Iontophoretic delivery of rotigotine for the treatment of Parkinson's disease

• US 20040116537A1
• Filed: 11/17/2003
• Published: 06/17/2004
• Est. Priority Date: 12/02/2002
• Status: Active Grant

• Current Assignee: UCB Pharma GmbH (UCB SA)
• Original Assignee: UCB Pharma GmbH (UCB SA)
• Inventors: Bouwstra, Johanna Aaltje, Li, Gai Ling, Nugroho, Akhmad Kharis, Wolff, Hans-Michael
• Granted Patent: US 7,632,859 B2
• Time in Patent Office: Days
• US Class Current: 514/663
• CPC Class Codes: A61K 31/381 having five-membered rings
• CPC Class Codes: A61K 9/0009 involving or responsive to electricity, magnetism or acoustic waves; Galenical aspects of sonophoresis, iontophoresis, electroporation or electroosmosis microelectromechanical systems A61K9/0097
• CPC Class Codes: A61P 25/00 Drugs for disorders of the nervous system
• CPC Class Codes: A61P 25/16 Anti-Parkinson drugs

Abstract

By using a composition comprising rotigotine and at least one chloride salt in a concentration of 1 to 140 mmol/l, the composition having a pH of 4 to 6.5 in a iontophoretic device for the treatment of Parkinson'"'"'s disease, it became possible to obtain a rotigotine flux across the human stratum corneum which was higher than the one previously obtained with conventional passive diffusion systems.

Claims

1. Use of a composition comprising rotigotine and at least one chloride salt in a concentration of 1 to 140 mmol/l, the composition having a pH of 4 to 6.5 for the preparation of a iontophoretic device for the treatment of Parkinson'"'"'s disease.

2. Use according to claim 1, wherein the concentration of rotigotine is at least 0.5 mg/ml.

3. Use according to any one of claims 1 or 2, wherein the concentration of rotigotine is 0.5 to 3 mg/ml.

4. Use according to any one of claims 1 to 3, wherein the chloride salt is selected from NaCl, triethylammonium chloride and tributylammonium chloride.

5. Use according to claim 4, wherein the chloride salt is triethylammonium chloride or tributylammonium chloride.

6. Use according to any one of claims 1 to 5, wherein the concentration of the chloride salt is 60 to 80 mmol/l.

7. Use according to any one of claims 1 to 6, wherein the composition is used in the donor phase of the iontophoretic device.

8. Use according to any one of claims 1 to 7, wherein the composition in the donor phase of the iontophoretic device comprises rotigotine in a concentration of 0.5 to 3 mg/ml and at least one of triethylammonium chloride and tributylammonium chloride in a concentration of 60 to 80 mmol/l, wherein the pH of the donor phase is 4.5 to 5.5.

9. A method for the treatment of Parkinson'"'"'s disease characterised by applying a iontophoretic device, which comprises a composition comprising rotigotine and at least one chloride salt in a concentration of 1 to 140 mmol/l, the composition having a pH of 4 to 6.5, onto the skin of a patient in need thereof.