IP Library Granted Patent US 11,660,274
Granted Patent B2
US 11,660,274 · App. 17/731,247 · Granted May 30, 2023

Dosage forms and methods for enantiomerically enriched or pure bupropion

Inventor: Herriot Tabuteau (New York, NY)
Assignee: AXSOME THERAPEUTICS, INC.
A61K31/137A61K9/0053
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Quick Facts
Patent No.
US 11,660,274
App. No.
17/731,247
Granted
May 30, 2023
Kind
B2
Abstract

This disclosure relates to dosage forms containing an enantiomerically enriched or pure bupropion such as enantiomeric excess of (S)-bupropion, enantiomerically enriched (S)-bupropion, or enantiomerically pure (S)-bupropion and methods of using these dosage forms. These dosage forms may be administered to human beings in a reduced amount as compared to the amount of racemic bupropion that would be administered in the same situation.

Claims (19)

1. A method of treating attention deficit/hyperactivity disorder in a human being comprising orally administering a dosage form containing (S)-bupropion that is at least 95% enantiomerically pure, one or two times per day, to the human being, wherein the (S)-bupropion is not deuterium-enriched, wherein the human being is in need of treatment with (S)-bupropion, wherein (R,R)-hydroxybupropion is at least 97% of the total amount of (R,R)-hydroxybupropion and (S,S)-hydroxybupropion present in the plasma of the human being, wherein a daily dose of the (S)-bupropion that is about 60 mg to about 180 mg is orally administered to the human being, wherein the method is effective in treating attention deficit/hyperactivity disorder, and wherein the dosage form contains no dextromethorphan, or contains less than 0.1% of dextromethorphan.

2. The method of claim 1 , wherein the dosage form is orally administered once daily.

3. The method of claim 2 , wherein the dosage form contains about 150 mg to about 180 mg of the (S)-bupropion.

4. The method of claim 1 , wherein the dosage form is orally administered twice daily.

5. The method of claim 4 , wherein the dosage form contains about 70 mg to about 80 mg of the (S)-bupropion.

6. The method of claim 1 , wherein the dosage form is orally administered for at least 8 consecutive days.

7. The method of claim 1 , wherein the dosage form is orally administered for at least 14 consecutive days.

8. The method of claim 1 , wherein the dosage form is orally administered for at least 21 consecutive days.

9. The method of claim 1 , wherein the dosage form is orally administered for at least 28 consecutive days.

10. The method of claim 1 , wherein the method achieves an AUC 0-12 of (S)-bupropion in the human being that is at least about 400 ng·hr/mL.

11. The method of claim 1 , wherein the method achieves an AUC 0-12 of (S)-bupropion in the human being that is about 500 ng·hr/mL to about 900 ng·hr/mL.

12. The method of claim 8 , wherein the method achieves a C max of (S)-bupropion in the human being that is about 60 ng/mL to about 140 ng/mL.

13. The method of claim 1 , wherein the dosage form provides sustained release of (S)-bupropion.

14. The method of claim 1 , wherein a daily dose of the (S)-bupropion that is about 60 mg to about 120 mg is orally administered to the human being.

15. The method of claim 1 , wherein a daily dose of the (S)-bupropion that is about 80 mg to about 150 mg is orally administered to the human being.

16. The method of claim 1 , wherein a daily dose of the (S)-bupropion that is about 100 mg to about 180 mg is orally administered to the human being.

17. The method of claim 1 , wherein a daily dose of the (S)-bupropion that is about 120 mg to about 180 mg is orally administered to the human being.

18. The method of claim 1 , wherein the dosage form contains no dextromethorphan.

19. The method of claim 1 , wherein the dosage form contains less than 0.1% of dextromethorphan.

Assignments (2)
SECURITY INTEREST Recorded May 9, 2025
From: AXSOME THERAPEUTICS, INC.; AXSOME MALTA LTD.
To: WILMINGTON TRUST, NATIONAL ASSOCIATION
Reel/Frame 071247/0836 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded May 5, 2022
From: TABUTEAU, HERRIOT
To: AXSOME THERAPEUTICS, INC.
Reel/Frame 059827/0177 →
Cited By (4)
US 12,599,576 US 12,653,795 US 12,661,408 US 12,678,506