Granted Patent B2

US 12,214,088 · App. 16/755,049 · Granted Feb 4, 2025

Inventors: Marco Emgenbroich (Rheinbach, DE); Eva-Marie Prinz (Weissenthurm, DE); Elke Klein (Bad Neuenahr-Ahrweiler, DE); Heike Kluth (Ochtendung, DE); Xavier Thomas (Famars, FR); Linda Sue Nartker (Midland, MI)

Assignees: LTS LOHMANN THERAPIE-SYSTEME AG; DDP SPECIALTY ELECTRONIC MATERIALS US 9, LLC

A61K9/7084A61K9/7069A61K31/165A61K47/08A61K47/10A61K47/32

Abstract

Claims (24)

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 C 8 -C 20 -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.

2. 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.

3. The transdermal therapeutic system according to claim 1 , wherein the guanfacine-containing layer structure is self-adhesive.

4. 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.

5. 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.

6. 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.

7. 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.

8. The transdermal therapeutic system according to claim 1 , wherein the guanfacine-containing layer has (i) an area weight ranging from 40 to 250 g/m 2 , (ii) an area of release ranging from 1 to 100 cm 2 , or both (i) and (ii).

9. 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.

10. 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 AUC 0-24h of about 10 to 600 ng*h/ml;

an AUC 0-72h of about 30 to 1800 ng*h/ml;

an AUC 0-84h of about 35 to 2100 ng*h/ml;

a C max to C 84 ratio of less than 3.5;

a C max to C 72 ratio of less than 3.0; and

a C max to C 24 ratio of less than 2.0.

Assignments (6)

Priority Claims (1)

Continuity (2)

References Cited (61)