Pramoxine compositions
Inventors
BULSARA, Pallav Arvind • CLARKE, Martyn J. • Dinner, Dara Lisa • Shalviri, Alireza
Assignees
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Publication Number
US-11510856-B2
Publication Date
2022-11-29
Expiration Date
Abstract
The invention provides a topical o/w emulsion which moisturizes, and protects, repairs or restores the skin lipid barrier of a mammal. The topical o/w emulsion composition comprises: a) a discontinuous oil phase;b) a continuous aqueous phase comprising water;c) a thickening agent;d) at least one lamellar membrane structure comprising (i) a phospholipid, (ii) a fatty alcohol, and (iii) a fatty acid;e) a pharmaceutically acceptable active agent; andf) optionally a dermatologically acceptable excipient. In one embodiment, the composition, in use, has a water vapor transmission rate of less than or about 75 g·m−2·hr−1 measured in vitro using the modWVTR test methodology.
Core Innovation
The invention relates to a topical oil-in-water emulsion composition comprising a discontinuous oil phase, a continuous aqueous phase containing water and glycerine, and a thickening agent. The composition further comprises at least one lamellar membrane structure having a phospholipid component, a fatty alcohol component, a fatty acid component, and an ester of a branched fatty acid and a branched fatty alcohol component, with the components defined by specific weight percentage ranges and weight ratio constraints in the composition.
The lamellar membrane structure includes hydrogenated phosphatidylcholine as the phospholipid component, behenyl alcohol or a mixture of behenyl alcohol and cetyl alcohol as the fatty alcohol component, behenic acid as the fatty acid component, and isostearylisostearate as the branched fatty acid and branched fatty alcohol ester component. The lamellar ingredient weight ratios are constrained such that the fatty alcohol to phospholipid, the fatty alcohol to fatty acid, and the fatty alcohol to the ester each fall within about 10:1 to about 1:1.
The topical emulsion is characterized for skin occlusivity by requiring that, in use, the composition has a water vapor transmission rate of less than about 65 gm−2 hr−1 measured in vitro using the modWVTR test methodology. The composition includes 1% pramoxine, optionally as a pharmaceutically acceptable salt, and optionally a dermatologically acceptable excipient.
Claims Coverage
Independent claim 1 defines a topical oil-in-water emulsion composition with a discontinuous oil phase and glycerine-containing aqueous phase, defined lamellar membrane components with ratio constraints, required pramoxine, and an in-use in vitro modWVTR water vapor transmission rate requirement. Inventive content is concentrated in a single independent composition claim, with dependent claims refining component ratios, amounts, and excipient options, and an application claim providing a specific therapeutic use on skin.
Topical oil-in-water emulsion with discontinuous hydrogenated oil phase and glycerine-containing aqueous phase
A topical oil-in-water emulsion composition comprising from about 5% to about 70% of a discontinuous oil phase comprising hydrogenated castor oil, mineral oil, and caprylic/capric triglyceride, and from about 10% to about 90% of a continuous aqueous phase comprising water and from about 5% to about 15% by weight of glycerine, together with a thickening agent.
Lamellar membrane structure with specified phospholipid, fatty alcohol, fatty acid, and branched fatty ester components
At least one lamellar membrane structure comprising from about 0.5% to about 5% by weight of a phospholipid component comprising hydrogenated phosphatidylcholine, from about 2% to about 15% by weight of a fatty alcohol component comprising behenyl alcohol or a mixture of behenyl alcohol and cetyl alcohol, from about 0.25% to about 2.5% by weight of a fatty acid component comprising behenic acid, and from about 0.1% to about 5% by weight of an ester of a branched fatty acid and a branched fatty alcohol component comprising isostearylisostearate; wherein the fatty alcohol and the phospholipid are present in a weight ratio of from about 10:1 to about 1:1, the fatty alcohol and the fatty acid are present in a weight ratio of from about 10:1 to about 1:1, and the fatty alcohol and the ester are present in a weight ratio of from about 10:1 to about 1:1.
Pramoxine inclusion with optional excipient and modWVTR water vapor transmission performance
The composition further comprises 1% pramoxine, optionally as the pharmaceutically acceptable salt, and optionally a dermatologically acceptable excipient, wherein in use the composition has a water vapor transmission rate of less than about 65 gm−2 hr−1 measured in vitro using the modWVTR test methodology.
Coverage is centered on the composition architecture: a topical O/W emulsion with defined discontinuous oil and glycerine-containing aqueous phases, a thickening agent, and lamellar membrane structures formed from specified hydrogenated phospholipid, behenyl/cetyl fatty alcohol, behenic acid, and isostearylisostearate components under defined ratio constraints, combined with required pramoxine and a modWVTR water vapor transmission rate limit.
Stated Advantages
Improved skin occlusivity, indicated by a water vapor transmission rate of less than about 65 gm−2 hr−1 measured in vitro using the modWVTR test methodology.
Documented Applications
An effective amount of the topical oil-in-water emulsion composition applied to the skin of a mammal to provide local anesthesia.
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