Econazole composition and methods of treatment therewith
Inventors
Hensby, Christopher N. • Silvander, Mats
Assignees
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Publication Number
US-9358209-B2
Publication Date
2016-06-07
Expiration Date
Abstract
The invention provides a water-based composition for treating an infection by a dermatophyte fungus comprising econazole or a pharmaceutically acceptable salt thereof. Also provided are methods of treatment utilizing the water-based foam composition, as well as its preparation.
Core Innovation
The disclosed invention is a water-based topical econazole antifungal formulation provided as an aerosol canister composition, in which econazole nitrate is combined with stearic acid substantially in an ionized form, povidone, humectants, dimethicone, triethanolamine, polysorbate 20, water, and one or more propellants. The composition has a pH in the range of 6-9 and is described as a foamable formulation suitable for aerosol delivery.
The problem addressed is treatment of skin infections caused by dermatophyte fungus and candida yeast, including tinea pedis, tinea cruris, tinea corporis, tinea versicolor, and cutaneous candidiasis. The disclosed antifungal activity is associated with azole antifungals, where inhibition of 14α-demethylase is discussed in relation to ergosterol.
The formulation vehicle, based on silicone oil emollient, fatty acids, and polymers, humectants, and emulsifying agents, is further linked to wound-healing and anti-inflammation activity. Documented studies include an animal split-thickness graft wound model, irritation and sensitization assessments for the vehicle, antimicrobial effect testing, and a multi-center clinical trial for tinea pedis supporting comparable efficacy and safety outcomes, including mycological cure endpoints.
In the disclosed context, the invention is also described for application prior to skin/mucosa piercing, and formulation component options include ionized fatty acid formation and specific azole salt forms such as econazole nitrate, together with pH control within 6-9 for the water-based topical composition presented in aerosol and foam format.
Claims Coverage
One independent claim is provided: an aerosol canister composition. The claim contains three inventive features, centered on the specific combination and proportioning of econazole nitrate with ionized stearic acid, povidone, humectants, silicone oil, triethanolamine, polysorbate 20, water, propellants, and a pH range of 6-9.
Aerosol canister composition with econazole nitrate, ionized stearic acid and defined vehicle components
An aerosol canister consisting of 0.5-1.5% by weight econazole nitrate, 6-8% by weight stearic acid substantially in an ionized form, 0.9-2.9% by weight of povidone, 6-9% by weight of humectants (propylene glycol and/or glycerol), 0.5-2.0% by weight of dimethicone, 2-3% by weight triethanolamine, 1-4% by weight polysorbate 20, water, and one or more propellants.
pH control in the 6-9 range
The composition has a pH in the range of 6-9.
Ingredient weight percentages defined exclusive of propellants
The weight % of the above ingredients are provided exclusive of the one or more propellants present in the composition.
The claim coverage centers on an aerosol canister for a water-based econazole nitrate formulation that combines an ionized stearic acid component with povidone, propylene glycol and/or glycerol humectants, dimethicone, triethanolamine, and polysorbate 20, with water and propellants, and a defined pH range of 6-9.
Stated Advantages
Non-irritating.
Non-sensitizing.
Non-greasy.
Non-watery.
Non-comedogenic.
Wound-healing activity.
Anti-inflammation activity.
Documented Applications
Treatment of tinea pedis, tinea cruris, tinea corporis, and tinea versicolor.
Treatment of cutaneous candidiasis.
Application prior to skin/mucosa piercing.
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