# US 8,569,320 B2 · Topical composition for the treatment of actinic keratosis > Agents: this data is available as JSON from the patentgrep API and MCP server — see https://patentgrep.com/llms.txt - Number: US 8,569,320 B2 - Document ID: US8569320B2 - Status: Granted - Kind: B2 - Application number: 13/002,971 - Filed: 2009-06-29 - Published: 2011-12-08 - Granted: 2013-10-29 - Earliest claimed: 2008-07-07 - Assignees: Almirall Hermal GmbH - Applicants: Manfred Melzer; Carmen Matthies; Klaus Treudler; Christoph Willers; Henning Mallwitz - Inventors: Manfred Melzer; Carmen Matthies; Klaus Treudler; Christoph Willers; Henning Mallwitz - Web page: https://patentgrep.com/patent/US8569320B2 ## CPC - A61K 9/06: Ointments; Bases therefor; {Other semi-solid forms, e.g. creams, sticks, gels (composition of ointments, creams or gels A61K47/00)} - 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 31/196: the amino group being directly attached to a ring, e.g. anthranilic acid, mefenamic acid, diclofenac, chlorambucil - A61K 31/513: having oxo groups directly attached to the heterocyclic ring, e.g. cytosine - A61K 31/60: Salicylic acid; Derivatives thereof - A61K 45/06: Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca - A61K 47/32: Macromolecular compounds obtained by reactions only involving carbon-to-carbon unsaturated bonds, e.g. carbomers {, poly(meth)acrylates, or polyvinyl pyrrolidone} - A61P 17/00: Drugs for dermatological disorders - A61P 17/02: for treating wounds, ulcers, burns, scars, keloids, or the like - A61P 17/12: Keratolytics, e.g. wart or anti-corn preparations - A61P 35/00: Antineoplastic agents - A61P 37/02: Immunomodulators - A61P 43/00: Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00 - 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 invention relates to a topical gel composition for use in the treatment of actinic keratosis comprising (a) an active agent for treatment of actinic keratosis, (b) a keratolytically active agent, (c) a gel former, and (d) an organic solvent. ## Claims ### Claim 1 A method of treating actinic keratosis in a patient, said method comprising the step of: applying a topical gel composition to the affected area of skin, wherein the topical gel composition comprises: (a) 0.25 to 4.5 wt.-% of an active agent for treatment of actinic keratosis selected from the group consisting of cyclooxygenase inhibitors, topical immune modulators, antimetabolites, and mixtures thereof, (b) a keratolytically active agent selected from the group consisting of retinoid receptor agonists, urea, organic acids, and mixtures thereof, (c) a gel former, wherein the viscosity of the gel is in the range of 300 to 1500 m Pas at 20° C., and (d) an organic solvent, wherein said topical gel composition comprises less than 5 wt.-% water. ### Claim 2 (depends on 1) The method according to claim 1, wherein the active agent for treatment of actinic keratosis is selected from the group consisting of ibuprofen, diclofenac, etodolac, celecoxib, piroxicam, imiquimod, resimiquimod, sotirimod, and 5′-fluorouracil. ### Claim 3 (depends on 1) The method according to claim 1, wherein the keratolytically active agent is selected from the group consisting of adapalene, tretinoin, isotretinoin, motretinide, tazarotene, retinol, urea, glycolic acid, acetic acid, lactic acid, salicylic acid, and mixtures thereof. ### Claim 4 (depends on 1) The method according to claim 1, wherein the composition comprises less than 1 wt.-% water. ### Claim 5 (depends on 4) The method according to claim 4, wherein the composition is substantially free of water. ### Claim 6 (depends on 1) The method according to claim 1, wherein the viscosity of the gel is in the range of 300 to 1500 mPas at 20° C. ### Claim 7 (depends on 6) The method according to claim 6, wherein the viscosity of the gel is in the range of 600 to 900 mPas at 20° C. ### Claim 8 (depends on 1) The method according to claim 1, wherein the active agent for treatment of actinic keratosis is 5′-fluorouracil. ### Claim 9 (depends on 1) The method according to claim 1, wherein the composition comprises 0.4 to 1 wt.-% of the active agent for treatment of actinic keratosis. ### Claim 10 (depends on 1) The method according to claim 1, wherein the keratolytically active agent is selected from the group consisting of glycolic acid, acetic acid, lactic acid, salicylic acid, and mixtures thereof. ### Claim 11 (depends on 1) The method according to claim 1, wherein the keratolytically active agent is salicylic acid. ### Claim 12 (depends on 1) The method according to claim 1, wherein the composition comprises 0.025 to 30 wt.-% of the keratolytically active agent. ### Claim 13 (depends on 12) The method according to claim 12, wherein the composition comprises 5 to 15 wt.-% of the keratolytically active agent. ### Claim 14 (depends on 1) The method according to claim 1, wherein the gel former is selected from the group consisting of vinyl homopolymers and copolymers, cellulose derivatives, and mixtures thereof. ### Claim 15 (depends on 1) The method according to claim 1, wherein the composition comprises 1 to 30 wt.-% of the gel former. ### Claim 16 (depends on 15) The method according to claim 15, wherein the composition comprises 5 to 15 wt.-% of the gel former. ### Claim 17 (depends on 1) The method according to claim 1, wherein the organic solvent is selected from the group consisting of C1-C10 alcohols, esters of C1-C10 alcohols with C1-C10 carboxylic acids, and mixtures thereof. ### Claim 18 (depends on 17) The method according to claim 17, wherein the organic solvent comprises a C1-C6 alcohol and an ester of C1-C6 alcohol with a C2-C6 carboxylic acid. ### Claim 19 (depends on 1) The method according to claim 1, wherein the boiling point of the organic solvent is below 100° C. ### Claim 20 (depends on 19) The method according to claim 19, wherein the boiling point of the organic solvent is below 80° C. ### Claim 21 (depends on 1) The method according to claim 1, wherein the composition comprises 1 to 90 wt.-% of the organic solvent. ### Claim 22 (depends on 21) The method according to claim 21, wherein the composition comprises 60 to 75 wt.-% of the organic solvent. ### Claim 23 (depends on 1) The method according to claim 1, said composition further comprising a skin penetration enhancer. ### Claim 24 (depends on 23) The method according to claim 23, wherein the skin penetration enhancer is selected from the group consisting of polyvalent aliphatic C2-C10 alcohols, polyalkylene glycols having C2-C4 alkylene groups, nonalkoxylated ethers of polyvalent aliphatic C2-C10 alcohols and polyalkylene glycols having C2-C4 alkylene groups, azones, terpenes, terpenoides, pyrrolidones, sulfoxides, and mixtures thereof. ### Claim 25 (depends on 24) The method according to claim 24, wherein the skin penetration enhancer is dimethyl sulfoxide. ### Claim 26 (depends on 23) The method according to claim 23, wherein the composition comprises 1 to 50 wt.-% of the skin penetration enhancer. ### Claim 27 (depends on 26) The method according to claim 26, wherein the composition comprises 5 to 10 wt.-% of the skin penetration enhancer. ### Claim 28 (depends on 1) The method according to claim 1, wherein the composition comprises: 0.25 to 4.5 wt.-% of the active agent for treatment of actinic keratosis, 2 to 20 wt.-% of the keratolytically active agent, 2 to 20 wt.-% of the gel former, 40 to 70 wt.-% of an ester of a C1-C4 alcohol with a C2-C4 carboxylic acid, 5 to 30 wt.-% of a C1-C4 alcohol, and 3 to 15 wt.-% of the skin penetration enhancer. ### Claim 29 (depends on 8) The method according to claim 8, wherein the composition comprises: 0.25 to 4.5 wt.-% of 5′-fluorouracil, 2 to 20 wt.-% of salicylic acid, 2 to 20 wt.-% of gel former comprising a combination of a (meth)acrylate homopolymer or copolymer and a cellulose derivative, 40 to 70 wt.-% of an ester of a C1-C4 alcohol with a C2-C4 carboxylic acid, 5 to 30 wt.-% of a C1-C4 alcohol, and 3 to 15 wt.-% of dimethylsulfoxide.