IP Library Granted Patent US 11,123,344
Granted Patent B2
US 11,123,344 · App. 17/071,925 · Granted Sep 21, 2021

Bupropion as a modulator of drug activity

Inventor: Herriot Tabuteau (New York, NY)
Assignee: AXSOME THERAPEUTICS, INC.
A61K31/485A61K9/0053A61K31/137A61K31/138A61K31/4748
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Quick Facts
Patent No.
US 11,123,344
App. No.
17/071,925
Granted
Sep 21, 2021
Kind
B2
Abstract

Dosage forms, drug delivery systems, and methods related to sustained release of dextromethorphan or improved therapeutic effects are disclosed. Typically, bupropion or a related compound is orally administered to a human being to be treated with, or being treated with, dextromethorphan.

Claims (30)

1. A method of enhancing dextromethorphan plasma levels in a human being, comprising co-administering a bupropion with a dextromethorphan, to the human being, twice daily for at least eight consecutive days, wherein the human being is a non-poor metabolizer of dextromethorphan in need of treatment with dextromethorphan, wherein the weight ratio of the dextromethorphan to the bupropion is about 0.4 to about 0.7, wherein, on the eighth day that the bupropion and the dextromethorphan are co-administered, the AUC 0-inf of dextromethorphan is at least about 15 times the AUC 0-inf of dextromethorphan that would result from administering the same amount of the dextromethorphan twice daily without the bupropion for eight consecutive days, and wherein the AUC 0-inf of dextromethorphan is at least about 2,400 ng·hr/mL.

2. The method of claim 1 , wherein the bupropion and the dextromethorphan are administered in a single dosage form.

3. The method of claim 2 , wherein the single dosage form is a solid.

4. The method of claim 2 , wherein about 40 mg to about 50 mg of the dextromethorphan is administered in the single dosage form.

5. The method of claim 2 , wherein about 30 mg to about 40 mg of the dextromethorphan is administered in the single dosage form.

6. The method of claim 2 , wherein about 30 mg to about 60 mg of the dextromethorphan is administered in the single dosage form.

7. The method of claim 2 , wherein a daily dose of about 150 mg to about 200 mg of the bupropion is administered.

8. The method of claim 2 , wherein a daily dose of about 200 mg to about 250 mg of the bupropion is administered.

9. The method of claim 1 , wherein the weight ratio of the dextromethorphan to the bupropion is about 0.4 to about 0.45.

10. The method of claim 1 , wherein, on the eighth day that the bupropion and the dextromethorphan are co-administered, the AUC 0-inf of dextromethorphan is at least about 20 times the AUC 0-inf of dextromethorphan that would result from administering the same amount of the dextromethorphan without the bupropion for eight consecutive days.

11. A method of enhancing dextromethorphan plasma levels in a human being, comprising co-administering a bupropion with a dextromethorphan, to the human being, twice daily for at least eight consecutive days, wherein the human being is a non-poor metabolizer of dextromethorphan in need of treatment with dextromethorphan, wherein the weight ratio of the dextromethorphan to the bupropion is about 0.4 to about 0.7, wherein, on the eighth day that the bupropion and the dextromethorphan are co-administered, the AUC 0-inf of dextromethorphan is at least about 15 times the AUC 0-inf of dextromethorphan that would result from administering the same amount of the dextromethorphan twice daily without the bupropion for eight consecutive days, and wherein the AUC 0-inf of dextromethorphan is about 3,700 ng·hr/mL.

12. The method of claim 11 , wherein the bupropion and the dextromethorphan are administered in a single dosage form.

13. The method of claim 12 , wherein the single dosage form is a solid.

14. The method of claim 12 , wherein about 40 mg to about 50 mg of the dextromethorphan is administered in the single dosage form.

15. The method of claim 12 , wherein about 30 mg to about 40 mg of the dextromethorphan is administered in the single dosage form.

16. The method of claim 12 , wherein about 30 mg to about 60 mg of the dextromethorphan is administered in the single dosage form.

17. The method of claim 12 , wherein a daily dose of about 150 mg to about 200 mg of the bupropion is administered.

18. The method of claim 12 , wherein a daily dose of about 200 mg to about 250 mg of the bupropion is administered.

19. The method of claim 11 , wherein the weight ratio of the dextromethorphan to the bupropion is about 0.4 to about 0.45.

20. The method of claim 11 , wherein, on the eighth day that the bupropion and the dextromethorphan are co-administered, the AUC 0-inf of dextromethorphan is at least about 20 times the AUC 0-inf of dextromethorphan that would result from administering the same amount of the dextromethorphan without the bupropion for eight consecutive days.

21. A method of enhancing dextromethorphan plasma levels in a human being, comprising co-administering a bupropion with a dextromethorphan, to the human being, twice daily for at least eight consecutive days, wherein the human being is a non-poor metabolizer of dextromethorphan in need of treatment with dextromethorphan, wherein the weight ratio of the dextromethorphan to the bupropion is about 0.4 to about 0.7, wherein, on the eighth day that the bupropion and the dextromethorphan are co-administered, the AUC 0-inf of dextromethorphan is at least about 15 times the AUC 0-inf of dextromethorphan that would result from administering the same amount of the dextromethorphan twice daily without the bupropion for eight consecutive days, and wherein the AUC 0-inf of dextromethorphan is about 2,400 ng·hr/mL to 7,237 ng·hr/mL.

22. The method of claim 21 , wherein the bupropion and the dextromethorphan are administered in a single dosage form.

23. The method of claim 22 , wherein the single dosage form is a solid.

24. The method of claim 22 , wherein about 40 mg to about 50 mg of the dextromethorphan is administered in the single dosage form.

25. The method of claim 22 , wherein about 30 mg to about 40 mg of the dextromethorphan is administered in the single dosage form.

26. The method of claim 22 , wherein about 30 mg to about 60 mg of the dextromethorphan is administered in the single dosage form.

27. The method of claim 22 , wherein a daily dose of about 150 mg to about 200 mg of the bupropion is administered.

28. The method of claim 22 , wherein a daily dose of about 200 mg to about 250 mg of the bupropion is administered.

29. The method of claim 21 , wherein the weight ratio of the dextromethorphan to the bupropion is about 0.4 to about 0.45.

30. The method of claim 21 , wherein, on the eighth day that the bupropion and the dextromethorphan are co-administered, the AUC 0-inf of dextromethorphan is at least about 20 times the AUC 0-inf of dextromethorphan that would result from administering the same amount of the dextromethorphan without the bupropion for eight consecutive days.

Assignments (1)
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Feb 9, 2021
From: TABUTEAU, HERRIOT
To: ANTECIP BIOVENTURES II LLC
Reel/Frame 055189/0032 →