Topical steroid ointment formulations
AssigneeE. R. Squibb & Sons, Inc.
InventorsJames Ling Chen, Jean M. Battaglia
Life of this patent
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Abstract
Steroid ointment formulations of the solution and biphasic types which are used as topical anti-inflammatory agents are provided wherein the steroid, such as 21-chloro-9.alpha.-fluoro-.DELTA..sup.4 -pregnene-11.beta.,16.alpha.,17.alpha.-triol-3,20-dione 16,17-acetonide, is at least partially dissolved in a ricinoleate vehicle such as castor oil.
Claims22
A non-aqueous composition for topical application in the form of an ointment, gel or lipophilic stick comprising at least one steroid selected from the group consisting of 21-chloro-9.alpha.-fluoro-.DELTA..sup.4 -pregnene-11.beta.,16.alpha.,17.alpha.-triol-3,20-dione 16,17-acetonide;
- 21-chloro-9-fluoro-2',3'-dihydro-11.beta.-hydroxy-5'-phenylpregna-1,4-dien o[16.alpha.,17-b][1,4]dioxin3,20-dione:dichloro methane solvate (1:1), and 9.alpha.-fluoro-11.beta.,16.alpha.,17,21-tetrahydroxy-pregna-1,4-diene-3,2 0-dione 16,17-acetonide, a ricinoleate vehicle in which said steroid is at least partially soluble, and an oleaginous material, said oleaginous material is selected from the group consisting of petrolatum, mineral oil thickened or gelled with polyethylene, high molecular weight paraffin waxes, mono and diglycerides of fatty acids gelled with high molecular weight fatty acids or polyamide complex of hydroxystearate, propylene glycol isostearate or isostearyl alcohol gelled with high molecular weight fatty acids and mixtures thereof.
A composition useful as a vehicle for steroids in the form of a clear lipophilic gel comprising a ricinoleate and an oleaginous material, said ricinoleate being present in an amount within the range of from about 0.5 to about 16% by weight of the composition, said oleaginous material being present in an amount within the range of from about 85 to about 94% by weight of the composition and comprising petrolatum, a mixture of mineral oil gelled with polyethylene, paraffin wax or a mixture of mono and diglycerides of fatty acids gelled with polyamide complex of hydroxystearate or high molecular weight fatty acids as a mixture having a molecular weight of at least 450 having a melting range of 67.degree.-73.degree. C, and a steroid present in an amount within the range of from about 0.005 to about 0.6% by weight of the total composition, said steroid being selected from the group consisting of 21-chloro-9.alpha.-fluoro-.DELTA..sup.4 -pregnene-11.beta.,16.alpha.,17.alpha.-triol-3,20-dione 16,17-acetonide;
- 21-chloro-9-fluoro-2',3' -dihydro-11.beta.-hydroxy-5'-phenylpregna-1,4-dieno[16.alpha.,17-b][1,4]di oxin-3,20-dione:dichloro methane solvate (1:1), and 9.alpha.-fluoro-11.beta.,16.alpha.,17,21-tetrahydroxy-pregna-1,4-diene-3,2 0-dione 16,17-acetonide.
A composition useful as a vehicle for steroids in the form of a lipophilic stick, comprising a ricinoleate and an oleaginous material selected from the group consisting of petrolatum, mineral oil thickened or gelled with polyethylene, high molecular weight paraffin waxes, mono and diglycerides of fatty acids gelled with high molecular weight fatty acids or polyamide complex of hydroxystearate, propylene glycol isostearate or isostearyl alcohol gelled with high molecular weight fatty acids and mixtures thereof, said ricinoleate being present in an amount within the range of from about 50 to about 70% by weight of the composition and said oleaginous material being present in an amount within the range of from about 20 to about 50% by weight of the composition, and a steroid present in an amount within the range of from about 0.005 to about 0.6% by weight of the total composition said steroid being selected from the group consisting of 21-chloro-9-fluoro-2',3'-dihydro-11.beta.-hydroxy-5'-phenylpregna-1,4-dien o[16.alpha.,17-b][1,4]dioxin-3,20-dione:dichloro methane solvate (1:1), 21-chloro-9.alpha.-fluoro-.DELTA..sup.4 -pregnene-11.beta.,16.alpha.,17.alpha.-triol-3,20-dione 16,17-acetonide, and 9.alpha.-fluoro-11.beta.,16.alpha.,17,21-tetrahydroxypregna-1,4-diene-3,20 -dione 16,17-acetonide.
Dependencies are inferred from the claim text.