Transdermal therapeutic system for the transdermal administration of guanfacine comprising a silicone polymer
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-12168074-B2
Publication Date
2024-12-17
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 silicone polymer.
Core Innovation
The invention relates to a transdermal therapeutic system for the transdermal administration of guanfacine. The system comprises a guanfacine-containing layer structure including a backing layer and a guanfacine-containing layer, wherein the guanfacine-containing layer comprises a first silicone polymer and a second silicone polymer within specified weight-percentage ranges based on the total weight of the guanfacine-containing layer.
The guanfacine-containing layer structure enables controlled delivery, including extended delivery durations of not less than 24 h, preferably about 72-84 h, and constant or continuous guanfacine delivery. The system is positioned to provide reduced plasma fluctuation compared with oral dosing while maintaining guanfacine delivery over an extended time period.
The described formulations further relate the guanfacine-containing layer structure to selectable compositional options and layer designs, including guanfacine in free base form and optional additives such as soluble polyvinylpyrrolidone (povidone), dispersing agents, permeation enhancers, and solubilizers. The document also describes testing and evaluation based on skin permeation testing and includes pharmacokinetic and release targets using metrics such as AUC and Cmax.
Claims Coverage
The independent claim coverage centers on a transdermal therapeutic system having a layered structure and a specific silicone-polymer composition in the guanfacine-containing layer, supported by dependent claims that refine guanfacine form and loading, layer physical parameters, selectable permeation enhancers, and therapeutic use for hypertension and ADHD. The inventive features focus on the guanfacine-containing layer structure and the relative amounts of first and second silicone polymers.
Transdermal therapeutic system with backing layer and guanfacine-containing layer
A transdermal therapeutic system for the transdermal administration of guanfacine comprising a guanfacine-containing layer structure, said guanfacine-containing layer structure comprising a backing layer and a guanfacine-containing layer.
First and second silicone polymers in specified weight ranges
The guanfacine-containing layer comprises a first silicone polymer in an amount of from 50 to 70% by weight based on the total weight of the guanfacine-containing layer, and a second silicone polymer in an amount of from 15 to 45% by weight based on the total weight of the guanfacine-containing layer.
Guanfacine-containing matrix layer with silicone polymers
The guanfacine-containing layer is a guanfacine-containing matrix layer comprising guanfacine and the first and second silicone polymers.
Guanfacine as free base and guanfacine loading per TTS
The guanfacine-containing layer structure has guanfacine in the form of the free base dispersed in the guanfacine-containing layer, with guanfacine in an amount of from 1 to 75 mg/TTS.
Area weight and/or area of release constraints
The guanfacine-containing layer has an area weight ranging from 40 to 250 g/m2 and/or an area of release ranging from 1 to 100 cm2.
Selectable permeation enhancer option set
The permeation enhancer is selected from a defined list including diethylene glycol monoethyl ether (transcutol), oleic acid, levulinic acid, caprylic/capric triglycerides, diisopropyl adipate, isopropyl myristate, isopropyl palmitate, lauryl lactate, triacetin, dimethylpropylene urea, and oleyl alcohol.
Method for treating hypertension or ADHD by skin administration
A method for treating hypertension or attention deficit hyperactivity disorder (ADHD) in a human patient comprises administering the transdermal therapeutic system to the skin of the human patient in need thereof.
Overall, the claim set is anchored by a layered transdermal therapeutic system with a backing layer and a guanfacine-containing layer that contains first and second silicone polymers in specified weight ranges. Dependent claim refinements specify a guanfacine-containing matrix embodiment, guanfacine as free base with defined loading per TTS, constraints on area weight and/or area of release, a defined selectable set of permeation enhancers, and therapeutic use via skin administration for hypertension or ADHD.
Stated Advantages
Extended delivery durations of not less than 24 h, preferably about 72-84 h.
Constant or continuous guanfacine delivery.
Reduced plasma fluctuation versus oral dosing.
Documented Applications
Medical use of the transdermal therapeutic system in human patients aged 6 to 17 years for hypertension.
Medical use of the transdermal therapeutic system in human patients aged 6 to 17 years for ADHD.
Medical use as adjunctive therapy to stimulant medications for ADHD.
Performance evaluation using Franz diffusion cells with dermatomed human skin, including reported skin permeation rates.
Pharmacokinetic documentation including steady-state mean plasma concentration and PK parameters.
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