comprising:
a betamethasone compound;
a non-polymeric emulsifying agent comprising sorbitan stearate;
a polymer selected from the group consisting of a cellulose, a gum, an alginate, and a phthalate;
water;
a water-immiscible substance; and
wherein said composition is substantially free of a propellant and propylene glycol; and
wherein the topical pharmaceutical composition is substantially non-occlusive to the skin.
14. The composition according to claim 13 , wherein the betamethasone compound is in amounts equivalent to about 0.025 to about 0.1 percent by weight of betamethasone base.
15. The composition according to claim 13 , wherein the betamethasone compound is betamethasone benzoate, betamethasone dipropionate, betamethasone sodium phosphate, or betamethasone valerate.
16. The composition according to claim 13 , wherein the polymer is selected from the group consisting of ethyl cellulose, methyl cellulose, hydroxyethyl cellulose, hydroxypropylcellulose, hydroxypropyl methylcellulose, hydroxybutyl methyl cellulose, xanthan gum, tragacanth, guar gum, locust bean gum, acacia, alginate, cellulose acetate phthalate, cellulose acetate butyrate, hydroxypropyl methylcellulose phthalate, and any combination thereof.
17. The composition according to claim 13 , wherein the water-immiscible substance is selected from the group consisting of vegetable oil, saturated paraffin oil, mineral oil, fatty acid, fatty ester of a natural fatty acid, triglyceride of animal or vegetable origin, medium chain triglyceride, mixture of mono-, di- and/or tri-glycerides, wax, hydrogenated vegetable oil, and any combination thereof.
18. The composition according to claim 13 , and further comprising a penetration enhancer.
19. The composition of claim 18 , wherein the penetration enhancer is in amounts of about 0.001 percent to about 15 percent by weight.
20. The composition according to claim 13 , wherein
the betamethasone compound is betamethasone benzoate, betamethasone dipropionate, betamethasone sodium phosphate, or betamethasone valerate;
the polymer is selected from the group consisting of ethyl cellulose, methyl cellulose, hydroxyethyl cellulose, hydroxypropyl cellulose, hydroxypropyl methylcellulose, hydroxybutyl methyl cellulose, xanthan gum, tragacanth, guar gum, locust bean gum, acacia, alginate, cellulose acetate phthalate, cellulose acetate butyrate, hydroxypropyl methylcellulose phthalate, and any combination thereof; and
the water-immiscible substance is selected from the group consisting of vegetable oil, saturated paraffin oil, mineral oil, fatty acid, fatty ester of a natural fatty acid, triglyceride of animal or vegetable origin, medium chain triglyceride, mixture of mono-, di- and/or tri-glycerides, wax, hydrogenated vegetable oil, and any combination thereof.
21. The composition according to claim 13 , wherein the betamethasone compound is betamethasone dipropionate; and the polymer is selected from the group consisting of ethyl cellulose, methyl cellulose, hydroxyethyl cellulose, hydroxypropyl cellulose, hydroxypropyl methylcellulose, hydroxybutyl methyl cellulose, and any combination thereof.
22. The composition according to claim 1 , wherein the viscosity of the composition is in the range of about 10 to about 15,000 centipoise.
23. The composition according to claim 13 , wherein the composition is substantially non-foaming.
24. A method of treating a skin condition comprising administering pharmaceutically effective amount of the composition according to claim 1 to a subject in need thereof, wherein the condition is selected from one or more of atopic dermatitis, seborrhoeic dermatitis, eczema, plaque psoriasis, erythroderma psoriasis, and psoriasis of the scalp, steroid responsive dermatoses, erythema, or contact sensitivity reactions, and other associated diseases or disorders.
25. A method of treating a skin condition comprising administering pharmaceutically effective amount of the composition according to claim 13 to a subject in need thereof, wherein the condition is selected from one or more of atopic dermatitis, seborrhoeic dermatitis, eczema, plaque psoriasis, erythroderma psoriasis, and psoriasis of the scalp, steroid responsive dermatoses, erythema, or contact sensitivity reactions, and other associated diseases or disorders.