# US 2025/0082584 A1 · Transdermal therapeutic system for the transdermal administration of selexipag

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- Number: US 2025/0082584 A1
- Document ID: US20250082584A1
- Status: Published application
- Kind: A1
- Application number: 18/728,006
- Filed: 2023-01-26
- Published: 2025-03-13
- Earliest claimed: 2022-01-27
- Assignees: LTS Lohmann Therapie-Systeme AG
- Applicants: Lts Lohmann Therapie-Systeme AG
- Inventors: Florian HAMMES; Anja TOMELERI; Tobias KLEUDGEN
- Web page: https://patentgrep.com/patent/US20250082584A1

## CPC

- A61K 9/7053: {obtained by reactions only involving carbon to carbon unsaturated bonds, e.g. polyvinyl, polyisobutylene, polystyrene}
- A61K 9/7069: {obtained otherwise than by reactions only involving carbon to carbon unsaturated bonds, e.g. polysiloxane, polyesters, polyurethane, polyethylene oxide}
- A61K 31/4965: Non-condensed pyrazines
- 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 invention relates to transdermal therapeutic systems (TTS) for the transdermal administration of selexipag.

## Claims

### Claim 1

Transdermal therapeutic system for the transdermal administration of selexipag comprising a self-adhesive selexipag-containing layer structure, said self-adhesive selexipag-containing layer structure comprising:
A) a backing layer;
B) a selexipag-containing layer comprising:
1. selexipag;
2. at least one polar polymer; and
3. at least one nonpolar polymer.

### Claim 2 (depends on 1)

Transdermal therapeutic system according to claim 1, wherein a content of selexipag in the selexipag-containing layer ranges from 0.1 to 8.0%, preferably from 0.5 to 5.5%, by weight based on the total weight of the selexipag-containing layer.

### Claim 3 (depends on 1, 2)

Transdermal therapeutic system according to claim 1 or 2, wherein the selexipag-containing layer further comprises an enhancer, preferably selected from the group consisting of tetrahydrofurfuryl alcohol polyethylene glycol ether, levulinic acid, transcutol, lauryl lactate, methyl laurate, dihydrolevoglucosenone, dimethyl propylene urea and a mixtures thereof, and in particular methyl laurate and/or wherein the selexipag-containing layer further comprises an enhancer in the range from 2.0 to 15.0%, more preferably from 3.0 to 8.0% by weight based on the total weight of the selexipag-containing layer.

### Claim 4 (depends on 1, 2, 3)

Transdermal therapeutic system according to any one of claims 1 to 3, wherein the at least one nonpolar polymer is a pressure sensitive adhesive and/or wherein the least one nonpolar polymer is selected from the group consisting of a silicone polymer, a polyisobutylene polymer, a styrenic polymer, and mixtures thereof, preferably selected from a polyisobutylene polymer, a styrenic polymer, and mixtures thereof.

### Claim 5 (depends on 1, 2, 3, 4)

Transdermal therapeutic system according to any one of claims 1 to 4, wherein the at least one nonpolar polymer is a polyisobutylene mixture being a combination of polyisobutylene and polybutene, preferably wherein the weight ratio of the mass of the polyisobutylene to the mass of the polybutene is of 20:1 to 1:1, and in particular of 8:1 to 3:1.

### Claim 6 (depends on 1, 2, 3, 4, 5)

Transdermal therapeutic system according to any one of claims 1 to 5, wherein the at least one nonpolar polymer is a styrenic polymer, preferably a styrene-isoprene-styrene block copolymer, more preferably wherein the weight ratio of the mass of the styrene to the mass of the isoprene is of 1:20 to 1:2, preferably of 1:15 to 1:3.

### Claim 7 (depends on 6)

Transdermal therapeutic system according to claim 6, wherein the selexipag-containing layer further comprises a tackifier, preferably a thermoplastic ester resin, and in particular a thermoplastic ester resin derived from glycerol and a highly stabilized rosin.

### Claim 8 (depends on 6, 7)

Transdermal therapeutic system according to claim 6 or 7, wherein the selexipag-containing layer further comprises a tackifier,
wherein the weight ratio of the mass of the styrenic polymer to the mass of the tackifier is of 1:5 to 1:1, preferably of 1:4 to 1:2 and/or wherein a content of the tackifier in the selexipag-containing layer ranges from 30.0 to 80.0%, preferably from 40.0 to 70.0%, and in particular from 45.0 to 60.0%, by weight based on the total weight of the selexipag-containing layer.

### Claim 9 (depends on 1, 2, 3, 4, 5, 6, 7, 8)

Transdermal therapeutic system according to any one of claims 1 to 8, wherein the at least one polar polymer is selected form the group consisting of acrylic polymer, polyvinylpyrrolidone, and mixtures thereof.

### Claim 10 (depends on 1, 2, 3, 4, 5, 6, 7, 8, 9)

Transdermal therapeutic system according to any one of claims 1 to 9, wherein the at least one polar polymer is polyvinylpyrrolidone, preferably crospovidone.

### Claim 11 (depends on 1, 2, 3, 4, 5, 6, 7, 8, 9, 10)

Transdermal therapeutic system according to any one of claims 1 to 10, wherein a content of the at least one nonpolar polymer in the selexipag-containing layer ranges from 50.0 to 90.0%, preferably from 60.0 to 85.0%, and in particular from 70.0 to 80.0%, by weight based on the total weight of the selexipag-containing layer or
wherein a content of the at least one nonpolar polymer in the selexipag-containing layer ranges from 5.0 to 40.0%, preferably from 10.0 to 30.0%, and in particular from 12.0 to 25.0%, by weight based on the total weight of the selexipag-containing layer.

### Claim 12 (depends on 1, 2, 3, 4, 5, 6, 7, 8, 9, 10, 11)

Transdermal therapeutic system according to any one of claims 1 to 11, wherein a content of the at least one polar polymer, preferably polyvinylpyrrolidone, in the selexipag-containing layer ranges from 5.0 to 30.0%, preferably from 15.0 to 27.0%, by weight based on the total weight of the selexipag-containing layer.

### Claim 13 (depends on 1, 2, 3, 4, 5, 6, 7, 8, 9, 10, 11, 12)

Transdermal therapeutic system according to any one of claims 1 to 12, wherein the selexipag-containing layer is a selexipag-containing matrix layer; and/or wherein the area weight of the selexipag-containing layer ranges from 70 to 220 g/m2, preferably from 95 to 160 g/m2.

### Claim 14 (depends on 1, 2, 3, 4, 5, 6, 7, 8, 9, 10, 11, 12, 13)

Transdermal therapeutic system according to any one of claims 1 to 13,
providing a cumulative permeated amount of selexipag as measured in a Franz diffusion cell with dermatomed human skin of 10 μg/cm2 to 120 μg/cm2, preferably of 20 μg/cm2 to 115 μg/cm2 over a time period of 48 hours and/or
providing a cumulative permeated amount of selexipag as measured in a Franz diffusion cell with dermatomed human skin of 30 μg/cm2 to 250 μg/cm2, preferably of 65 μg/cm2 to 230 μg/cm2 over a time period of 168 hours.

### Claim 15 (depends on 1, 2, 3, 4, 5, 6, 7, 8, 9, 10, 11, 12, 13, 14)

Transdermal therapeutic system according to any one of claims 1 to 14 for use in a method of treating a human patient.
