# US 8,784,869 B2 · Controlled release delivery system for nasal applications and methods of treatment > Agents: this data is available as JSON from the patentgrep API and MCP server — see https://patentgrep.com/llms.txt - Number: US 8,784,869 B2 - Document ID: US8784869B2 - Status: Granted - Kind: B2 - Application number: 13/547,774 - Filed: 2012-07-12 - Published: 2012-11-01 - Granted: 2014-07-22 - Earliest claimed: 2003-11-11 - Assignees: Mattern Pharma AG - Applicants: Claudia Mattern - Inventors: Claudia Mattern - Web page: https://patentgrep.com/patent/US8784869B2 ## CPC - A61K 31/57: substituted in position 17 beta by a chain of two carbon atoms, e.g. pregnane or progesterone - A61K 9/0043: {Nose} - A61K 9/06: Ointments; Bases therefor; {Other semi-solid forms, e.g. creams, sticks, gels (composition of ointments, creams or gels A61K47/00)} - A61K 31/568: substituted in positions 10 and 13 by a chain having at least one carbon atom, e.g. androstanes, e.g. testosterone - A61K 47/02: Inorganic compounds - A61K 47/14: Esters of carboxylic acids, e.g. fatty acid monoglycerides, medium-chain triglycerides, parabens or PEG fatty acid esters - 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 15/00: Drugs for genital or sexual disorders (for disorders of sex hormones A61P5/24); Contraceptives - 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 This invention relates to a gel formulation for nasal administration of a controlled release formulation of hormones to the systemic circulation and/or to the brain. The special lipophilic or partly lipophilic system of the invention leads to higher bioavailability of the active ingredient caused by sustained serum levels in plasma but also leads to a more favorable serum level profile. The special lipophilic or partly lipophilic system also allows for the modulation of brain functioning. The invention also relates to the nasal administration of steroid hormones for treatment of female sexual dysfunction (FSD) or female arousal disorder. ## Claims ### Claim 1 A formulation for nasal application comprising: a) testosterone, wherein said testosterone is present within the formulation in an amount of from about 0.2% to about 6% by weight of the formulation; b) at least one lipophilic or partly lipophilic carrier present in an amount of from about 60% to about 98% by weight of the formulation; c) at least one compound having surface tension decreasing activity present in an amount of from about 1% to about 20% by weight of the formulation; and d) at least one viscosity regulating agent present in an amount of from about 0.5% to about 10% by weight of the formulation. ### Claim 2 (depends on 1) The formulation according to claim 1, wherein the lipophilic carrier comprises castor oil. ### Claim 3 (depends on 1) The formulation according to claim 1, wherein the at least one compound having surface tension decreasing activity comprises at least one surfactant selected from the group consisting of lecithin, fatty acid ester of polyvalent alcohols, of sorbitanes, of polyoxyethylensorbitans, of polyoxyethylene, of sucrose, of polyglycerol and/or at least one humectant selected from the group consisting of sorbitol, glycerine, polyethylene glycol, and macrogol glycerol fatty acid ester, or a mixture thereof. ### Claim 4 (depends on 3) The formulation according to claim 3, wherein the at least one compound having surface tension decreasing activity comprises an oleoyl macrogolglyceride or a mixture of oleoyl macrogolglycerides. ### Claim 5 (depends on 1) The formulation according to claim 1, wherein said viscosity regulating agent comprises a thickener or gelling agent selected from the group consisting of cellulose and cellulose derivatives, polysaccharides, carbomers, polyvinyl alcohol, povidone, colloidal silicon dioxide, cetyl alcohols, stearic acid, beeswax, petrolatum, triglycerides and lanolin, or a mixture thereof. ### Claim 6 (depends on 5) The formulation according to claim 5, wherein said viscosity increasing agent is colloidal silicon dioxide. ### Claim 7 (depends on 1) A method for the treatment of Female Sexual Dysfunction (FSD) comprising nasally administering to a patient in need of such treatment an effective amount of a formulation according to claim 1. ### Claim 8 (depends on 1) A method for the treatment of female arousal disorder comprising nasally administering to a patient in need of such treatment an effective amount of a formulation according to claim 1. ### Claim 9 (depends on 1) A method of increasing an amygdala response in women comprising the step of nasally administering to a woman an effective amount of a formulation according to claim 1.