IP Library Granted Patent US 12,156,914
Granted Patent B2
US 12,156,914 · App. 18/169,402 · Granted Dec 3, 2024

Pharmaceutical compositions comprising bupropion and cysteine

Inventor: Herriot Tabuteau (New York, NY)
Assignee: AXSOME THERAPEUTICS, INC.
A61K47/542A61K9/2009A61K9/2013A61K9/2054A61K9/209A61K31/485
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Quick Facts
Patent No.
US 12,156,914
App. No.
18/169,402
Granted
Dec 3, 2024
Kind
B2
Abstract

This disclosure relates to pharmaceutical compositions comprising bupropion and cysteine, and pharmaceutical dosage forms comprising bupropion and cysteine. The disclosure also relates to molecular complexes of bupropion and cysteine. These compositions and dosage forms may have improved stability of bupropion.

Claims (17)

1. A pharmaceutical dosage form comprising bupropion and cysteine, wherein the dosage form is a solid and comprises about 100 mg to about 120 mg of the bupropion in the free base form or a salt form, and about 50 mg to about 100 mg of cysteine in the neutral form or a salt form, and wherein the dosage form has a molar ratio of the bupropion to the cysteine that is about 0.5:1 to about 1.1:1.

2. The pharmaceutical dosage form of claim 1 , wherein the dosage form has a molar ratio of the bupropion to the cysteine that is about 0.7:1 to about 1.1:1.

3. The pharmaceutical dosage form of claim 1 , wherein the molar ratio of the bupropion to the cysteine is about 1:1.

4. The pharmaceutical dosage form of claim 1 , further comprising a sustained release polymer.

5. The pharmaceutical dosage form of claim 4 , wherein the sustained release polymer is an acrylate polymer or copolymer, a methylcellulose, or a combination thereof.

6. The pharmaceutical dosage form of claim 1 , which is in the form of a capsule, pill, or tablet.

7. A pharmaceutical dosage form comprising bupropion and cysteine, wherein the dosage form is a solid and comprises about 100 mg to about 120 mg of the bupropion in the free base form or a salt form, and about 50 mg to about 100 mg of the cysteine in the neutral form or a salt form, wherein the dosage form has a molar ratio of the bupropion to the cysteine that is about 0.5:1 to about 1.1:1, wherein the dosage form further comprises dextromethorphan, and wherein the dosage form contains bupropion and dextromethorphan, and no other therapeutically active agents.

8. The pharmaceutical dosage form of claim 7 , which is a bilayer dosage form, wherein the bupropion and the cysteine are in a first layer and the dextromethorphan is in a second layer.

9. The pharmaceutical dosage form of claim 1 , further comprising a filler.

10. The pharmaceutical dosage form of claim 9 , wherein the filler is microcrystalline cellulose.

11. The pharmaceutical dosage form of claim 1 , further comprising a lubricant.

12. The pharmaceutical dosage form of claim 11 , wherein the lubricant is magnesium stearate.

13. The pharmaceutical dosage form of claim 1 , wherein the cysteine is L-cysteine hydrochloride monohydrate.

14. The pharmaceutical dosage form of claim 1 , comprising a molecular complex of bupropion and cysteine.

15. The pharmaceutical dosage form of claim 1 , wherein the bupropion is more stable than bupropion alone.

16. The pharmaceutical composition of claim 14 , wherein the bupropion is more stable than bupropion alone.

17. The pharmaceutical dosage form of claim 1 , wherein the bupropion is bupropion hydrochloride.

Assignments (4)
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Mar 4, 2026
From: AXSOME THERAPEUTICS, INC.
To: ANTECIP BIOVENTURES II LLC
Reel/Frame 073973/0726 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Jul 25, 2025
From: AXSOME THERAPEUTICS, INC.
To: ANTECIP BIOVENTURES II LLC
Reel/Frame 071835/0738 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Dec 17, 2024
From: AXSOME THERAPEUTICS, INC.,
To: ANTECIP BIOVENTURES II LLC
Reel/Frame 069608/0054 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded May 3, 2023
From: TABUTEAU, HERRIOT
To: AXSOME THERAPEUTICS, INC.
Reel/Frame 063518/0458 →