# US 10,307,382 B2 · Transdermal therapeutic system for 5-aminolevulinic acid hydrochloride

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- Number: US 10,307,382 B2
- Document ID: US10307382B2
- Status: Granted
- Kind: B2
- Application number: 14/240,810
- Filed: 2012-08-24
- Published: 2014-10-30
- Granted: 2019-06-04
- Earliest claimed: 2011-08-31
- Assignees: Photonamic GmbH & Co. KG
- Applicants: Tobias Jung; Michael Horstmann; Gerd Hoffmann
- Inventors: Tobias Jung; Michael Horstmann; Gerd Hoffmann
- Web page: https://patentgrep.com/patent/US10307382B2

## CPC

- A61K 9/7061: {Polyacrylates}
- A61K 31/195: having an amino group
- A61K 31/197: the amino and the carboxyl groups being attached to the same acyclic carbon chain, e.g. gamma-aminobutyric acid [GABA], beta-alanine, epsilon-aminocaproic acid or pantothenic acid (carnitine A61K31/205)
- A61P 17/00: Drugs for dermatological disorders
- A61P 35/00: Antineoplastic agents
- 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)
- A61P: SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS

## Abstract

The invention relates to a transdermal therapeutic system, comprising a back layer that is impermeable to an active ingredient, a polymer matrix containing the active ingredient, and a protective layer that can be pulled off, wherein 5-aminolevulinic acid hydrochloride is used as the active ingredient and the basic polymer of the polymer matrix is an adhesive polyacrylate. Said transdermal therapeutic system is suitable for diagnosing and treating preliminary stages of skin cancer, such as actinic keratosis, and oncological skin diseases.

## Claims

### Claim 1

A transdermal therapeutic system, comprising:
a back layer that is impermeable to an active ingredient;
an active ingredient-containing polymer matrix; and
a protective layer that can be pulled off;
wherein the polymer matrix consists of:
about 28% by weight of crystalline 5-aminolevulinic acid hydrochloride as the active ingredient; and
about 72% by weight of a non-crosslinked polyacrylate adhesive based on acrylic acid, 2-ethylhexyl acrylate, and methyl acrylate;
wherein the transdermal therapeutic system is a monolithic active ingredient-in-adhesive system; and
wherein the transdermal therapeutic system releases within about four hours, an amount of at least 3 mg 5-aminolevulinic acid hydrochloride.

### Claim 2 (depends on 1)

The transdermal therapeutic system according to claim 1;
wherein 50% of the crystals of the crystalline 5-aminolevulinic acid hydrochloride are larger than the layer thickness of the polymer matrix.

### Claim 3 (depends on 1)

The transdermal therapeutic system according to claim 1;
wherein more than 99.9% of the crystals of the crystalline 5-aminolevulinic acid hydrochloride are smaller than about 250 μm.

### Claim 4 (depends on 1)

The transdermal therapeutic system according to claim 1;
wherein the polyacrylate has acid functionalities.

### Claim 5 (depends on 1)

A method comprising:
utilizing the transdermal therapeutic system according to claim 1 as a therapeutic agent.

### Claim 6 (depends on 1)

A method comprising:
utilizing the transdermal therapeutic system according to claim 1 for treating preliminary skin cancer stages.

### Claim 7 (depends on 1)

A method comprising:
utilizing the transdermal therapeutic system according to claim 1 for diagnosing and treating preliminary skin cancer stages.

### Claim 8 (depends on 3)

The transdermal therapeutic system according to claim 3;
wherein more than 99.9% of the crystals of the crystalline 5-aminolevulinic acid hydrochloride have a particle size of 90 to 160 μm.

### Claim 9 (depends on 6)

The method according to claim 6;
wherein the skin cancer is selected from the group consisting of actinic keratosis and oncological skin diseases.

### Claim 10 (depends on 7)

The method according to claim 7;
wherein the skin cancer is selected from the group consisting of actinic keratosis and oncological skin diseases.

### Claim 11 (depends on 1)

The transdermal therapeutic system according to claim 1;
wherein the transdermal therapeutic system releases at least 35% of the 5-aminolevulinic acid hydrochloride within thirty minutes.

### Claim 12 (depends on 1)

The transdermal therapeutic system according to claim 1;
wherein the polymer matrix consists of:
28% by weight of crystalline 5-aminolevulinic acid hydrochloride as the active ingredient; and
72% by weight of a non-crosslinked polyacrylate adhesive based on acrylic acid, 2-ethylhexyl acrylate, and methyl acrylate.