High concentration baclofen preparations

Patent metadata

Field	Value
Publication number	US-9289408-B2
Application number	US-201313961352-A
Country	US
Kind code	B2
Filing date	Aug 7, 2013
Priority date	Jul 12, 2004
Publication date	Mar 22, 2016
Grant date	Mar 22, 2016

Abstract

Stable aqueous solutions comprising concentrations of baclofen in the range of greater than 2.0 mg/mL up to about 10 mg/mL are disclosed. These solutions can be used as pharmaceuticals for parenteral or oral administration. The invention also provides methods of preparing said stable aqueous baclofen solutions.

First claim

What is claimed is:

1. A solution for intrathecal administration, the solution consisting of baclofen at a concentration from about 2.8 mg/mL to about 6.0 mg/mL and normal saline, wherein the solution is stable for at least 60 days at 37° C.

2. The solution of claim 1 , wherein the solution is stable for at least 12 months at room temperature.

3. The solution of claim 1 , wherein the baclofen is at a concentration of from about 3.0 mg/mL to about 4.2 mg/mL.

4. The solution of claim 1 , wherein the baclofen is at a concentration of from greater than about 3.5 mg/mL to less than about 4.0 mg/mL.

5. The solution of claim 1 , wherein the baclofen is at a concentration of about 3.4 mg/mL.

6. The solution of claim 1 , wherein the baclofen is at a concentration of about 3.6 mg/mL.

7. The solution of claim 1 , wherein the baclofen is at a concentration of about 3.7 mg/mL.

8. The solution of claim 1 , wherein the baclofen is at a concentration of about 3.8 mg/mL.

9. The solution of claim 1 , wherein the baclofen is at a concentration of about 3.9 mg/mL.

10. The solution of claim 1 , wherein the baclofen is at a concentration of about 4.1 mg/mL.

11. A medical package comprising a single dose container and the solution of claim 1 , wherein the solution is disposed within the single dose container.

12. The medical package of claim 11 , wherein the container is a vial.

13. The medical package of claim 12 , wherein the vial comprises 20 mL of the solution.

14. The medical package of claim 11 , wherein the container is a syringe.

15. The medical package of claim 14 , wherein the syringe comprises 20 mL of the solution.

16. A method of managing severe spasticity of spinal cord origin, the method comprising administering intrathecally to a patient in need thereof the solution of claim 1 .

17. The medical package of claim 11 , wherein the solution is stable for at least 12 months at room temperature.

18. The medical package of claim 11 , wherein when the concentration of the solution is from about 2.8 to 4.0 mg/mL, the solution is stable for at least 24 months at room temperature, and when the concentration of the solution is greater than 4.0 mg/mL to about 6.0 mg/mL, the solution is stable for at least 16 months at room temperature.

19. A solution consisting of baclofen at a concentration of greater than 4.0 mg/mL to about 6.0 mg/mL and normal saline, wherein the solution is stable for at least 30 days at 37° C.

20. The solution of claim 19 , wherein the solution is stable for at least 60 days at 37° C.

21. The solution of claim 19 , wherein the solution is stable for at least 16 months at room temperature.

Assignees

• Univ Texas

Inventors

• Trissel Lawrence A
• Zhang Yanping

Classifications

• A61K31/195

  having an amino group · CPC title

• A61K31/197 Primary

  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) · CPC title

• A61K9/08

  Solutions {(composition of solutions A61K47/00)} · CPC title

• A61P43/00

  Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00 · CPC title