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Publication Number
US-10369135-B2
Publication Date
2019-08-06
Expiration Date
Abstract
The present invention relates to compositions, in particular for the treatment of hyperthyreosis (also designated hyperthyroidism), especially in cats. These compositions are formulated for transdermal administration of an active substance and may, for example, be applied into the auricle (or pinna) of the cat. They comprise an active agent such as methimazole (or 2-mercapto-1-methylimidazole) or carbimazole, at least one wax, at least one fatty oil, and optionally an emulsifier. As emulsifier a nanocarrier may be used, for example. Unimolecular nanocarriers of dendritic structure are preferred, wherein the nanocarrier comprises a dendritic core and at least two shells, wherein an inner shell is coupled to the dendritic core via a first linker, and an outer shell is coupled to the inner shell via a second linker. In one embodiment, the composition is provided as a stick, in another, a semi-solid formulation in a suitable applicator which may contain one or more dosage units.
Core Innovation
A water-free composition for transdermal hyperthyreosis treatment is provided that includes an active agent selected from methimazole and/or carbimazole, beeswax, at least one fatty oil selected from peanut oil, almond oil, sunflower oil, linseed oil, olive oil, and evening primrose oil, and an emulsifier. The composition is free of water and is formulated for transdermal pharmaceutical administration.
The emulsifier is a unimolecular nanocarrier comprising a dendritic core and at least two shells. The dendritic core is made of polyglycerol, the inner shell is an alkyl chain with a carbon length of C2 to C40, and the outer shell is polyethylene glycol having the structural formula (—CH2—H2O—)n with n=3-130 and bears a terminal methyl group, a hydroxyl group or a carboxyl group.
The first linker is an ester or amide linkage and the second linker is an ester bond, or any combination thereof. The composition is claimed with specified formulation ranges for 2.5-15% (w/w) active agent, 5-18% (w/w) beeswax, 45-75% (w/w) fatty oil, and 0.25 to 3.5% (w/w) emulsifier, and includes product formats such as grease stick and semi-solid applicator formats.
Claims Coverage
The independent claim covers a water-free transdermal hyperthyreosis formulation with four inventive features: specified composition ranges, a unimolecular nanocarrier emulsifier, a defined dendritic-core/inner-shell/outer-shell architecture, and a transdermal product format. Dependent refinements also direct treatment use.
Water-free nanocarrier emulsified transdermal composition for hyperthyreosis
A composition comprising 2.5-15% (w/w) of an active agent selected from methimazole and/or carbimazole; 5-18% (w/w) beeswax; 45-75% (w/w) of at least one fatty oil selected from peanut oil, almond oil, sunflower oil, linseed oil, olive oil, and evening primrose oil; and 0.25 to 3.5% (w/w) of at least one emulsifier comprising a unimolecular nanocarrier, wherein the composition is free of water.
Dendritic core/inner shell/outer shell nanocarrier architecture with specific linkers
A unimolecular nanocarrier in which the dendritic core is made of polyglycerol; the inner shell is an alkyl chain with a carbon length of C2 to C40; the outer shell is polyethylene glycol having structural formula (—CH2—H2O—)n with n=3-130 bearing a terminal methyl group, a hydroxyl group or a carboxyl group; the first linker is an ester or amide linkage; and the second linker is an ester bond, or any combination thereof.
Transdermal administration formulation
A composition formulated for transdermal administration.
Treatment of hyperthyreosis by administration of the defined composition
A method of treating hyperthyreosis by administering a composition as defined in claim 1 to a patient.
Grease stick or applicator-contained lipophilic formulation
A grease stick or lipophilic formulation provided in a suitable applicator.
Overall claim coverage centers on a specific water-free lipophilic composition for transdermal hyperthyreosis treatment that uses methimazole and/or carbimazole with beeswax and fatty oil, emulsified by a unimolecular dendritic nanocarrier defined by a polyglycerol dendritic core, an alkyl inner shell, a PEG outer shell, and ester/amide first and ester second linkers. Dependent refinements further direct transdermal use, a treatment method, and product format in grease stick or applicator-contained formulations.
Stated Advantages
Reduced agent amount.
Fewer GI side effects versus oral administration.
Potential avoidance of contact gloves.
Documented Applications
Transdermal administration of a hyperthyreosis treatment composition.
Method of treating hyperthyreosis in a patient by administering the defined composition.
Grease stick or applicator format use for a lipophilic formulation.
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