# US 7,611,727 B2 · Pharmaceutical composition for transdermal or transmucous administration > Agents: this data is available as JSON from the patentgrep API and MCP server — see https://patentgrep.com/llms.txt - Number: US 7,611,727 B2 - Document ID: US7611727B2 - Status: Granted - Kind: B2 - Application number: 10/436,380 - Filed: 2003-05-12 - Published: 2004-09-09 - Granted: 2009-11-03 - Earliest claimed: 2003-02-20 - Assignees: Besins International Belgique - Inventors: Brigitte Taravella; Valėrie Masini-Eteve - Web page: https://patentgrep.com/patent/US7611727B2 ## CPC - 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)} - A61P 5/24: of the sex hormones - A61P 5/26: Androgens - A61P 5/28: Antiandrogens - A61P 5/30: Oestrogens - A61P 5/32: Antioestrogens - A61K 47/02: Inorganic compounds - A61K 47/12: Carboxylic acids; Salts or anhydrides thereof - A61K 47/14: Esters of carboxylic acids, e.g. fatty acid monoglycerides, medium-chain triglycerides, parabens or PEG fatty acid esters - 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 a novel pharmaceutical composition for transdermal or transmucous administration of at least one active substance, and comprising especially a fatty acid as a percutaneous absorption promoter, at least one alcoholic vehicle and also a stabilizer capable of stabilizing the fatty acid in the said pharmaceutical composition. ## Claims ### Claim 1 A pharmaceutical composition for transdermal or transmucous administration of at least one active substance, comprising an active substance, a fatty acid percutaneous absorption promoter in an amount of between 0.1% and 20%, these percentages being expressed on a weight basis relative to 100 g of pharmaceutical composition, an alcoholic vehicle comprising an alcohol selected from the group consisting of ethanol and isopropanol, and a stabilizer capable of stabilizing the fatty acid in said pharmaceutical composition, wherein said stabilizer comprises the fatty acid ester of said fatty acid and said alcohol and is present in an amount of between 0.1% and 10%, these percentages being expressed on a weight basis relative to 100 g of pharmaceutical composition and wherein said composition is in the form of a gel or solution, and wherein the amount of said fatty acid percutaneous absorption promoter does not vary by more than +/−5% after storage for 6 months at 40° C. and 75% relative humidity. ### Claim 2 (depends on 1) A pharmaceutical composition according to claim 1, wherein the fatty acid is selected from the group consisting of capric acid, lauric acid, myristic acid, palmitic acid, stearic acid, oleic acid, palmitoleic acid, linoleic acid and linolenic acid. ### Claim 3 (depends on 1) A pharmaceutical composition according to claim 1, having a pH of between 4 and 10. ### Claim 4 (depends on 1) A pharmaceutical composition according to claim 1, wherein the fatty acid ester is selected from the group consisting of ethyl oleate, isopropyl oleate, isopropyl myristate, isopropyl palmitate, ethyl octanoate, ethyl dodecanoate, ethyl linoleate and ethyl linolenate. ### Claim 5 (depends on 1) A pharmaceutical composition according to claim 1, wherein the alcoholic vehicle comprises ethanol. ### Claim 6 (depends on 1) A pharmaceutical composition according to claim 1, having an alcoholic vehicle content of between 10% and 90%, these percentages being expressed on a weight basis relative to 100 g of pharmaceutical composition. ### Claim 7 (depends on 1) A pharmaceutical composition according to claim 1, further comprising a co-solvent selected from the group consisting of glycerol, propylene glycol, polyethylene glycol, and mixtures thereof. ### Claim 8 (depends on 7) A pharmaceutical composition according to claim 7, having a co-solvent content of between 0.5% and 20% these percentages being expressed on a weight basis relative to 100 g of pharmaceutical composition. ### Claim 9 (depends on 1) A pharmaceutical composition according to claim 1, being in the form of a gel, and-further comprising between 0.2% and 30% of a gelling agent, these percentages being expressed on a weight basis relative to 100 g of pharmaceutical composition. ### Claim 10 (depends on 9) A pharmaceutical composition according to claim 9, wherein the gelling agent is selected from the group consisting of carbomers, non-preneutralized acrylic polymers, cellulose derivatives, poloxamers, poloxamines, chitosan, dextran pectins, natural gums, and mixtures thereof. ### Claim 11 (depends on 9) A pharmaceutical composition according to claim 9, further comprising a neutralizer. ### Claim 12 (depends on 11) A pharmaceutical composition according to claim 11, wherein the neutralizer is selected from the group consisting of triethanolamine, sodium hydroxide, ammonium hydroxide, potassium hydroxide, arginine, aminomethylpropanol and tromethamine, and mixtures thereof. ### Claim 13 (depends on 11) A pharmaceutical composition according to claim 11, wherein the neutralizer/gelling agent ratio is between 10/1 and 0.1/1. ### Claim 14 (depends on 1) A pharmaceutical composition according to claim 1, wherein the active substance is selected from the group consisting of oestrogens, progestins, androgens, anti-oestrogens and anti-androgens, or mixtures thereof. ### Claim 15 (depends on 14) A pharmaceutical composition according to claim 14, having an active substance content of between 0.01% and 5%, these percentages being expressed on a weight basis relative to 100 g of pharmaceutical composition. ### Claim 16 (depends on 1) A pharmaceutical composition according to claim 1, having a fatty acid content of between 0.2% and 10%, these percentages being expressed on a weight basis relative to 100 g of pharmaceutical composition. ### Claim 17 (depends on 1) A pharmaceutical composition according to claim 1, having a fatty acid content of between 0.5% and 5%, these percentages being expressed on a weight basis relative to 100 g of pharmaceutical composition. ### Claim 18 (depends on 1) A pharmaceutical composition according to claim 1, having a pH of between 5 and 9. ### Claim 19 (depends on 1) A pharmaceutical composition according to claim 1, having a pH of between 6 and 8. ### Claim 20 (depends on 1) A pharmaceutical composition according to claim 1, having a fatty acid ester content of between 0.2% and 5%, these percentages being expressed on a weight basis relative to 100 g of pharmaceutical composition. ### Claim 21 (depends on 1) A pharmaceutical composition according to claim 1, having a fatty acid ester content of between 0.5% and 2.5%, these percentages being expressed on a weight basis relative to 100 g of pharmaceutical composition. ### Claim 22 (depends on 1) A pharmaceutical composition according to claim 1, having an alcoholic vehicle content of between 20% and 80%, these percentages being expressed on a weight basis relative to 100 g of pharmaceutical composition. ### Claim 23 (depends on 1) A pharmaceutical composition according to claim 1, having an alcoholic vehicle content of between 40% and 70%, these percentages being expressed on a weight basis relative to 100 g of pharmaceutical composition. ### Claim 24 (depends on 7) A pharmaceutical composition according to claim 7, having a co-solvent content of between 1% and 10%, these percentages being expressed on a weight basis relative to 100 g of pharmaceutical composition. ### Claim 25 (depends on 1) A pharmaceutical composition according to claim 1, being in the form of a gel, and-further comprising between 0.5% and 10% of a gelling agent, these percentages being expressed on a weight basis relative to 100 g of pharmaceutical composition. ### Claim 26 (depends on 1) A pharmaceutical composition according to claim 1, being in the form of a gel, and-further comprising between 0.3% and 5% of a gelling agent, these percentages being expressed on a weight basis relative to 100 g of pharmaceutical composition. ### Claim 27 (depends on 9) A pharmaceutical composition according to claim 9, wherein the gelling agent is selected from the group consisting of carbomers, cellulose derivatives, and mixtures thereof. ### Claim 28 (depends on 9) A pharmaceutical composition according to claim 9, wherein the gelling agent is selected from the group consisting of Carbopol® 980, hydroxypropylcellulose and mixtures thereof. ### Claim 29 (depends on 11) A pharmaceutical composition according to claim 11, wherein the neutralizer is selected from the group consisting of triethanolamine, tromethamine, and mixtures thereof. ### Claim 30 (depends on 11) A pharmaceutical composition according to claim 11, wherein the neutralizer/gelling agent ratio is between 7/1 and 0.5/1. ### Claim 31 (depends on 11) A pharmaceutical composition according to claim 11, wherein the neutralizer/gelling agent ratio is between 4/1 and 1/1. ### Claim 32 A pharmaceutical composition for transdermal or transmucous administration of at least one active substance, comprising an active substance, oleic acid in an amount of between 0.1% and 20%, these percentages being expressed on a weight basis relative to 100 g of pharmaceutical composition, an alcoholic vehicle comprising ethanol, and ethyl oleate in an amount of between 0.1% and 10%, these percentages being expressed on a weight basis relative to 100 g of pharmaceutical composition, wherein said composition is in the form of a gel or solution, and wherein the amount of oleic acid does not vary by more than +/−5% after storage for 6 months at 40° C. and 75% relative humidity. ### Claim 33 A method of making a pharmaceutical composition for transdermal or transmucous administration of at least one active substance, comprising admixing: an active substance, a fatty acid percutaneous absorption promoter in an amount of between 0.1% and 20%, these percentages being expressed on a weight basis relative to 100 g of pharmaceutical composition, an alcoholic vehicle comprising an alcohol selected from the group consisting of ethanol and isopropanol, and a stabilizer capable of stabilizing the fatty acid in said pharmaceutical composition, wherein said stabilizer comprises the fatty acid ester of said fatty acid and said alcohol and is present in an amount of between 0.1% and 10%, these percentages being expressed on a weight basis relative to 100 g of pharmaceutical composition, wherein said composition is in the form of a gel or solution. ### Claim 34 (depends on 33) A pharmaceutical composition made by a method according to claim 33.