Transdermal therapeutic system for the transdermal administration of guanfacine comprising at least one additive
Inventors
Emgenbroich, Marco • PRINZ, Eva-Marie • Klein, Elke • Kluth, Heike • Thomas, Xavier • Nartker, Linda Sue
Assignees
LTS Lohmann Therapie Systeme AG • Dow Silicones Corp • DDP Specialty Electronic Materials US 9 LLC
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Publication Number
US-12214088-B2
Publication Date
2025-02-04
Expiration Date
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.
Core Innovation
The invention relates to a transdermal therapeutic system for the transdermal administration of guanfacine that includes a guanfacine-containing layer structure with a backing layer and a guanfacine-containing layer. The guanfacine-containing layer structure comprises at least one polymer and a combination of a dispersing agent, a permeation enhancer, and a solubilizer. 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.
The guanfacine-containing layer structure is described with guanfacine in free base form and defined drug-loading relationships to the TTS and the guanfacine-containing layer. The system is also described as self-adhesive and as including selected polymer classes in the guanfacine-containing layer. These features are presented as supporting a homogeneous composition and effective transdermal delivery.
The disclosure also describes performance targets in terms of pharmacokinetic/exposure parameters, including AUC and Cmax ratio thresholds across defined time windows. Example content in the provided portion includes in vitro permeation testing using Franz diffusion cell conditions with dermatomed human skin and reporting cumulative permeated amounts over time to support the extended delivery objective.
Claims Coverage
The independent claim defines a guanfacine transdermal therapeutic system with a layered structure and a specific dispersing agent, permeation enhancer, and solubilizer combination, with dependent claims refining composition, guanfacine form, layer configuration, and pharmacokinetic/exposure performance targets. The main inventive features are grounded in these specified material selections and exposure-related requirements.
Layered guanfacine TTS structure with polymer and functional additive combination
A transdermal therapeutic system for the transdermal administration of guanfacine comprising a guanfacine-containing layer structure including a backing layer and 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.
Specific dispersing agent, permeation enhancer, and solubilizer selections
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.
Self-adhesive guanfacine-containing layer structure
The transdermal therapeutic system includes a self-adhesive guanfacine-containing layer structure.
Guanfacine free base in the guanfacine-containing layer with defined loading per TTS
Guanfacine in the guanfacine-containing layer is guanfacine free base dispersed in that layer and the layer structure further comprises 1 to 100 mg/TTS guanfacine.
Polymer content range and selected polymer classes in the guanfacine-containing layer
The guanfacine-containing layer contains 20% to 97% by weight of at least one specified polymer, where the polymer is selected from silicones, acrylates, silicone acrylic hybrid polymers, polyisobutylenes, or styrene-isoprene-styrene block copolymers.
Pharmacokinetic/exposure targeting using AUC and Cmax ratio thresholds
The transdermal therapeutic system is configured to provide at least one specified pharmacokinetic parameter within the stated AUC and Cmax ratio ranges.
Across the independent claim and its dependent refinements, the coverage centers on a guanfacine TTS with a backing layer and guanfacine-containing layer, where at least one polymer is combined with a specifically defined dispersing agent, oleyl alcohol as permeation enhancer, and a polyvinyl caprolactam-polyvinyl acetate-polyethylene glycol graft copolymer solubilizer, with further constraints on self-adhesive structure, guanfacine free base loading, polymer selection/content, and pharmacokinetic/exposure targets using AUC and Cmax ratio thresholds.
Stated Advantages
Extended wear (at least 24 h, preferably about 84 h).
Steady-state plasma concentration suitable for the described TTS performance.
Flatter plasma curve supported by Cmax to C ratio limits.
Improved skin permeation performance supported by described skin permeation rate and cumulative permeation over 72 h.
Homogeneous dispersion.
Improved skin permeation.
Reduced plasma concentration fluctuation.
Therapeutically effective extended delivery.
Targeted pharmacokinetic/exposure performance using AUC and Cmax ratio thresholds.
Documented Applications
Transdermal administration of guanfacine using the disclosed transdermal therapeutic system (TTS).
Transdermal administration of guanfacine for hypertension.
Transdermal administration of guanfacine for ADHD.
Methods of treatment for ages 6-17.
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