# US 2016/0038404 A1 · Anti-Malarial Pharmaceutical Composition > Agents: this data is available as JSON from the patentgrep API and MCP server — see https://patentgrep.com/llms.txt - Number: US 2016/0038404 A1 - Document ID: US20160038404A1 - Status: Published application - Kind: A1 - Application number: 14/808,707 - Filed: 2015-07-24 - Published: 2016-02-11 - Earliest claimed: 2007-10-25 - Assignees: Protopharma Limited - Applicants: Protopharma Limited - Inventors: Clive Booles; Calvin Ross; Martin Sams - Web page: https://patentgrep.com/patent/US20160038404A1 ## CPC - A61K 9/006: {Oral mucosa, e.g. mucoadhesive forms, sublingual droplets; Buccal patches or films; Buccal sprays} - A61K 9/0043: {Nose} - A61K 9/0073: {Sprays or powders for inhalation; Aerolised or nebulised preparations generated by other means than thermal energy; (nasal sprays A61K9/0043; inhalation of vapours of volatile or heated drugs, e.g. essential oils or nicotine, A61K9/007; devices A61M)} - A61K 31/357: having two or more oxygen atoms in the same ring, e.g. crown ethers, guanadrel - A61K 47/10: Alcohols; Phenols; Salts thereof, e.g. glycerol; Polyethylene glycols [PEG]; Poloxamers; PEG/POE alkyl ethers - A61K 47/14: Esters of carboxylic acids, e.g. fatty acid monoglycerides, medium-chain triglycerides, parabens or PEG fatty acid esters - A61M 11/001: {Particle size control} - A61M 11/006: {operated by applying mechanical pressure to the liquid to be sprayed or atomised} - A61M 15/009: {using medicine packages with incorporated spraying means, e.g. aerosol cans (pocket atomiser of the injector type A61M11/08)} - A61M 39/22: Valves or arrangement of valves {(A61M39/02, A61M39/0247, A61M39/16 take precedence; regulating valves in infusion systems A61M5/16881; in devices worn by the patient for the reception of urine, faeces, catamenial or other discharge, or in colostomy devices A61F5/4405)} - A61P 33/00: Antiparasitic agents - A61P 33/06: Antimalarials - Y02A 50/30: Against vector-borne diseases, e.g. mosquito-borne, fly-borne, tick-borne or waterborne diseases whose impact is exacerbated by climate change - 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) - A61M: DEVICES FOR INTRODUCING MEDIA INTO, OR ONTO, THE BODY (introducing media into or onto the bodies of animals A61D7/00; means for inserting tampons A61F13/26; devices for administering food or medicines orally A61J; containers for collecting, storing or administering blood or medical fluids A61J1/05); DEVICES FOR TRANSDUCING BODY MEDIA OR FOR TAKING MEDIA FROM THE BODY (surgery A61B; chemical aspects of surgical articles A61L); DEVICES FOR PRODUCING OR ENDING SLEEP OR STUPOR {(Electrotherapy, e.g. producing anaesthesia by the use of alternating or intermittent currents A61N1/36021)} - A61P: SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS - Y02A: TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE ## Abstract The invention provides pharmaceutical compositions for the treatment and prophylaxis of malaria, comprising artemether and a medium chain triglyceride formulated for transmucosal sublingual, buccal or nasal delivery, especially by a spray. Also provided are delivery devices containing the compositions. ## Claims ### Claim 1 A pharmaceutical composition comprising: artemether or arteether; and a pharmaceutically-acceptable excipient selected from the group consisting of: a medium chain length triglyceride; a short chain triglyceride; an omega-3-marine triglyceride; and a fish oil, rich in omega-3-acids; said composition formulated for transmucosal sublingual, buccal, or nasal dosage. ### Claim 2 (depends on 1) The composition according to claim 1 consisting essentially of: artemether or arteether; and one or more pharmaceutically-acceptable excipients selected from the group consisting of: a medium chain length triglyceride; a short chain triglyceride; an omega-3-marine triglyceride; and a fish oil, rich in omega-3-acids; said composition formulated for transmucosal sublingual, buccal, or nasal dosage. ### Claim 3 (depends on 1) The composition according to claim 1 comprising: artemether and a pharmaceutically-acceptable excipient selected from the group consisting of: a medium chain length triglyceride; a short chain triglyceride; an omega-3-marine triglyceride; and a fish oil, rich in omega-3-acids; said composition formulated for transmucosal sublingual, buccal, or nasal dosage. ### Claim 4 (depends on 1) The composition according to claim 1 consisting essentially of: artemether and one or more pharmaceutically-acceptable excipients selected from the group consisting of: a medium chain length triglyceride; a short chain triglyceride; an omega-3-marine triglyceride; and a fish oil, rich in omega-3-acids; said composition formulated for transmucosal sublingual, buccal, or nasal dosage. ### Claim 5 (depends on 1) The composition according to claim 1 consisting essentially of: artemether or arteether; and a pharmaceutically acceptable excipient consisting essentially of: a triglyceride which is liquid at 37° C. and a medium chain length triglyceride; said composition formulated for transmucosal sublingual, buccal, or nasal dosage. ### Claim 6 (depends on 1) The composition according to claim 1, substantially free of water. ### Claim 7 (depends on 1) The composition according to claim 1, substantially free of ethanol. ### Claim 8 (depends on 1) The composition according to claim 1, wherein artemether or arteether is present at a concentration of between 2 and 250 milligrams per gram of excipient. ### Claim 9 (depends on 1) The composition according to claim 1, wherein said excipient comprises a medium chain length triglyceride, said triglyceride comprising a minimum of 95 percent of saturated fatty acids with between 6 and 12 carbon atoms. ### Claim 10 (depends on 8) The composition according to claim 8, wherein said excipient comprises a medium chain length triglyceride, said triglyceride comprising a minimum of 95 percent of saturated fatty acids with 8 and 10 carbon atoms. ### Claim 11 (depends on 1) The composition according to claim 1, further comprising an essential oil selected from the group consisting of menthol, vanillin oil, orange oil, lemon oil, clove oil, peppermint oil, and spearmint oil. ### Claim 12 (depends on 1) A method of treating malaria, comprising the administration to a patient in need thereof a therapeutically effective amount of a composition according to claim 1 for the treatment or prophylaxis of malaria. ### Claim 13 (depends on 1) The composition according to claim 1, wherein the composition is formulated for sublingual delivery. ### Claim 14 (depends on 1) A medicament delivery device containing a composition according to claim 1, said device adapted to deliver individual or successive doses of said composition, each individual or successive dose having a volume of less than 1000 microlitres. ### Claim 15 (depends on 1) A medicament delivery device containing a composition according to claim 1, said device and composition adapted to deliver individual or successive doses of said composition, each individual or successive dose containing no more than 80 mg of artemether or arteether. ### Claim 16 (depends on 1) A medicament delivery device containing a composition according to claim 1, said device and composition adapted to deliver individual or successive doses of said composition, each individual or successive dose containing no more than 10 mg of artemether or arteether. ### Claim 17 (depends on 14) The delivery device according to claim 14, wherein said device comprises a pump spray. ### Claim 18 (depends on 17) The delivery device according to claim 17, wherein said device is adapted to produce a spray of composition having a mean droplet diameter greater than 20 microns. ### Claim 19 (depends on 1) A device for providing pharmaceutical doses comprising a container containing a pharmaceutical composition according to claim 1 and a valve means arranged to transfer doses of said pharmaceutical composition to the exterior of the container. ### Claim 20 (depends on 1) A kit for the treatment or prophylaxis of malaria comprising a composition according to claim 1 and instructions to administer said composition to a patient in need thereof by the transmucosal sublingual, buccal, or nasal route. ### Claim 21 A method of treating a disease responsive to artemether or arteether, comprising the administration to a patient in need thereof of a therapeutically effective amount of artemether or arteether by the transmucosal sublingual, buccal, or nasal route. ### Claim 22 (depends on 21) A method of treating a disease responsive to artemether as in claim 21, comprising the administration to a patient in need thereof of a therapeutically effective amount of artemether by the transmucosal sublingual, buccal, or nasal route. ### Claim 23 (depends on 21) The method according to claim 21, wherein said administration is by the sublingual route. ### Claim 24 (depends on 21) The method according to claim 21, wherein said disease is malaria.