# US 11,304,912 B2 · Transdermal therapeutic system on the basis of adhesive plasticizer-polymer matrices

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- Number: US 11,304,912 B2
- Document ID: US11304912B2
- Status: Granted
- Kind: B2
- Application number: 16/765,800
- Filed: 2018-11-21
- Published: 2020-09-10
- Granted: 2022-04-19
- Earliest claimed: 2017-11-21
- Assignees: LTS Lohmann Therapie-Systeme AG
- Applicants: Lts Lohmann Therapie-Systeme AG
- Inventors: Michael Linn; Markus Müller; Marius Bauer
- Web page: https://patentgrep.com/patent/US11304912B2

## CPC

- A61K 9/7069: {obtained otherwise than by reactions only involving carbon to carbon unsaturated bonds, e.g. polysiloxane, polyesters, polyurethane, polyethylene oxide}
- A61K 9/7076: {the adhesive comprising ingredients of undetermined constitution or reaction products thereof, e.g. rosin or other plant resins}
- A61K 31/122: having the oxygen directly attached to a ring, e.g. quinones, vitamin K1, anthralin
- A61K 31/135: having aromatic rings {, e.g. ketamine, nortriptyline (methadone A61K31/137)}
- A61K 31/216: of acids having aromatic rings, e.g. benactizyne, clofibrate
- A61K 31/24: having an amino or nitro group
- A61K 31/381: having five-membered rings
- A61K 31/4468: having a nitrogen directly attached in position 4, e.g. clebopride, fentanyl
- A61K 31/4545: containing a six-membered ring with nitrogen as a ring hetero atom, e.g. pipamperone, anabasine
- A61K 31/506: not condensed and containing further heterocyclic rings
- A61K 31/663: Compounds having two or more phosphorus acid groups or esters thereof, e.g. clodronic acid, pamidronic acid
- A61K: PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES (devices or methods specially adapted for bringing pharmaceutical products into particular physical or administering forms A61J3/00; chemical aspects of, or use of materials for deodorisation of air, for disinfection or sterilisation, or for bandages, dressings, absorbent pads or surgical articles A61L; soap compositions C11D)

## Abstract

The present application relates to a transdermal therapeutic system comprising a backing layer impermeable to active substances and a polymer matrix on one side of the backing layer impermeable to active substances, wherein the polymer matrix comprises at least one pharmaceutically active substance, at least one inherently non-self-adhesive polymer and at least one plasticizer, said polymer matrix being free of adhesive polymers. The invention further relates to a method of producing the transdermal therapeutic system and to the use thereof as a drug.

## Claims

### Claim 1

A transdermal therapeutic system, comprising a backing layer impermeable to active substances and a polymer matrix layer on one side of the backing layer impermeable to active substances, wherein the polymer matrix comprises at least one pharmaceutically active substance, at least one inherently non-adhesive polymer, wherein the inherently non-adhesive polymer comprises a polyvinyl caprolactam/polyvinyl acetate/polyethylene glycol copolymer, shellac, a vinylpyrrolidone/vinyl acetate copolymer, hyroxypropyl cellulose, hydroxypropyl methyl cellulose and/or polyvinylpyrrolidone, and the amount of the at least one inherently non-adhesive polymer in the matrix layer is approximately 50 to 90 wt. %, and at least one plasticiser, wherein the at least one plasticizer comprises glycerol and/or polyethylene glycol, the amount of the at least one plasticizer in the matrix layer is approximately 5 to 50 wt. % in relation to the total weight of the matrix layer, characterised in that the polymer matrix is free of inherently adhesive polymers.

### Claim 2 (depends on 1)

The transdermal therapeutic system according to claim 1, characterised in that the transdermal therapeutic system does not comprise an additional adhesive layer on the side of the polymer matrix on which the backing layer impermeable to active substance is not situated.

### Claim 3 (depends on 1)

The transdermal therapeutic system according to claim 1, characterised in that the inherently adhesive polymer comprises a water-soluble polymer.

### Claim 4 (depends on 1)

The transdermal therapeutic system according to claim 1, characterised in that the at least one plasticiser comprises polyethylene glycol 200.

### Claim 5 (depends on 1)

The transdermal therapeutic system according to claim 1, characterised in that the at least one pharmaceutically active substance is selected from the group consisting of idebenone, oxybutynin, riociguat, rotigotine, apixaban, ketamine, alendronate and/or fentanyl.

### Claim 6 (depends on 1)

The transdermal therapeutic system according to claim 1, characterised in that the amount of the at least one pharmaceutically active substance is from approximately 1 to 20 wt. % in relation to the total weight of the matrix layer.

### Claim 7 (depends on 1)

The transdermal therapeutic system according to claim 1, characterised in that the transdermal therapeutic system comprises at least one auxiliary selected from the group comprising dyes, emulsifiers, penetration enhancers, pH regulators, humectants, preservatives and/or antioxidants.

### Claim 8 (depends on 1)

A medicinal product comprised of the transdermal therapeutic system according to claim 1.

### Claim 9 (depends on 7)

The transdermal therapeutic system according to claim 7, characterised in that the at least one auxiliary is present in an amount of from 0.01 to 20 wt. % in relation to the total weight of the matrix layer.

### Claim 10 (depends on 1)

The transdermal therapeutic system of claim 1, wherein the polymer matrix is applied directly to the backing layer comprised of polyethylene terephthalate.

### Claim 11 (depends on 1)

The transdermal therapeutic system of claim 1, consisting of the backing layer, the polymer matrix and a removable barrier.

### Claim 12 (depends on 1)

The transdermal therapeutic system of claim 1 being adapted for application to a skin of a patient.

### Claim 13 (depends on 1)

The transdermal therapeutic system of claim 1 including no (meth)acrylate, poly(meth) acrylate, polyisobutyhene or silicone inclusive polymers.

### Claim 14 (depends on 1)

The transdermal therapeutic system according to claim 1, wherein the amount of the at least one inherently non-adhesive polymer in the matrix layer is approximately 60 to 80 wt. % in relation to the total weight of the matrix layer, the at least one plasticiser in the matrix layer is approximately 10 to 30 wt. % in relation to the total weight of the matrix layer, and the weight ratio in parts by weight of the at least one polymer to the at least one plasticiser is approximately 80 to 60 to approximately 20 to 40.

### Claim 15 (depends on 1)

The transdermal therapeutic system according to claim 1 including a penetration enhancer selected from pentanoic acid, hexanoic acid, octanoic acid, nonanoic acid, decanoic acid, lauric acid, myristic acid, palmitic acid, stearic acid, arachidic acid, behenic acid, lignoceric acid, isovaleric 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, ethyl acetate, methyl propylate, butyl acetate, methyl valerate, diethyl sebacate, methyl laurate, ethyl oleate, isopropyl decanoate, isopropyl myristate (myristic acid isopropyl ester), isopropyl palmitate, and isopropyl oleinate (oleic acid isopropyl ester) and/or esters thereof.

### Claim 16 (depends on 15)

The transdermal therapeutic system of claim 15, wherein the penetration enhancer comprises oleic acid and/or acid esters thereof.
