# US 10,369,135 B2 · Formulations for treatment of hyperthyroidism > Agents: this data is available as JSON from the patentgrep API and MCP server — see https://patentgrep.com/llms.txt - Number: US 10,369,135 B2 - Document ID: US10369135B2 - Status: Granted - Kind: B2 - Application number: 15/311,030 - Filed: 2015-05-12 - Published: 2017-05-25 - Granted: 2019-08-06 - Earliest claimed: 2014-05-13 - Assignees: Dendropharm GmbH - Applicants: Dendropharm GmbH - Inventors: Sam Moré - Web page: https://patentgrep.com/patent/US10369135B2 ## CPC - A61K 31/4164: 1,3-Diazoles - A61K 9/0014: {Skin, i.e. galenical aspects of topical compositions (non-active ingredients are additionally classified in A61K47/00; A61K9/0009, A61K9/0021, A61K9/7015, A61K9/7023 take precedence; cosmetic preparations A61K8/00, A61Q; preparations for wound dressings or bandages A61L26/00)} - A61K 9/0017: {Non-human animal skin, e.g. pour-on, spot-on} - A61K 9/0046: {Ear} - A61K 31/164: of a carboxylic acid with an aminoalcohol, e.g. ceramides - A61K 31/355: Tocopherols, e.g. vitamin E - A61K 47/14: Esters of carboxylic acids, e.g. fatty acid monoglycerides, medium-chain triglycerides, parabens or PEG fatty acid esters - A61K 47/32: Macromolecular compounds obtained by reactions only involving carbon-to-carbon unsaturated bonds, e.g. carbomers {, poly(meth)acrylates, or polyvinyl pyrrolidone} - A61K 47/44: Oils, fats or waxes according to two or more groups of A61K47/02-A61K47/42; Natural or modified natural oils, fats or waxes, e.g. castor oil, polyethoxylated castor oil, montan wax, lignite, shellac, rosin, beeswax or lanolin (synthetic glycerides, e.g. medium-chain triglycerides, A61K47/14) - A61P 5/14: of the thyroid hormones, e.g. T3, T4 - A61P 5/16: for decreasing, blocking or antagonising the activity of the thyroid hormones - A61K: PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES (devices or methods specially adapted for bringing pharmaceutical products into particular physical or administering forms A61J3/00; chemical aspects of, or use of materials for deodorisation of air, for disinfection or sterilisation, or for bandages, dressings, absorbent pads or surgical articles A61L; soap compositions C11D) - A61P: SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS ## 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. ## Claims ### Claim 1 A composition comprising a) 2.5-15% (w/w) of an active agent selected from the group comprising methimazole and/or carbimazole; b) 5-18% (w/w) beeswax; c) 45-75% (w/w) of at least one fatty oil selected from the group consisting of peanut oil, almond oil, sunflower oil, linseed oil, olive oil, and evening primrose oil; and d) 0.25 to 3.5% (w/w) of at least one emulsifier comprising a unimolecular nanocarrier, wherein the nanocarrier is composed of 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; wherein a) the dendritic core of the nanocarrier is made of polyglycerol, b) the inner shell of the nanocarrier is an alkyl chain with a carbon length of C2 to C40, c) the outer shell is polyethylene glycol having the structural formula (—CH2—H2O—)n, with n=3-130, which bears a terminal a methyl group, a hydroxyl group or a carboxyl group, d) the first linker is an ester or amide linkage, e) the second linker is an ester bond, or any combination thereof; and wherein the composition is free of water. ### Claim 2 (depends on 1) The composition according to claim 1, wherein the active substance is methimazole. ### Claim 3 (depends on 1) The composition according to claim 1, wherein the active substance is carbimazole. ### Claim 4 (depends on 1) The composition according to claim 1, wherein the beeswax is cera alba. ### Claim 5 (depends on 1) The composition according to claim 1, wherein the fatty oil is almond oil. ### Claim 6 (depends on 1) The composition according to claim 1, wherein a) the dendritic core of the nanocarrier is made of polyglycerol with a molecular weight of 3-20 kDa; b) the inner shell of the nanocarrier is a linear alkyl chain with a carbon length of C2 to C40; c) the outer shell is polyethylene glycol having the structural formular (—CH2—H2)—)n, with n=3-130, which bears a terminal a methyl group, a hydroxyl group or a carboxyl group; d) the first linker is an ester or amide linkage; e) the second linker is an ester bond; or any combination thereof. ### Claim 7 (depends on 1) The composition according to claim 1, wherein the nanocarrier is polyglyceroldodecanic acid polyethylenglycolate or polyglycerol pentadecanoic acid polyethylene glycolate. ### Claim 8 (depends on 1) The composition according to claim 1, further comprising dexpanthenol. ### Claim 9 (depends on 1) The composition according to claim 1, which is a grease stick or comprises a grease stick, or a lipophilic formulation in a suitable applicator or comprising the same. ### Claim 10 (depends on 1) The composition according to claim 1 which is a gel, an ointment, or a cream. ### Claim 11 (depends on 1) The composition according to claim 1, which is a pharmaceutical composition formulated for transdermal administration. ### Claim 12 (depends on 1) A method for the treatment of hyperthyreosis, comprising administering a composition according to claim 1 to a patient. ### Claim 13 (depends on 9, 12) The method of claim 12, comprising transdermally administering the lipophilic composition of claim 9 in an applicator for transdermal delivery of an active substance, selected from the group consisting of methimazole and carbimazole, to a cat. ### Claim 14 (depends on 1) The composition according to claim 1, wherein a) the dendritic core of the nanocarrier is made of polyglycerol with a molecular weight of 3-20 kDa; b) the inner shell of the nanocarrier is a linear alkyl chain with a carbon length of C8-C14; c) the outer shell is polyethylene glycol having the structural formula (—CH2—H2O—)n, d) the first linker is an ester linkage; e) the second linker is an ester bond; or any combination thereof. ### Claim 15 (depends on 1) The composition according to claim 1, wherein a) the dendritic core of the nanocarrier is made of polyglycerol with a molecular weight of 3-20 kDa; b) the inner shell of the nanocarrier is a preferably linear alkyl chain with a carbon length of C2 to C40; c) the outer shell is polyethylene glycol having the structural formulat (—CH2—H2)—)n, with n=3-130, which bears a terminal a methyl group, a hydroxyl group or a carboxyl group; d) the first linker is an ester or amide linkage; and e) the second linker is an ester bond.