# US 12,214,088 B2 · Transdermal therapeutic system for the transdermal administration of guanfacine comprising at least one additive > Agents: this data is available as JSON from the patentgrep API and MCP server — see https://patentgrep.com/llms.txt - Number: US 12,214,088 B2 - Document ID: US12214088B2 - Status: Granted - Kind: B2 - Application number: 16/755,049 - Filed: 2018-10-11 - Published: 2020-12-24 - Granted: 2025-02-04 - Earliest claimed: 2017-10-11 - Assignees: LTS Lohmann Therapie-Systeme AG; DDP Specialty Electronic Materials US 9, LLC - Applicants: Lts Lohmann Therapie-Systeme AG; DDP Specialty Electronic Materials US 9, LLC - Inventors: Marco Emgenbroich; Eva-Marie Prinz; Elke Klein; Heike Kluth; Xavier Thomas; Linda Sue Nartker - Web page: https://patentgrep.com/patent/US12214088B2 ## 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 9/7069: {obtained otherwise than by reactions only involving carbon to carbon unsaturated bonds, e.g. polysiloxane, polyesters, polyurethane, polyethylene oxide} - A61K 31/165: having aromatic rings, e.g. colchicine, atenolol, progabide - A61K 47/08: containing oxygen, {e.g. ethers, acetals, ketones, quinones, aldehydes, peroxides} - A61K 47/10: Alcohols; Phenols; Salts thereof, e.g. glycerol; Polyethylene glycols [PEG]; Poloxamers; PEG/POE alkyl ethers - A61K 47/32: Macromolecular compounds obtained by reactions only involving carbon-to-carbon unsaturated bonds, e.g. carbomers {, poly(meth)acrylates, or polyvinyl pyrrolidone} - A61P 9/12: Antihypertensives - A61P 25/00: Drugs for disorders of the nervous system - 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 transdermal therapeutic system for the transdermal administration of guanfacine comprising a guanfacine-containing layer structure, said guanfacine-containing layer structure comprising: A) a backing layer; and B) a guanfacine-containing layer; wherein the transdermal therapeutic system comprises at least one polymer and at least additive. ## Claims ### Claim 1 A transdermal therapeutic system for the transdermal administration of guanfacine comprising a guanfacine-containing layer structure, said guanfacine-containing layer structure comprising: A) a backing layer; and B) a guanfacine-containing layer; wherein the transdermal therapeutic system comprises at least one polymer and a combination of a dispersing agent, a permeation enhancer, and a solubilizer; wherein the dispersing agent is a polyethylene glycol C8-C20-alkyl ether having from 2 to 10 EO units, the permeation enhancer is oleyl alcohol, and the solubilizer is a polyvinyl caprolactam-polyvinyl acetate-polyethylene glycol graft copolymer. ### Claim 2 (depends on 1) The transdermal therapeutic system according to claim 1, wherein the guanfacine-containing layer is a guanfacine-containing matrix layer comprising: i) guanfacine; ii) the at least one polymer; and iii) the combination of the dispersing agent, the penetration enhancer, and the solubilizer. ### Claim 3 (depends on 1) The transdermal therapeutic system according to claim 1, wherein the guanfacine-containing layer structure is self-adhesive. ### Claim 4 (depends on 1) The transdermal therapeutic system according to claim 1, wherein the guanfacine in the guanfacine-containing layer structure is guanfacine free base dispersed in the guanfacine-containing layer, and wherein the guanfacine-containing layer structure further comprises from 1 to 100 mg/TTS guanfacine. ### Claim 5 (depends on 1) The transdermal therapeutic system according to claim 1, wherein the guanfacine-containing layer comprises from 1 to 20% guanfacine by weight, based on the total weight of the guanfacine-containing layer. ### Claim 6 (depends on 1) The transdermal therapeutic system according to claim 1, wherein the guanfacine-containing layer comprises from 20 to 97% of the at least one polymer by weight, based on the total weight of the guanfacine-containing layer, and wherein the at least one polymer is selected from the group consisting of silicones, acrylates, silicone acrylic hybrid polymers, polyisobutylenes, and styrene-isoprene-styrene block copolymers. ### Claim 7 (depends on 1) The transdermal therapeutic system according to claim 1, wherein the dispersing agent is present in an amount of from 1 to 10% by weight, based on the total weight of the guanfacine-containing layer, the permeation enhancer is present in an amount of from 1 to 10% by weight, based on the total weight of the guanfacine-containing layer, and the solubilizer is present in an amount of from 0.5 to 10% by weight, based on the total weight of the guanfacine-containing layer. ### Claim 8 (depends on 1) The transdermal therapeutic system according to claim 1, wherein the guanfacine-containing layer has (i) an area weight ranging from 40 to 250 g/m2, (ii) an area of release ranging from 1 to 100 cm2, or both (i) and (ii). ### Claim 9 (depends on 1) The transdermal therapeutic system according to claim 1, wherein the transdermal therapeutic system provides by transdermal delivery at steady state a plasma concentration of guanfacine of from 1 to 20 ng/ml. ### Claim 10 (depends on 1) The transdermal therapeutic system according to claim 1, wherein the transdermal therapeutic system provides at least one pharmacokinetic parameter selected from the group consisting of: an AUC0-24h of about 10 to 600 ng*h/ml; an AUC0-72h of about 30 to 1800 ng*h/ml; an AUC0-84h of about 35 to 2100 ng*h/ml; a Cmax to C84 ratio of less than 3.5; a Cmax to C72 ratio of less than 3.0; and a Cmax to C24 ratio of less than 2.0.