Transdermal therapeutic system for the transdermal administration of guanfacine comprising a silicone polymer

1. A transdermal therapeutic system (TTS) 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; and

wherein the guanfacine-containing layer comprises from 20 to 99% of the at least one silicone polymer; and

wherein the guanfacine-containing layer further comprises at least two additives selected from the group consisting of dispersing agents, permeation enhancers, and solubilizers, and

wherein the guanfacine-containing layer comprises from 0.5 to 10% of the at least two additives, by weight, based on the total weight of the guanfacine-containing layer.

2. The transdermal therapeutic system according to claim 1 ,

wherein the guanfacine-containing layer is a guanfacine-containing matrix layer comprising:

i) guanfacine; and

ii) the at least one silicone polymer.

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-containing layer structure comprises the guanfacine in the form of the free base dispersed in the guanfacine-containing layer, and

wherein the guanfacine-containing layer structure comprises from 1 to 75 mg/TTS guanfacine.

5. The transdermal therapeutic system according to claim 1 ,

wherein the guanfacine-containing layer comprises from 1 to 20% of guanfacine by weight, based on the total weight of the guanfacine-containing layer.

6. The transdermal therapeutic system according to claim 1 ,

wherein the at least one silicone polymer is obtainable by polycondensation of silanol endblocked polydimethylsiloxane with a silicate resin.

7. The transdermal therapeutic system according to claim 1 ,

wherein the guanfacine-containing layer comprises from 35 to 70% of a first polymer by weight, based on the total weight of the guanfacine-containing layer, wherein the first polymer is a first silicone polymer, and wherein the guanfacine-containing layer further comprises from 15 to 45% of a second polymer by weight, based on the total weight of the guanfacine-containing layer, wherein the second polymer is selected from the group consisting of silicone polymers, acrylate polymers, and silicone acrylic hybrid polymers.

8. The transdermal therapeutic system according to claim 1 ,

wherein at least one of the at least one additive two additives is a dispersing agent, and wherein the dispersing agent is selected from the group consisting of esters of fatty acids with polyols, fatty alcohols, polyethylene glycols having a number average molecular weight of from 300 to 400, and polyethylene glycol alkyl ethers.

9. The transdermal therapeutic system according to claim 1 ,

wherein at least one of the at least two additives is a permeation enhancer, and wherein the permeation enhancer is selected from the group consisting of 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.

10. The transdermal therapeutic system according to claim 1 ,

wherein at least one of the at least two additives is a solubilizer, and wherein the solubilizer is selected from the group consisting of copolymers derived from esters of acrylic and methacrylic acid, polyvinylpyrrolidone, vinylpyrrolidone-vinyl acetate copolymers, and polyvinyl caprolactam-polyvinyl acetate-polyethylene glycol graft copolymers.

11. 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).

12. A method of treating hypertension or attention deficit hyperactivity disorder (ADHD) in a human patient, the method comprising administering the transdermal therapeutic system according to claim 1 to the skin of the human patient in need thereof.

13. The method according to claim 12 , wherein the transdermal therapeutic system is applied to the skin of the human patient for at least 24 hours.

14. The method according to claim 13 , wherein the transdermal therapeutic system is applied to the skin of the human patient for at least 72 hours.

15. The method according to claim 13 , wherein the transdermal therapeutic system is applied to the skin of the human patient for about 84 hours.

16. The method according to claim 12 , wherein the human patient is at the age of from 6 to 17.

17. The method according to claim 12 , wherein the transdermal therapeutic system is provided as an adjunctive therapy to stimulant medications in the human patient.