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Claims for Patent: 8,454,998

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Claims for Patent: 8,454,998

Title:Controlled release formulations of levodopa and uses thereof
Abstract: The current invention provides a controlled release oral solid formulation of levodopa comprising levodopa, a decarboxylase inhibitor, and a carboxylic acid. Also provided by this invention is multiparticulate, controlled release oral solid formulations of levodopa comprising: i) a controlled release component comprising a mixture of levodopa, a decarboxylase inhibitor and a rate controlling excipient; ii) a carboxylic acid component; and iii) an immediate release component comprising a mixture of levodopa and a decarboxylase inhibitor.
Inventor(s): Hsu; Ann (Los Altos Hills, CA), Kou; Jim H. (San Jose, CA), Alani; Laman (Hillsborough, CA)
Assignee: Impax Laboratories, Inc. (Hayward, CA)
Application Number:13/367,230
Patent Claims: 1. A method for the symptomatic treatment of a movement disorder selected from a group consisting of Parkinson's disease, secondary parkinsonism, postencephalitic parkinsonism, symptomatic parkinsonism, and injury to the nervous system by carbon monoxide or managanese intoxication comprising administering to a patient an effective amount of a controlled release oral solid formulation of levodopa, (i) wherein the controlled release oral solid formulation of levodopa is a multiparticulate, controlled release oral solid formulation of levodopa comprising (a) a controlled release component comprising levodopa, carbidopa and one or more rate controlling excipients; (b) an immediate release component comprising levodopa and carbidopa, and (c) a carboxylic acid component comprising (1) a carboxylic acid that is not levodopa or carbidopa and (2) one or more rate controlling excipients, wherein the carboxylic acid component is a distinct component and is coated with an enteric polymer; and wherein the controlled release component (a), the immediate release component (b) and the carboxylic acid component (c) comprise beads or granules.

2. The method of claim 1, wherein the disorder is Parkinson's disease.

3. The method of claim 1, wherein Parkinson's disease is idiopathic Parkinson's disease.

4. The method of claim 1, wherein the disorder is secondary parkinsonism.

5. The method of claim 1, wherein the carboxylic acid is selected from a group consisting of tartaric acid, adipic acid, succinic acid, citric acid, benzoic acid, acetic acid, edetic acid, fumaric acid, lactic acid, malic acid, oleic acid, sorbic acid, stearic acid, palmitic acid and boric acid or mixtures thereof

6. The method of claim 1, wherein the carboxylic acid is tartaric acid.

7. The method of claim 1, wherein the carbidopa and levodopa are present in the formulation in a ratio of about 1:4.

8. The method of claim 1, wherein the disorder is postencephalitic parkinsonism.

9. The method of claim 1, wherein the disorder is symptomatic parkinsonism.

10. The method of claim 1, wherein the controlled release oral solid formulation has a levodopa plasma or serum concentration profile comprising: a. a time of administration, b. a first concentration, and c. a second concentration, wherein, said first concentration is equal to the maximum concentration of said profile; said second concentration is the minimum concentration occurring at a time later than said first concentration and earlier than or equal to about six hours following said time of administration; and wherein said second concentration is greater than or equal to about fifty percent of said first concentration.

11. The method of claim 1, wherein the disorder is an injury to the nervous system by carbon monoxide or manganese intoxication.

12. The method of claim 1, wherein the bead or granule is in a tablet or capsule.

13. The method of claim 1, wherein the bead or granule of the controlled release component has a size that passes through (a) 12, 14, or 16 mesh but is retained on 18 or 25 mesh screens or (b) 18 mesh but is retained on 25 mesh screens.

14. The method of claim 1, wherein the multiparticulate, controlled release oral solid formulation of levodopa is encapsulated in a capsule and the beads or granules therein may be removed from the capsule and sprinkled on food or liquid prior to administration.

15. The method of claim 1, wherein the controlled release component and the carboxylic acid component are separately coated with an enteric polymer.

16. The method of claim 1, wherein the controlled release oral solid formulation of levodopa has a ratio of moles of carboxylic acid to levodopa of greater than 1:4.

17. The method of claim 1, wherein the controlled release oral solid formulation of levodopa has a ratio of moles of carboxylic acid to levodopa of greater than 1:4 and less than 3:2.

18. The method of claim 1, wherein the patient is human and a single dose of the controlled release oral solid formulation administered to a human provides a levodopa plasma concentration profile comprising: a. a time of administration; b. a first peak concentration at a first time that occurs less than or equal to about two hours from said time of administration; c. a second peak concentration at a second time that occurs between about 4 and about 7 hours after said time of administration.

19. The method of claim 18, wherein the minimum concentration between the first time and the second time is greater than or equal to 50% of the first peak concentration and greater than or equal to 50% of the second peak concentration.

20. The method of claim 1, wherein the controlled release oral solid formulation of levodopa comprises two controlled release components that release carbidopa and levodopa at different rates.

21. The method of claim 1, wherein the controlled release component comprises a carbidopa bead.

22. The method of claim 1, wherein the controlled release component comprises a levodopa bead.

23. The method of claim 1, wherein the component of (a), (b), or (c) is a bead or granule.

24. The method of claim 1, wherein the carboxylic acid is tartaric acid and the ratio of carbidopa to levodopa is about 1:4, and a ratio of moles of carboxylic acid to levodopa is greater than 1:4 and less than 3:2.

25. The method of claim 1, wherein the amount of carbidopa is about 48.75 mg and the amount of levodopa is about 195 mg.

26. The method of claim 1, wherein the amount of carbidopa is about 61.25 mg and the amount of levodopa is about 245 mg.

27. The method of claim 1, wherein the rate controlling excipient is an enteric polymer or a mixture of more than one type of enteric polymer.

28. The method of claim 1, wherein the carboxylic acid is physically separated from levodopa and carbidopa.

29. The method of claim 1, wherein a ratio in weight of levodopa:carbidopa:carboxylic acid component is any of: a. 245.00 mg:61.25 mg:132.53 mg; b. 195.00 mg:48.75 mg:105.48 mg; c. 190.00 mg:47.50 mg:88.52 mg; d. 180.00 mg:45.00 mg:82.20 mg; e. 180.00 mg:45.00 mg:54.80 mg; f. 120.00 mg:30.00 mg:103.20 mg; or g. 150.00 mg:37.50 mg:134.50 mg; with each value capable of varying by +10%.

30. The method of claim 12, wherein the tablet is a multi-layered or matrix tablet.
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