Patent application EP17173510A (EP), filed 2017-05-30
Publication number: EP3251657A1
Title: TOPICAL AQUEOUS SPRAY COMPOSITIONS OF HALOBETASOL
Abstract: The present invention relates to topical aqueous spray compositions of halobetasol. The topical aqueous spray compositions may be in the form of solutions or emulsions. It also relates to processes for the preparation of the topical aqueous spray compositions. It further relates to a method of treating topical skin conditions by administering said topical aqueous spray compositions.
IPC codes: A61K  31/   573            A I
A61K  47/    10            A I
A61K   9/    00            A I
A61K   9/    12            A I
Claims: number: 1
text: A topical aqueous spray composition comprising:
number: 2
text: The topical aqueous spray composition of claim 1, wherein the composition comprises about 0.05% w/w of halobetasol based on the total weight of the composition.
number: 3
text: The topical aqueous spray composition of claim 2, wherein the halobetasol is halobetasol propionate.
number: 4
text: The topical aqueous spray composition of claim 1, wherein the water-miscible co-solvent is selected from group consisting of alcohols and glycols including ethyl alcohol, isopropyl alcohol, propylene glycol, butanediol, pentanediol, hexanediol, triethylene glycol, tetraethylene glycol, dipropylene glycol, and dibutylene glycol; glycerin; dimethyl isosorbide; tetrahydrofurfuryl alcohol polyethylene glycol ether; N-methyl-2-pyrrolidone; 1-methyl-2-pyrrolidinone; dimethylsulfoxide; dimethylacetamide; lactic acid; glycolic acid; methylene chloride; methyl-ethyl-ketone; ethyl acetate; methylene dimethyl ether; polyethylene glycols such as polyethylene glycol 400; and mixtures thereof.
number: 5
text: The topical aqueous spray composition of claim 4, wherein the water-miscible co-solvent is ethyl alcohol.
number: 6
text: The topical aqueous spray compositions of claim 1, wherein the composition is an emulsion.
number: 7
text: The topical aqueous spray composition of claim 1, wherein the composition further comprises an emulsifier.
number: 8
text: The topical aqueous spray composition of claim 7, wherein the water-immiscible co-solvent is selected from group consisting of fatty acid esters including isopropyl myristate and isopropyl palmitate; light and heavy liquid paraffins; fatty acid triglycerides including mixtures of caprylic and capric triglycerides (Crodamol™ GTCC, Miglyol<®> , Captex<®> , Labrafac<®> Lipophile WL); mixtures of mono-, di-, and/or triglycerides; waxes; hydrogenated vegetable oils; and mixtures thereof.
number: 9
text: The topical composition of claim 8, wherein the emulsifier is selected from the group consisting of sucrose esters; polymers, including poloxamers; polyysorbates, including Tween<®> 20, Tween<®> 40, Tween<®> 60, and Tween<®> 80; polyoxyethylene fatty acid esters, including Myrj<®> 45, Myrj<®> 49, and Myrj<®> 59; poly(oxyethylene)alkylyl ethers including poly(oxyethylene)cetyl ether, poly(oxyethylene)palmityl ether, polyethylene oxide hexadecyl ethers such as Brij<®> 58, and polyethylene glycol cetyl ethers such as Brij<®> 38, Brij<®> 52, Brij<®> 56, and Brij<®> W1; partial esters of sorbitol and sorbitol anhydrides including sorbitan monolaurate and sorbitan monolaurate-mono or diglycerides; alkyl isethionates; alkyl and alkyl ether sulfates and salts thereof; alkyl and alkyl ether phosphates and salts thereof; alkyl methyl taurates; soaps (e.g., alkali metal salts, sodium salts, and potassium salts of fatty acids); alkylimino acetates; imino-dialkanoates and aminoalkanoates; imidazolinium and ammonium derivatives; betaines; sultaines; hydroxysultaines; alkyl sarcosinates; alkanoyl sarcosinates, sorbitan esters, including Arlacel<®> 20 and Arlacel<®> 40; polyethylene glycol ethers of stearic acid including steareth-2, steareth-4, and steareth-6; polyethylene glycol ethers of stearyl alcohol (steareth-21); silicone emulsifying agents such as dimethicone copolyols; polyoxyethylene sorbitan fatty acid esters; non-solid fatty substances at room temperature, including sesame oil, sweet almond oil, apricot stone oil, sunflower oil, octoxyglyceryl palmitate (or 2-ethylhexyl glyceryl ether palmitate), octoxyglyceryl behenate (or 2-ethylhexyl glyceryl ether behenate), and dioctyl adipate; PEG-20 hexadecenyl succinate; PEG-15 stearyl ether; disodium cocoamphodiacetate; oxyethylenated glyceryl cocoate (7 EO); ricinoleic monoethanolamide monosulfosuccinate salts; oxyethylenated hydrogenated ricinoleic triglyceridesincluding Cremophor<®> RH 60 (polyoxyl 60 hydrogenated castor oil) and Cremophor<®> RH 40 (polyoxyl 40 hydrogenated castor oil); and mixtures thereof.
number: 10
text: The topical aqueous spray composition of claim 1, wherein the composition further comprises an emollient.
number: 11
text: The topical aqueous spray composition of claim 10, wherein the emollient is selected from the group consisting of fatty acid triglycerides including mixtures of caprylic and capric triglycerides (e.g., Crodamol™ GTCC, Miglyol<®> , Captex<®> , Labrafac<®> Lipophile WL), palmitic triglyceride, oleic triglyceride, caprylic triglyceride, capric triglyceride, and linoleic triglyceride; fatty acid esters including isopropyl myristate, isopropyl palmitate, dibutyl adipate, and dibutyl phthalate; polyhydric alcohols including propylene glycol, butylene glycol, polyethylene glycol, glycerol, and sorbitol; fatty acids including oleic acid and stearic acid; oils such as mineral oil, lanolin oil, coconut oil, cocoa butter, olive oil, jojoba oil, and castor oil; cyclomethicone; hydrogenated lanolin; waxes; lecithin; and mixtures thereof.
number: 12
text: The topical aqueous spray composition of claim 11, wherein the composition further comprises a propellant.
number: 13
text: The topical aqueous spray composition of claim 12, wherein the propellant is selected from the group consisting of propane, butane, isobutane, pentane, isopentane, cyclopropane, 1,1,1,2-tetrafluoroethane, 1,1,1,2,3,3,3-heptafluoropropane, 1,1-difluoroethane, 1,1,1,3,3,3-hexafluoropropane, dimethyl ether, fluorocarbon gas, liquefied petroleum gas, nitrogen, carbon dioxide, nitrous oxide, and mixtures thereof.
number: 14
text: A process for the preparation of a topical aqueous spray composition of halobetasol of claim 1, wherein the process comprises the steps of:
number: 15
text: A process for the preparation of a topical aqueous spray composition of halobetasol of claim 7, wherein the process comprises the steps of:
number: 16
text: A topical aqueous spray composition of halobetasol of claim1 for use in treating a topical skin condition.
number: 17
text: The topical aqueous spray composition of claim 16, wherein the condition is one or more conditions selected from the group consisting of corticosteroid-responsive dermatoses, including psoriasis, atopic dermatitis, eczema, rosacea, acne vulgaris, pruritis, seborrhea, skin cancers, and inflammation.
number: 18
text: The topical aqueous spray composition of claim 17, wherein the condition is a corticosteroid-responsive dermatosis.
number: 19
text: The topical aqueous spray composition of claim 18, which comprises co-administrable additional drug(s) used to treat the topical skin condition.
Office action: search_report, dated 2017-12-06
Rejection reasons: novelty_epc_54
Prior art cited: ref_id: WO2015044857A1
ref_type: patent
severity: background
ref_id: WO2015044879A1
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severity: background
ref_id: US2015258119A1
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ref_id: WO2006051287A1
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ref_id: WO2011026076A2
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ref_id: US2005069499A1
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ref_id: US2006018937A1
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severity: background
ref_id: WO2017103719A1
ref_type: patent
severity: background
ref_id: WO2017103720A1
ref_type: patent
severity: background
ref_id: WO2011026076
ref_type: patent
severity: novelty_destroying
ref_id: US2005069499
ref_type: patent
severity: background
ref_id: US2006018937
ref_type: patent
severity: background
ref_id: WO2017103719
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severity: novelty_destroying
ref_id: WO2017103720
ref_type: patent
severity: novelty_destroying
Final disposition: pending (2017-12-06)