Esketamine-suspension-tts

Patent metadata

Field	Value
Publication number	US-2023285323-A1
Application number	US-202118019505-A
Country	US
Kind code	A1
Filing date	Jul 22, 2021
Priority date	Aug 6, 2020
Publication date	Sep 14, 2023
Grant date	—

Abstract

The present invention concerns a transdermal therapeutic system, comprising a backing layer, which is not permeable N for the active ingredient, and at least one matrix layer on one side of the backing layer, wherein the matrix layer contains at least one pressure sensitive adhesive and ketamine or a pharmaceutically acceptable salt or solvate thereof, wherein the at least one pressure sensitive adhesive comprises a silicone pressure sensitive adhesive, as well as its use as medicament, in particular for the treatment of depression and pain.

First claim

1 . A transdermal therapeutic system comprising:
a backing layer, which is not permeable for the active ingredient; and at least one matrix layer on one side of the backing layer; wherein the matrix layer contains at least one pressure sensitive adhesive and ketamine or a pharmaceutically acceptable salt or solvate thereof; and wherein the at least one pressure sensitive adhesive comprises a silicone pressure sensitive adhesive.

2 . The transdermal therapeutic system of claim 1 , wherein the ketamine is (S)-ketamine or a pharmaceutically acceptable salt or solvate thereof.

3 . The transdermal therapeutic system of claim 1 , wherein the ketamine is present in the form of the ketamine free base.

4 . The transdermal therapeutic system of claim 1 , wherein the silicone pressure sensitive adhesive comprises a dimethiconol/trimethylsiloxysilicate crosspolymer and/or a trimethylsilyl treated dimethiconol/trimethylsiloxysilicate crosspolymer.

5 . The transdermal therapeutic system of claim 1 , wherein the silicone pressure sensitive adhesive is present in the matrix layer in an amount of 70 to 95 wt.-%, based on the total weight of the matrix layer.

6 . The transdermal therapeutic system of claim 1 , wherein the matrix layer comprises at least one penetration enhancer.

7 . The transdermal therapeutic system of claim 6 , wherein the at least one penetration enhancer is selected from the group consisting of levulinic acid, valeric acid, hexanoic acid, caprylic acid, nonanoic acid, decanoic acid, lauric acid, myristic acid, palmitic acid, stearic acid, arachidic acid, behenic acid, lignoceric acid, 3-methylbutanoic acid, neoheptanoic acid, neonanonic acid, isostearic acid, oleic acid, palmitoleic acid, linolenic acid, vaccenic acid, petroselinic acid, elaidic acid, oleic acid, arachidonic acid, gadoleic acid, erucic acid, methyl propionate, methyl valerate, diethyl sebacate, methyl laurate, ethyl laurate, ethyl oleate, isopropyl decanoate, isopropyl myristate, isopropyl palmitate, isopropyl oleate, diethyltoluamide, propylene glycol monocaprylate, propylene glycol, polyethylene glycol, diisopropyl adipate, eugenol, transcutol, lauryl lactate, and/or oleyl alcohol.

8 . The transdermal therapeutic system of claim 6 , wherein the matrix layer comprises the at least one penetration enhancer in an amount of 1 to 15 wt.-%, based on the total weight of the matrix layer.

9 . The transdermal therapeutic system of claim 1 , wherein the matrix layer does not comprise any pressure sensitive adhesive that comprises (meth)acrylate groups.

10 . The transdermal therapeutic system of claim 1 , wherein the matrix layer comprises ketamine in an amount of 1 to 25 wt.-%, based on the weight of the matrix layer.

11 . The transdermal therapeutic system of claim 1 , wherein the matrix layer comprises at least one antioxidant.

12 . The transdermal therapeutic system of claim 1 , wherein the matrix layer has an area weight of 30 to 400 g/m 2 .

13 . The transdermal therapeutic system of claim 1 , wherein the transdermal therapeutic system comprises a detachable protective layer on that side of the matrix layer on which the backing layer is not arranged.

14 . The transdermal therapeutic system of claim 1 for use as a medicament.

15 . The transdermal therapeutic system of claim 1 for use in the treatment of depression and/or pain.

16 . The transdermal therapeutic system of claim 3 , wherein the ketamine is (S)-ketamine.

17 . The transdermal therapeutic system of claim 6 , wherein the at least one penetration enhancer comprises methyl laurate.

18 . The transdermal therapeutic system of claim 11 , wherein the at least one antioxidant comprises alpha-tocopherol, ascorbyl palmitate and/or dibutylhydroxytoluene.

Assignees

• Lts Lohmann Therapie Systeme Ag

Inventors

• Hammes Florian
• Tomeleri Anja
• Kleudgen Tobias

Classifications

• A61K9/7069 Primary

  obtained otherwise than by reactions only involving carbon to carbon unsaturated bonds, e.g. polysiloxane, polyesters, polyurethane, polyethylene oxide · CPC title

• A61K31/135 Primary

  having aromatic rings {, e.g. ketamine, nortriptyline (methadone A61K31/137)} · CPC title

• A61K47/14

  Esters of carboxylic acids, e.g. fatty acid monoglycerides, medium-chain triglycerides, parabens or PEG fatty acid esters · CPC title

• A61K47/22

  Heterocyclic compounds, e.g. ascorbic acid, tocopherol or pyrrolidones · CPC title

• A61K47/10

  Alcohols; Phenols; Salts thereof, e.g. glycerol; Polyethylene glycols [PEG]; Poloxamers; PEG/POE alkyl ethers · CPC title