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Claims for Patent: 9,089,608

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Claims for Patent: 9,089,608

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 Lynn (Fort Worth, TX)
Assignee: Impax Laboratories, Inc. (Hayward, CA)
Application Number:14/030,792
Patent Claims: 1. A controlled release oral solid formulation of levodopa comprising: a. levodopa, b. a decarboxylase inhibitor, and c. a carboxylic acid that is not (a) or (b), wherein the carboxylic acid of (c) is in a distinct bead from (a) or (b).

2. The controlled release oral solid formulation 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, ascorbic acid, edetic acid, fumaric acid, lactic acid, malic acid, oleic acid, sorbic acid, stearic acid, palmitic acid and boric acid or mixtures thereof.

3. The controlled release oral solid formulation of claim 1, wherein the carboxylic acid is a polycarboxylic acid.

4. The controlled release oral solid formulation of claim 1, wherein the carboxylic acid is a dicarboxylic acid.

5. The controlled release oral solid formulation of claim 4, wherein the dicarboxylic acid is tartaric acid.

6. The controlled release oral solid formulation of claim 1, wherein the decarboxylase inhibitor is carbidopa.

7. The controlled release oral solid formulation of claim 1, wherein the formulation is a tablet or a caplet.

8. The controlled release oral solid formulation of claim 1, wherein the formulation is a multiparticulate formulation.

9. The controlled release oral solid formulation of claim 1, wherein the formulation reduces intrasubject variability in levodopa absorption.

10. The controlled release oral solid formulation of claim 9, wherein the intrasubject variability; calculated as the standard deviation of the levodopa concentration divided by the mean levodopa concentration determined over the range of 0.5 hours after administration to six hours after administration for a single dose of said formulation to an individual subject, and averaged over at least 12 subjects; is less than or equal to 0.40.

11. The controlled release oral solid formulation of claim 6, wherein the carbidopa and levodopa are present in the formulation in a ratio of about 1:1 to about 1:10.

12. The controlled release oral solid formulation of claim 11, wherein the ratio of carbidopa to levodopa is about 1:4.

13. The controlled release oral solid formulation of claim 4, having a ratio of moles of dicarboxylic acid to levodopa of greater than 1:4 and less than 3:2.

14. The controlled release oral solid formulation of claim 1, comprising from about 25 mg to about 2000 mg levodopa.

15. The controlled release oral solid formulation of claim 1 comprising 10 mg to 80 mg carbidopa.

16. A controlled release oral solid formulation of levodopa of claim 1 having 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.

17. The formulation of claim 16, wherein said concentration profile is the mean plasma or serum concentration profile.

18. The formulation of claim 16, wherein said concentration profile further comprises a third concentration, wherein said third concentration is greater than or equal to fifty percent of said first concentration and said third concentration occurs at a time earlier than said first concentration and within about ninety minutes of said time of administration.

19. The formulation of claim 16, having a ratio of mean AUC in said profile, where said AUC is measured in units of ng h/mL, to the mass of levodopa in the formulation, where said mass is measured in mg, is between 11:1 and 25:1.

20. The formulation of claim 16, having a mean AUC in said profile of between 4330 and 8000 ng h/mL for a 380 mg dose of levodopa.

21. A controlled release oral solid formulation of levodopa having a median levodopa plasma or serum concentration profile comprising: a. a time of administration; b. a first concentration at a first time, that occurs within one hour of said time of administration; c. a second concentration at a second time, that occurs after said first time; d. a third concentration at a third time, that occurs at least four hours after said second time; wherein said second concentration is equal to the maximum concentration of said profile; said first concentration is equal to about fifty percent of said second concentration; said third concentration is equal to about fifty percent of said second concentration.
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