Intranasal formulation of rotigotine

• US 20070191308A1
• Filed: 12/22/2004
• Published: 08/16/2007
• Est. Priority Date: 12/23/2003
• Status: Active Grant

• Current Assignee: UCB Pharma GmbH (UCB SA)
• Original Assignee: SRZ Properties Incorporated
• Inventors: Kramer, Robert
• Granted Patent: US 7,683,040 B2
• Time in Patent Office: Days
• US Class Current: 514/60
• CPC Class Codes: A61K 31/381 having five-membered rings
• CPC Class Codes: A61P 25/00 Drugs for disorders of the nervous system
• CPC Class Codes: A61P 25/16 Anti-Parkinson drugs
• CPC Class Codes: A61P 43/00 Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00

Abstract

This invention pertains to a liquid intranasal pharmaceutical formulation comprising a pharmaceutically acceptable acid addition salt of rotigotine and α-cyclodextrin, preferably in the form of a buffered aqueous solution having a viscosity of 0.5-1.5 mm²/s

Claims

1. Liquid intranasal pharmaceutical formulation comprising a pharmaceutically acceptable acid addition salt of rotigotine and α

-cyclodextrin.

2. Intranasal formulation according to claim 1 characterised in that it further contains a buffer system.

3. Intranasal formulation according to claim 2 characterised in that the buffer system is phosphate buffered saline (PBS).

4. Intranasal formulation according to any of the preceding claims characterised in that it further contains a viscosity-enhancing substance so as to give a viscosity of 0.5-1.5 mm²/s.

5. Intranasal formulation according to claim 4 characterised in that the viscosity-enhancing substance is glycerol.

6. Intranasal formulation according to any of the preceding claims characterised in that it has a pH-value in the range of 5-6.5.

7. Intranasal formulation according to any of the preceding claims characterised in that it further contains a pharmaceutically acceptable acid for the adjustment of the pH-value.

8. Intranasal formulation according to claim 7 characterised in that the pharmaceutically acceptable acid is citric acid.

9. Intranasal formulation according to any of the preceding claims characterised in that the formulation does not contain a solubility enhancer.

10. Intranasal formulation according to any of the preceding claims characterised in that it does not contain any preservative.

11. Intranasal formulation according to any of the preceding claims characterised in that it does not contain any antioxidants.

12. Intranasal formulation according to any of the preceding claims characterised in that it further contains an absorption enhancer selected from non-ionic surfactants.

13. Intranasal formulation according to claim 12 characterised in that the absorption enhancer is TWEEN 80 or cremophor RH40.

14. Intranasal formulation according to any of the preceding claims characterised in that the pharmaceutically acceptable acid addition salt of rotigotine is rotigotine hydrochloride.

15. Intranasal formulation according to any of the preceding claims characterised in that it contains 1-6 mg/ml rotigotine-HCL in an aqueous buffered solution.

16. Intranasal formulation according to any of the preceding claims characterised in that the formulation contains between 0.03 and 0.1 g/ml α

-cyclodextrin in the solution.

17. Intranasal formulation according to any of the preceding claims characterised in that it consists of 2-5 mg/ml rotigotine-HCl, 0.05-0.1 g/ml α

-cyclodextrin and 2.2-3% glycerol in phosphate buffered saline (PBS).

18. Intranasal formulation according to claim 17 characterised in that it further contains citric acid to adjust the pH-value between 5 and 6.5.