# US 10,945,968 B2 · Memantine transdermal delivery systems > Agents: this data is available as JSON from the patentgrep API and MCP server — see https://patentgrep.com/llms.txt - Number: US 10,945,968 B2 - Document ID: US10945968B2 - Status: Granted - Kind: B2 - Application number: 15/660,929 - Filed: 2017-07-26 - Published: 2018-02-01 - Granted: 2021-03-16 - Earliest claimed: 2016-07-27 - Assignees: Corium, Inc. - Applicants: Corium, Inc. - Inventors: Eun Soo Lee; Parminder Singh; Appala Sagi; Amit K. Jain - Web page: https://patentgrep.com/patent/US10945968B2 ## CPC - A61K 9/7084: {Transdermal patches having a drug layer or reservoir, and one or more separate drug-free skin-adhesive layers, e.g. between drug reservoir and skin, or surrounding the drug reservoir; Liquid-filled reservoir patches} - A61K 9/7038: {Transdermal patches of the drug-in-adhesive type, i.e. comprising drug in the skin-adhesive layer} - A61K 9/7061: {Polyacrylates} - A61K 9/7092: {Transdermal patches having multiple drug layers or reservoirs, e.g. for obtaining a specific release pattern, or for combining different drugs} - A61K 31/045: Hydroxy compounds, e.g. alcohols; Salts thereof, e.g. alcoholates - A61K 31/13: Amines {(A61K31/04 takes precedence)} - A61P 9/10: for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis - A61P 25/00: Drugs for disorders of the nervous system - A61P 25/28: for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia - 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 47/16: containing nitrogen, {e.g. nitro-, nitroso-, azo-compounds, nitriles, cyanates} - 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 Transdermal delivery systems for the systemic delivery of memantine are described, wherein the system comprises a drug reservoir layer and an adhesive layer, optionally together with one or more intermediate and/or supporting layers, wherein the drug reservoir layer comprises an acrylate polymer or copolymer, a permeation enhancer, a carrier, and memantine base generated in situ by reaction of a memantine salt and an alkaline salt. Compositions and kits comprising the various components, e.g., drug reservoir and/or adhesive compositions are described. Methods relating to treatment of CNS disorders, e.g., Alzheimer's disease and/or dementia, using the aforementioned transdermal delivery devices and/or compositions are also described. ## Claims ### Claim 1 A composition, comprising: a drug reservoir consisting essentially of a salt of memantine and an alkaline salt; a permeation enhancer; a hydrophilic solvent carrier; a crosslinked polyvinylpyrrolidone; and an acrylate copolymer, wherein, after application of the composition to the skin of a subject, memantine base is generated in situ by reaction of the salt of memantine and the alkaline salt. ### Claim 2 (depends on 1) The composition of claim 1, wherein the hydrophilic solvent carrier is glycerol. ### Claim 3 (depends on 1) The composition of claim 1, wherein the permeation enhancer is a higher alcohol selected from the group consisting of lauryl alcohol, isostearyl alcohol, octyldodecanol, and oleyl alcohol. ### Claim 4 (depends on 1) The composition of claim 1, wherein the salt of memantine is memantine hydrochloride and the alkaline salt is selected from the group consisting of sodium acetate, sodium borate, sodium metaborate, sodium carbonate, sodium bicarbonate, potassium carbonate, potassium bicarbonate, potassium citrate, potassium acetate, sodium phosphate, potassium phosphate, disodium hydrogen phosphate, sodium oxylate, sodium succinate, sodium citrate, and sodium salicylate. ### Claim 5 (depends on 1) The composition of claim 1, further comprising a skin contact adhesive comprised of polyisobutylene (PIB), polybutylene, or a mixture thereof. ### Claim 6 (depends on 5) The composition of claim 5, wherein the skin contact adhesive comprises (i) about 5-15 wt % octyldodecanol; (ii) a mixture of polyisobutylene and polybutylene; and optionally (iii) about 10-30 wt % cross-linked PVP. ### Claim 7 (depends on 5) The composition of claim 5, wherein the skin contact adhesive comprises, (i) about 8-12 wt % octyldodecanol; (ii) about 65-90 wt % of a mixture of polyisobutylene and polybutylene; and optionally (iii) about 15-25 wt % cross-linked PVP. ### Claim 8 (depends on 1) The composition of claim 1, wherein memantine base is generated in situ in the drug reservoir over a 3-5 day period. ### Claim 9 (depends on 1) The composition of claim 1, wherein the salt of memantine is memantine hydrochloride and the alkaline salt is sodium bicarbonate. ### Claim 10 (depends on 9) The composition of claim 9, wherein the drug reservoir comprises a molar amount of memantine hydrochloride and an equimolar or less than less than equimolar amount of sodium bicarbonate. ### Claim 11 (depends on 10) The composition of claim 10, wherein the drug reservoir comprises between about 10-30 wt % memantine hydrochloride. ### Claim 12 (depends on 10) The composition of claim 10, wherein the drug reservoir comprises between about 22-27 wt % memantine hydrochloride. ### Claim 13 (depends on 10) The composition of claim 10, wherein the drug reservoir comprises between about 5-15 wt % sodium bicarbonate. ### Claim 14 A composition, comprising: a drug reservoir consisting essentially of (a) between about 10-30 wt % memantine HCl and between about 5-15 wt % sodium bicarbonate; (b) about 5-15 wt % octyldodecanol; (c) about 5-15 wt % glycerol; (d) about 10-30 wt % crosslinked polyvinylpyrrolidone; and (e) about 20-50 wt % acrylate polymer, wherein, after application of the composition to the skin of a subject, memantine base is generated in situ by reaction of the memantine HCl and the sodium bicarbonate. ### Claim 15 (depends on 1) A method for delivering memantine to a subject in need thereof, comprising: administering the composition of claim 1 to the skin of a human subject, whereby said administering achieves transdermal delivery of memantine base to the subject. ### Claim 16 (depends on 15) The method of claim 15, wherein the subject is suffering from or has been diagnosed with a CNS disorder. ### Claim 17 (depends on 16) The method of claim 16, wherein the CNS disorder is Alzheimer's disease.