Intranasal formulation of rotigotine

• US 7,683,040 B2
• Filed: 12/22/2004
• Issued: 03/23/2010
• Est. Priority Date: 12/23/2003
• Status: Expired due to Fees

• Current Assignee: UCB Pharma GmbH (UCB SA)
• Original Assignee: SRZ Properties Incorporated
• Inventors: Kramer, Robert
• Primary Examiner(s): Maier; Leigh C
• Application Number:
  US10/545,530
• Publication Number:
  US 20070191308A1
• Time in Patent Office: 1,917 Days
• Field of Search: None
• US Class Current: 514/58
• 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. A liquid intranasal pharmaceutical formulation comprising a pharmaceutically acceptable acid addition salt of rotigotine and α

-cyclodextrin.

2. The formulation of claim 1, further comprising a buffer system.

3. The formulation of claim 2, wherein the buffer system is phosphate buffered saline.

4. The formulation of claim 1, further comprising a viscosity-enhancing substance effective to give a viscosity of 0.5-1.5 mm²/s.

5. The formulation of claim 4, wherein the viscosity-enhancing substance is glycerol.

6. The formulation of claim 1, having a pH of 5-6.5.

7. The formulation of claim 1, further comprising a pharmaceutically acceptable acid for adjustment of pH.

8. The formulation of claim 7, wherein the pharmaceutically acceptable acid is citric acid.

9. The formulation of claim 1 that does not contain any preservative.

10. The formulation of claim 1 that does not contain any antioxidant.

11. The formulation of claim 1, further comprising an absorption enhancer selected from non-ionic surfactants.

12. The formulation of claim 11, wherein the absorption enhancer is polysorbate 80 or PEG-40 hydrogenated castor oil.

13. The formulation of claim 1, wherein the pharmaceutically acceptable acid addition salt of rotigotine is rotigotine hydrochloride.

14. The formulation of claim 13, comprising 1-6 mg/ml rotigotine hydrochloride in an aqueous buffered solution.

15. The formulation of claim 13, comprising between 0.03 and 0.1 g/ml α

-cyclodextrin in an aqueous buffered solution.

16. The formulation of claim 3, wherein the formulation comprises 2-5 mg/ml rotigotine hydrochloride, 0.05-0.1 g/ml α

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

17. The formulation of claim 16, further comprising citric acid in an amount effective to adjust pH of the formulation to a value of 5-6.5.