Foamable composition combining a polar solvent and a hydrophobic carrier

Inventors

Tamarkin, Dov • Friedman, Doron • Eini, Meir • Besonov, Alex

Assignees

Vyne Therapeutics Inc

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Publication Number

US-10117812-B2

Patent

Publication Date

2018-11-06

Expiration Date


Abstract

The present invention relates to a foamable vehicle or cosmetic or pharmaceutical composition, comprising: (1) an organic carrier, at a concentration of 10% to 70% by weight, wherein said organic carrier concurrently comprises: (i) at least one hydrophobic organic carrier, and (ii) at least one polar solvent; (2) at least one surface-active agent; (3) water; and (4) at least one liquefied or compressed gas propellant at a concentration of 3% to 25% by weight of the total composition.The present invention further provides a method of treating, alleviating or preventing a disorder of mammalian subject, comprising administering the above-mentioned compositions to an afflicted target site.

Core Innovation

The invention provides a foamable pharmaceutical vehicle or composition supplied in an aerosol container, comprising a liquid organic carrier and water, and a liquefied or compressed gas propellant that upon release expands to form a breakable foam that collapses upon application of shear force. The liquid organic carrier concurrently comprises at least one hydrophobic organic carrier comprising a triglyceride and at least one polar solvent comprising dimethyl isosorbide. The composition further includes a surface-active agent system and a polymeric agent selected from a specified group of gelling, film-forming, bioadhesive, and/or phase-change polymeric agents.

The invention specifies the surface-active agent selection and relative non-ionic to ionic surfactant proportions, including at least one non-ionic surface-active agent, or a mixture of a non-ionic surface-active agent and an ionic surface-active agent, wherein the ratio of non-ionic surface-active agent to ionic surface-active agent is greater than 14:1. Water is present together with at least one liquefied or compressed gas propellant at a concentration of 3% to 25% by weight of the total composition. In the non-flammable embodiment, the propellant comprises at least one hydrofluorocarbon at the same concentration range.

The invention further defines that the aerosol foam is thermally stable yet breakable under shear, and that the formulation provides safety and skin benefits by counteracting polar solvent-induced drying and irritation through selection of a hydrophobic carrier and foam structure. It also describes polymeric and foam-adjuvant functionality as contributing to foam properties, including foam breakability and collapse behavior upon shear. The document describes multiple foam formulation examples and an inflammability test using specified foam formulations containing hydrofluorocarbon propellants, reporting non-flammable outcomes.

The invention is positioned for topical use by administering the foamed composition obtained from a canister to a surface having a disorder. Disorders explicitly listed include acne, an infection, an inflammation, psoriasis, and rosacea, and the method includes administering a foamed composition comprising the specified liquid organic carrier, surface-active agent system, water, propellant, polymeric agent, and an active agent. The document describes a broad list of active agents and herbal extracts used as part of the topical compositions, with the foam intended to collapse upon application of shear force during use.

Claims Coverage

The independent claims cover three main inventive aspects: a foamable pharmaceutical vehicle/composition with a specific liquid organic carrier pairing, a constrained surfactant system, water, propellant, polymeric agent, and a breakable foam outcome; a method of treating selected skin disorders topically using the foamable aerosol composition and an active agent; and a non-flammable version of the foamable pharmaceutical aerosol composition using a hydrofluorocarbon propellant.

Breakable foam aerosol vehicle with triglyceride and dimethyl isosorbide carrier

A foamable pharmaceutical vehicle or composition in an aerosol container including a liquid organic carrier comprising at least one hydrophobic organic carrier comprising a triglyceride and at least one polar solvent comprising dimethyl isosorbide, water, a liquefied or compressed gas propellant (3% to 25% by weight), and a polymeric agent from a specified group, where release expands to form a breakable foam that collapses upon application of shear force.

Non-ionic/ionic surfactant system with ratio greater than 14:1

A surface-active agent selected from at least one non-ionic surface-active agent, or a mixture of a non-ionic surface-active agent and an ionic surface-active agent, wherein the ratio of non-ionic surface-active agent to ionic surface-active agent is greater than 14:1, used in the foamable pharmaceutical vehicle/composition.

Topical treatment method using foamable aerosol composition that collapses under shear

A method of treating or alleviating a disorder selected from acne, an infection, an inflammation, psoriasis, and rosacea by administering topically a foamed composition obtained from a canister comprising the foamable composition with the triglyceride and dimethyl isosorbide carrier, the constrained surface-active agent system, water, propellant, polymeric agent, and an active agent, wherein release expands to form a breakable foam that collapses upon application of shear force.

Non-flammable foamable pharmaceutical composition with hydrofluorocarbon propellant

A non-flammable foamable pharmaceutical composition comprising a liquid organic carrier including triglyceride and a polar solvent comprising dimethyl isosorbide and a diol, water, a surface-active agent system with non-ionic to ionic ratio greater than 14:1, at least one hydrofluorocarbon propellant (3% to 25% by weight), and a polymeric agent from a specified group, where release in an aerosol container expands to form a breakable foam that collapses upon application of shear force.

Across the independent claims, the core coverage is directed to an aerosol foamable pharmaceutical composition where the liquid organic carrier combines a triglyceride hydrophobic component with a dimethyl isosorbide polar solvent, the surfactant system is defined with a non-ionic dominant ratio greater than 14:1, and the release outcome is a breakable foam collapsing under shear; the method claim applies this to treating acne, infection, inflammation, psoriasis, and rosacea, and a separate independent claim defines a non-flammable version using hydrofluorocarbon propellant.

Stated Advantages

Thermally stable foam that is breakable and collapses upon application of shear force.

Counteracts polar solvent-induced drying and irritation through selection of a hydrophobic carrier and foam structure.

Provides improved spreadability and drip-free application compared to hydroalcoholic foams.

Non-flammable outcomes for specified hydrofluorocarbon-containing foam formulations based on an inflammability test.

Documented Applications

Topical treatment or alleviation of disorders selected from acne, an infection, an inflammation, psoriasis, and rosacea using a foamed composition administered from a canister.

Use of foamable compositions for dermatologic and mucosal disorders with many example active agents described in the document.

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