# US 9,433,630 B1 · Topical formulations comprising a steroid > Agents: this data is available as JSON from the patentgrep API and MCP server — see https://patentgrep.com/llms.txt - Number: US 9,433,630 B1 - Document ID: US9433630B1 - Status: Granted - Kind: B1 - Application number: 15/135,259 - Filed: 2016-04-21 - Published: 2016-08-18 - Granted: 2016-09-06 - Earliest claimed: 2009-08-31 - Assignees: Dr. Reddy's Laboratories, Inc. - Applicants: Dr. Reddy's Laboratories Ltd. - Inventors: Udhumansha Ubaidulla; Sateesh Kandavilli; Ajay Sunil Vairale; Jeffrey A. Wayne; Vijendra Nalamothu; Mistry Meghal; Refika Isil Pakunlu - Web page: https://patentgrep.com/patent/US9433630B1 ## CPC - A61K 31/573: substituted in position 21, e.g. cortisone, dexamethasone, prednisone or aldosterone - A61K 9/0014: {Skin, i.e. galenical aspects of topical compositions (non-active ingredients are additionally classified in A61K47/00; A61K9/0009, A61K9/0021, A61K9/7015, A61K9/7023 take precedence; cosmetic preparations A61K8/00, A61Q; preparations for wound dressings or bandages A61L26/00)} - A61K 9/107: Emulsions {; Emulsion preconcentrates; Micelles (composition of emulsions A61K47/00)} - A61K 9/7015: {Drug-containing film-forming compositions, e.g. spray-on} - A61K 31/56: Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids - A61K 31/575: substituted in position 17 beta by a chain of three or more carbon atoms, e.g. cholane, cholestane, ergosterol, sitosterol - A61K 31/58: containing heterocyclic rings, e.g. danazol, stanozolol, pancuronium or digitogenin (digitoxin {A61K31/7048}) - A61K 47/10: Alcohols; Phenols; Salts thereof, e.g. glycerol; Polyethylene glycols [PEG]; Poloxamers; PEG/POE alkyl ethers - A61K 47/14: Esters of carboxylic acids, e.g. fatty acid monoglycerides, medium-chain triglycerides, parabens or PEG fatty acid esters - A61K 47/22: Heterocyclic compounds, e.g. ascorbic acid, tocopherol or pyrrolidones - A61K 47/26: Carbohydrates, e.g. sugar alcohols, amino sugars, nucleic acids, mono-, di- or oligo-saccharides; Derivatives thereof, e.g. polysorbates, sorbitan fatty acid esters or glycyrrhizin - A61K 47/32: Macromolecular compounds obtained by reactions only involving carbon-to-carbon unsaturated bonds, e.g. carbomers {, poly(meth)acrylates, or polyvinyl pyrrolidone} - A61K 47/36: Polysaccharides; Derivatives thereof, e.g. gums, starch, alginate, dextrin, hyaluronic acid, chitosan, inulin, agar or pectin - A61K 47/38: Cellulose; Derivatives thereof - A61K 47/44: Oils, fats or waxes according to two or more groups of A61K47/02-A61K47/42; Natural or modified natural oils, fats or waxes, e.g. castor oil, polyethoxylated castor oil, montan wax, lignite, shellac, rosin, beeswax or lanolin (synthetic glycerides, e.g. medium-chain triglycerides, A61K47/14) - A61P 17/00: Drugs for dermatological disorders - A61P 17/06: Antipsoriatics - A61P 17/08: Antiseborrheics - A61P 37/08: Antiallergic agents (antiasthmatic agents A61P11/06; ophthalmic antiallergics A61P27/14) - B05B 1/02: designed to produce a jet, spray, or other discharge of particular shape or nature, e.g. in single drops, {or having an outlet of particular shape}(B05B1/26, B05B1/28, B05B1/34 take precedence) - B05B 1/30: designed to control volume of flow, e.g. with adjustable passages {(B05B11/0094 takes precedence)} - B05B 11/1045: {the pump being preassembled as an independent unit before being mounted on the container (B05B11/1047, B05B11/1049 take precedence)} - B05B 15/30: Dip tubes - A61K: PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES (devices or methods specially adapted for bringing pharmaceutical products into particular physical or administering forms A61J3/00; chemical aspects of, or use of materials for deodorisation of air, for disinfection or sterilisation, or for bandages, dressings, absorbent pads or surgical articles A61L; soap compositions C11D) - A61P: SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS - B05B: SPRAYING APPARATUS; ATOMISING APPARATUS; NOZZLES (spray-mixers with nozzles B01F25/72; processes for applying liquids or other fluent materials to surfaces by spraying B05D) ## Abstract 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. ## Claims ### Claim 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. ### Claim 2 (depends on 1) 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. ### Claim 3 (depends on 1) 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. ### Claim 4 (depends on 1) 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. ### Claim 5 (depends on 1) The composition according to claim 1, and further comprising a penetration enhancer. ### Claim 6 (depends on 5) The composition according to claim 5, wherein the penetration enhancer is in amounts of about 0.001 percent to about 15 percent by weight. ### Claim 7 (depends on 6) 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. ### Claim 8 (depends on 1) 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. ### Claim 9 (depends on 1) 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. ### Claim 10 (depends on 1) The composition according to claim 1, wherein the steroid is betamethasone dipropionate. ### Claim 11 (depends on 1) The composition according to claim 1, wherein the viscosity of the composition is in the range of about 10 to about 15,000 centipoise. ### Claim 12 (depends on 1) The composition according to claim 1, wherein the composition is substantially non-foaming. ### Claim 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. ### Claim 14 (depends on 13) 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. ### Claim 15 (depends on 13) The composition according to claim 13, wherein the betamethasone compound is betamethasone benzoate, betamethasone dipropionate, betamethasone sodium phosphate, or betamethasone valerate. ### Claim 16 (depends on 13) 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. ### Claim 17 (depends on 13) 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. ### Claim 18 (depends on 13) The composition according to claim 13, and further comprising a penetration enhancer. ### Claim 19 (depends on 18) The composition of claim 18, wherein the penetration enhancer is in amounts of about 0.001 percent to about 15 percent by weight. ### Claim 20 (depends on 13) 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. ### Claim 21 (depends on 13) 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. ### Claim 22 (depends on 1) The composition according to claim 1, wherein the viscosity of the composition is in the range of about 10 to about 15,000 centipoise. ### Claim 23 (depends on 13) The composition according to claim 13, wherein the composition is substantially non-foaming. ### Claim 24 (depends on 1) 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. ### Claim 25 (depends on 13) 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.