# US 2019/0314294 A1 · Polyvinylpyrrolidone For The Stabilization Of A Solid Dispersion Of The Non-Crystalline Form Of Rotigotine

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- Number: US 2019/0314294 A1
- Document ID: US20190314294A1
- Status: Published application
- Kind: A1
- Application number: 16/420,501
- Filed: 2019-05-23
- Published: 2019-10-17
- Earliest claimed: 2009-12-22
- Assignees: UCB Pharma S.A.; LTS Lohmann Therapie-Systeme AG
- Applicants: UCB Pharma GmbH
- Inventors: Hans-Michael WOLFF; Christoph ARTH; Luc QUERE; Walter MÜLLER
- Web page: https://patentgrep.com/patent/US20190314294A1

## CPC

- A61K 9/7069: {obtained otherwise than by reactions only involving carbon to carbon unsaturated bonds, e.g. polysiloxane, polyesters, polyurethane, polyethylene oxide}
- A61K 9/7053: {obtained by reactions only involving carbon to carbon unsaturated bonds, e.g. polyvinyl, polyisobutylene, polystyrene}
- A61K 31/381: having five-membered rings
- A61P 25/00: Drugs for disorders of the nervous system
- A61P 25/14: for treating abnormal movements, e.g. chorea, dyskinesia
- A61P 25/16: Anti-Parkinson drugs
- A61P 25/24: Antidepressants
- A61P 25/28: for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
- A61P 29/00: Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
- A61P 43/00: Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
- 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 present invention relates to a method for stabilizing rotigotine, the method comprising providing a solid dispersion comprising polyvinylpyrrolidone and a nom-crystalline form of rotigotine, wherein the weight ratio of rotigotine to polyvinylpyrrolidone is in a range from about 9:3.5 to about 9:6. The present invention also relates to a solid dispersion comprising a dispersing agent and a dispersed phase, said dispersed phase comprising rotigotine and polyvinylpyrrolidone wherein the weight ratio of rotigotine to polyvinylpyrrolidone is in a range from about 9:3.5 to about 9:6, a pharmaceutical composition comprising such a solid dispersion, in particular a transdermal therapeutic system, as well as a method for the preparation thereof.

## Claims

### Claim 1

A method for stabilizing rotigotine, the method comprising providing a solid dispersion comprising polyvinylpyrrolidone and a non-crystalline form of rotigotine, wherein the weight ratio of rotigotine to polyvinylpyrrolidone is in a range from about 9:3.5 to about 9:6.

### Claim 2 (depends on 1)

The method of claim 1, wherein the weight ratio of rotigotine to polyvinylpyrrolidone is in a range from about 9:3.5 to about 9:4.5.

### Claim at position 3

3-13. (canceled)

### Claim 14

A method for preparing a transdermal therapeutic system, the method comprising preparing a solid dispersion comprising a dispersing agent and a dispersed phase, said dispersed phase comprising rotigotine and polyvinylpyrrolidone (PVP), wherein the weight ratio of rotigotine to PVP is in a range from about 9:3.5 to about 9:6.

### Claim 15 (depends on 14)

The method of claim 14, wherein the weight ratio of rotigotine to (PVP) is in a range from about 9:3.5 to about 9:4.5.

### Claim 16 (depends on 14)

The method of claim 14, wherein the rotigotine is rotigotine free base.

### Claim 17 (depends on 16)

The method of claim 16, further comprising mixing rotigotine free base and the PVP in a solution to obtain the dispersed phase.

### Claim 18 (depends on 14)

The method of claim 14, wherein the PVP has a molecular weight of 1,000,000 to 1,500,000 g/mol.

### Claim 19 (depends on 14)

The method of claim 14, wherein the dispersing agent comprises at least one silicone pressure sensitive adhesive.

### Claim 20 (depends on 19)

The method of claim 19, wherein the dispersing agent comprises a mixture of at least two silicone pressure sensitive adhesives.

### Claim 21 (depends on 20)

The method of claim 20, wherein the mixture of at least two silicone pressure sensitive adhesives comprises BIO-PSA® Q7 4301 and BIO-PSA® Q7 4201.

### Claim 22 (depends on 14)

The method of claim 14, wherein the dispersing agent comprises at least a first adhesive having a complex viscosity between 40 and 250 MP.

### Claim 23 (depends on 14)

The method of claim 14, wherein the dispersing agent comprises at least a second adhesive having a complex viscosity between 1 and 10 MP.

### Claim 24 (depends on 14)

The method of claim 14, wherein the dispersing agent has a complex viscosity between 5 and 25 MP.

### Claim 25 (depends on 14)

The method of claim 14, wherein the dispersing agent comprises at least a first adhesive and a second adhesive and the solid dispersion has a complex viscosity between 5 and 15 MP.

### Claim 26 (depends on 14)

The method of claim 14, wherein the dispersing agent comprises at least a first adhesive and a second adhesive and the solid dispersion has a peel adhesion between 3 and 16 N/50 mm at a thickness of 50 g/m2 and/or a peel adhesion between 14 and 26 N/50 mm at a thickness of 150 g/m2.

### Claim 27 (depends on 14)

The method of claim 14, wherein the dispersing agent comprises at least a first adhesive and a second adhesive and the solid dispersion has a static shear adhesion between 20 and 150 min.
