# US 2013/0157985 A1 · Pain relief compositions, manufacture and uses > Agents: this data is available as JSON from the patentgrep API and MCP server — see https://patentgrep.com/llms.txt - Number: US 2013/0157985 A1 - Document ID: US20130157985A1 - Status: Published application - Kind: A1 - Application number: 13/609,100 - Filed: 2012-09-10 - Published: 2013-06-20 - Earliest claimed: 2011-09-09 - Assignees: API Genesis, LLC - Inventors: Daniel BUCKS; Philip J. BIRBARA - Web page: https://patentgrep.com/patent/US20130157985A1 ## CPC - A61K 31/165: having aromatic rings, e.g. colchicine, atenolol, progabide - 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 9/06: Ointments; Bases therefor; {Other semi-solid forms, e.g. creams, sticks, gels (composition of ointments, creams or gels A61K47/00)} - A61K 9/08: Solutions {(composition of solutions A61K47/00)} - A61K 31/045: Hydroxy compounds, e.g. alcohols; Salts thereof, e.g. alcoholates - A61K 31/05: Phenols {(cannabinoids A61K31/658)} - A61K 31/125: Camphor; Nuclear substituted derivatives thereof - A61K 31/196: the amino group being directly attached to a ring, e.g. anthranilic acid, mefenamic acid, diclofenac, chlorambucil - A61K 31/35: having six-membered rings with one oxygen as the only ring hetero atom - A61K 31/351: not condensed with another ring - A61K 31/352: condensed with carbocyclic rings, e.g. methantheline {(cannabinoids A61K31/658)} - A61K 31/513: having oxo groups directly attached to the heterocyclic ring, e.g. cytosine - A61K 31/60: Salicylic acid; Derivatives thereof - A61K 31/618: having the carboxyl group in position 1 esterified, e.g. salsalate - A61K 45/06: Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca - A61K 47/10: Alcohols; Phenols; Salts thereof, e.g. glycerol; Polyethylene glycols [PEG]; Poloxamers; PEG/POE alkyl ethers - A61P 1/02: Stomatological preparations, e.g. drugs for caries, aphtae, periodontitis - A61P 11/02: Nasal agents, e.g. decongestants - A61P 13/10: of the bladder - A61P 15/00: Drugs for genital or sexual disorders (for disorders of sex hormones A61P5/24); Contraceptives - A61P 17/00: Drugs for dermatological disorders - A61P 17/04: Antipruritics - A61P 17/06: Antipsoriatics - A61P 19/02: for joint disorders, e.g. arthritis, arthrosis - A61P 25/04: Centrally acting analgesics, e.g. opioids - A61P 25/06: Antimigraine agents - A61P 29/00: Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID] - A61P 31/22: for herpes viruses - 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 present invention relates to TRPV1 selective agonist topical compositions including capsaicinoid and analgesic agent compositions and methods of manufacture and methods of providing pain relief as well as treating a variety of disorders with such compositions. ## Claims ### Claim 1 A composition comprising: i) 0.075-30% by weight of a TRPV1 selective agonist, and ii) 50-95% by weight of an analgesic agent comprising a) a topical salicylate and b) TRPM8 agonist or a TRPV3 agonist, capable of solubilizing said TRPV1 selective agonist, wherein said composition has an amount of TRPV1 selective agonist sufficient to decrease the density of functional nociceptive nerve fibers when said composition is applied topically, and said composition has an amount of analgesic agent sufficient to eliminate or reduce the burning and/or stinging sensation or erythema created by the topical administration of the TRPV1 selective agonist. ### Claim 2 A composition comprising: 0.075-30% by weight of a TRPV1 selective agonist, and 70-95% by weight of an analgesic agent capable of solubilizing said TRPV1 selective agonist, wherein said composition has an amount of TRPV1 selective agonist sufficient to decrease the density of functional nociceptive nerve fibers when said composition is applied topically, and said composition has an amount of analgesic agent sufficient to eliminate or reduce the burning and/or stinging sensation or erythema created by the topical administration of the TRPV1 selective agonist, and wherein said composition does not include turpentine oil. ### Claim 3 (depends on 1, 2) A composition as in claim 1 or 2 wherein said analgesic agent is a topical salicylate, a TRPM8 agonist, and a TRPV3 agonist. ### Claim 4 (depends on 1, 2) A composition as in claim 1 or 2 wherein the composition is a liquid solution. ### Claim 5 (depends on 1) A composition as in claim 1 comprising: i) 0.2-20% by weight of said TRPV1 selective agonist, ii) 50-95% by weight of said analgesic agent. ### Claim 6 (depends on 1) A composition as in claim 1 comprising: 2-20% by weight of said TRPV1 selective agonist, 50-95% by weight of said analgesic agent. ### Claim 7 (depends on 1) A composition as in claim 1 wherein said TRPV1 selective agonist is a vanilloid. ### Claim 8 (depends on 1) A composition as in claim 1 wherein said TRPV1 selective agonist is a capsaicinoid. ### Claim 9 (depends on 1) A composition as in claim 1 wherein said TRPV1 selective agonist is capsaicin. ### Claim 10 (depends on 1) A composition as in claim 1 wherein said TRPV1 selective agonist is trans-capsaicin or nonivamide. ### Claim 11 (depends on 1) A composition as in claim 1 wherein said TRPM8 agonist is menthol, icilin or eucalyptol. ### Claim 12 (depends on 1) A composition as in claim 1 wherein the TRPV3 agonist is camphor. ### Claim 13 (depends on 1, 2) A composition as in claim 1 or 2 wherein said analgesic agent is i) methyl salicylate and ii) menthol or camphor. ### Claim 14 (depends on 1, 2) A composition as in claim 1 or 2 wherein said analgesic agent is i) methyl salicylate, ii) menthol, and iii) camphor. ### Claim 15 (depends on 1) A composition as in claim 1 wherein said analgesic agent is methyl salicylate, menthol and phenol. ### Claim 16 (depends on 1, 2) A composition as in claim 1 or 2 wherein said analgesic agent is methyl salicylate, camphor, and phenol. ### Claim 17 (depends on 1, 2) A composition as in claim 1 or 2 further comprising an alcohol. ### Claim 18 (depends on 1) A composition as in claim 1 comprising: 0.20-30% by weight of a capsaicinoid, 30-70% by weight methyl salicylate, 1-20% by weight menthol, and 1-20% by weight camphor, wherein the percentage by weight of the methyl salicylate, menthol, and camphor is greater than 50% of the composition. ### Claim 19 (depends on 1) A composition as in claim 1 comprising: 0.20-30% by weight of a capsaicinoid, 30-75% by weight methyl salicylate and/or ethanol, 1-20% by weight menthol, and 1-20% by weight camphor, wherein the percentage by weight of the methyl salicylate, menthol, and camphor is greater than 50% of the composition. ### Claim 20 (depends on 1) A composition as in claim 1 comprising: 0.20-30% by weight of a capsaicinoid, 40-75% by weight methyl salicylate, 10-25% ethanol, 10-20% by weight menthol, and 10-20% by weight camphor, wherein the percentage by weight of the methyl salicylate, menthol, and camphor is greater than 50% of the composition. ### Claim 21 (depends on 1) A composition as in claim 1 comprising: 0.20-30% by weight of a capsaicin, 40-75% by weight methyl salicylate 10-25% ethanol, 10-20% by weight menthol, 10-20% by weight camphor, and 0.5-5% phenol, wherein the percentage by weight of the methyl salicylate, menthol, camphor and phenol is greater than 50% of the composition. ### Claim 22 (depends on 19) A composition as in claim 19, further comprising glycerol. ### Claim 23 (depends on 22) A composition as in claim 22 wherein said composition is a gel. ### Claim 24 (depends on 1) A composition as in claim 1, further comprising a flavonoid. ### Claim 25 (depends on 1) A composition as in claim 1, further comprising an anti-inflammatory agent. ### Claim 26 (depends on 1) A composition as in claim 1, further comprising a surfactant. ### Claim 27 (depends on 1) A composition as in claim 1, further comprising an NSAID. ### Claim 28 (depends on 27) A composition as in claim 27, wherein the NSAID is selected from the group consisting of aspirin, ibuprofen, naproxen, ketoprofen, and diclofenac. ### Claim 29 (depends on 28) A composition of claim 28, wherein the NSAID is diclofenac sodium. ### Claim 30 (depends on 1) A composition as in claim 1, further comprising an odor reducing agent. ### Claim 31 A composition comprising: 70-95% by weight methyl salicylate and/or ethanol, 10-20% by weight menthol, and 10-20% by weight camphor, and optionally 0.5-5.0% by weight phenol, wherein the percentage by weight of the methyl salicylate, menthol, and camphor is greater than 70% of the composition. ### Claim 32 (depends on 1, 31) A composition as in claim 1 or 31 further comprising phenol. ### Claim 33 A composition comprising: a capsaicinoid, methyl salicylate and/or ethyl alcohol, and phenol, wherein the percentage by weight of the methyl salicylate and phenol is greater than 50% of the composition. ### Claim 34 (depends on 33) A composition as in claim 33 comprising: 0.075-30% by weight of a capsaicinoid compound, 30-75% by weight methyl salicylate and/or ethyl alcohol, and 0.5-5% phenol. ### Claim 35 (depends on 18, 33) A composition as in claim 18 or 33, wherein the capsaicinoid compound is trans-capsaicin or nonivamide. ### Claim 36 (depends on 1) A method of treating pain in a mammal suffering from pain comprising topically administering the composition of claim 1 to said mammal. ### Claim 37 (depends on 36) A method as in claim 36 wherein said mammal is a human. ### Claim 38 (depends on 36) A method as in claim 36 further comprising administering an NSAID. ### Claim 39 (depends on 38) A method as in claim 38, wherein the NSAID is administered by a different route than the TRPV-1 selective agonist composition. ### Claim 40 (depends on 38) A method as in claim 38, wherein the NSAID is administered orally or parentally. ### Claim 41 (depends on 1) A method of reducing the density of nociceptor nerve fibers in the dermis and epidermis of a selected region of a mammal, comprising administering the composition of claim 1 to said region. ### Claim 42 (depends on 41) A method as in claim 41 wherein said mammal suffers from a capsaicin responsive condition. ### Claim 43 (depends on 42) A method as in claim 42 wherein the capsaicin responsive condition is pain including neuropathic pain, inflammatory hyperalgia, vulvodynia, interstitial cystitis, rhinitis, burning mouth syndrome, oral mucositis, herpes, dermatitis, pruritus, tinnitus, psoriasis, or headaches. ### Claim 44 (depends on 1) A method of treating arthritis pain in a mammal comprising topically administering the composition of claim 1. ### Claim 45 (depends on 44) A method as in claim 44 wherein said arthritis is osteoarthritis or rheumatoid arthritis. ### Claim 46 (depends on 1) A method of treating itching in a mammal comprising topically administering the composition of claim 1. ### Claim 47 A method of formulating a capsaicinoid liquid comprising: dissolving a capsaicinoid in methyl salicylate and/or ethanol to form a solution, and adding camphor and/or menthol to the solution. ### Claim 48 A method of producing a topical formulation of capsaicin comprising: mixing a capsaicinoid and methyl salicylate and/or ethanol, and adding one or more of methyl salicylate, camphor and phenol. ### Claim 49 (depends on 1) A kit comprising: i) a liquid composition as in claim 1, and ii) a non occlusive applicator device. ### Claim 50 (depends on 49) A kit as in claim 49 further comprising a cleaning solution for removal of residual agonist.