IP Library Granted Patent US 10,695,304
Granted Patent B2
US 10,695,304 · App. 16/579,305 · Granted Jun 30, 2020

Dosage forms and methods for enantiomerically enriched or pure bupropion

Inventor: Herriot Tabuteau (New York, NY)
Assignee: AXSOME THERAPEUTICS, INC.
A61K31/137
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Quick Facts
Patent No.
US 10,695,304
App. No.
16/579,305
Granted
Jun 30, 2020
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 (AD/HD) comprising administering an (S)-bupropion to a human being in need thereof, wherein the (S)-bupropion is administered at a daily dose that is therapeutically effective for treating AD/HD and is about 1 mg to about 150 mg of at least 95% enantiomerically pure (S)-bupropion.

2. The method of claim 1 , wherein the human being has an age of about 18 years or less.

3. The method of claim 1 , wherein the (S)-bupropion is administered in a dosage form containing a binder.

4. The method of claim 1 , wherein the (S)-bupropion is administered in a dosage form containing an excipient.

5. The method of claim 1 , wherein the (S)-bupropion is administered in a dosage form containing a disintegrating agent.

6. The method of claim 1 , wherein the (S)-bupropion is administered in a dosage form containing a lubricant.

7. The method of claim 1 , wherein the method achieves a C max of (S)-bupropion in the human being that is at least about 60 ng/mL.

8. The method of claim 1 , wherein the method is effective in achieving a C max of (S)-bupropion that is at least 5-fold greater than the C max of (R)-bupropion that results from administering the same amount of (R)-bupropion to the human being.

9. The method of claim 1 , wherein the method achieves a C max of (R,R)-hydroxybupropion that is at least about 500 ng/mL in the human being.

10. The method of claim 1 , wherein the method is effective in achieving a C min of (R,R)-hydroxybupropion that is at least 3-fold greater than the C min of (R,R)-hydroxybupropion that results from administering the same amount of (R)-bupropion to the human being.

11. The method of claim 1 , wherein administering the (S)-bupropion results in (R,R)-hydroxybupropion that is at least 97% of the total amount of hydroxybupropion present in the plasma of the human being.

12. The method of claim 1 , wherein the (S)-bupropion is administered for at least 8 consecutive days.

13. The method of claim 1 , wherein the (S)-bupropion is administered for at least 14 consecutive days.

14. The method of claim 1 , wherein the (S)-bupropion is administered for at least 21 consecutive days.

15. 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.

16. 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.

17. The method of claim 1 , wherein the (S)-bupropion is orally administered in a dosage form that provides sustained release of the (S)-bupropion.

18. The method of claim 1 , wherein the method achieves a C max of (R,R)-hydroxybupropion in the human being that is at least about 600 ng/mL.

19. The method of claim 1 , wherein the method achieves an AUC 0-12 of (R,R)-hydroxybupropion in the human being that is at least about 7000 ng·hr/mL.

Assignments (4)
RELEASE OF SECURITY INTEREST Recorded May 22, 2025
From: HERCULES CAPITAL, INC.
To: AXSOME THERAPEUTICS, INC.
Reel/Frame 071337/0004 →
SECURITY INTEREST Recorded May 9, 2025
From: AXSOME THERAPEUTICS, INC.; AXSOME MALTA LTD.
To: WILMINGTON TRUST, NATIONAL ASSOCIATION
Reel/Frame 071247/0836 →
INTELLECTUAL PROPERTY SECURITY AGREEMENT Recorded Sep 25, 2020
From: AXSOME THERAPEUTICS, INC.
To: HERCULES CAPITAL, INC., AS AGENT
Reel/Frame 053941/0491 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Nov 5, 2019
From: TABUTEAU, HERRIOT
To: AXSOME THERAPEUTICS, INC.
Reel/Frame 050922/0607 →
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