# US 2021/0330613 A1 · Dosage forms and methods for enantiomerically enriched or pure bupropion

> Agents: this data is available as JSON from the patentgrep API and MCP server — see https://patentgrep.com/llms.txt

- Number: US 2021/0330613 A1
- Document ID: US20210330613A1
- Status: Published application
- Kind: A1
- Application number: 17/305,195
- Filed: 2021-07-01
- Published: 2021-10-28
- Earliest claimed: 2018-09-20
- Assignees: Axsome Therapeutics, Inc.
- Applicants: Axsome Therapeutics, Inc.
- Inventors: Herriot Tabuteau
- Web page: https://patentgrep.com/patent/US20210330613A1

## CPC

- A61K 31/137: Arylalkylamines, e.g. amphetamine, epinephrine, salbutamol, ephedrine {or methadone}
- A61P 25/14: for treating abnormal movements, e.g. chorea, dyskinesia
- A61P 25/28: for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
- A61K: PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES (devices or methods specially adapted for bringing pharmaceutical products into particular physical or administering forms A61J3/00; chemical aspects of, or use of materials for deodorisation of air, for disinfection or sterilisation, or for bandages, dressings, absorbent pads or surgical articles A61L; soap compositions C11D)
- A61P: SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS

## 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

### Claim 1

A method of treating Huntington's disease chorea, comprising:
orally administering a daily dose of an (S)-bupropion to a human being in need thereof, wherein the (S)-bupropion is not deuterium-enriched, wherein the daily dose of the (S)-bupropion is about 100 mg to about 300 mg;
wherein the (S)-bupropion is at least 95% enantiomerically pure, and no other bupropion is orally administered with the daily dose of the (S)-bupropion, wherein the (S)-bupropion is in a dosage form, and wherein the dosage form contains less than 0.1% of any dextromethorphan.

### Claim 2 (depends on 1)

The method of claim 1, wherein the (S)-bupropion is orally administered once daily.

### Claim 3 (depends on 1)

The method of claim 1, wherein the (S)-bupropion is orally administered in two doses per day, and wherein the sum of the two doses per day is the daily dose.

### Claim 4 (depends on 1)

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

### Claim 5 (depends on 1)

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

### Claim 6 (depends on 1)

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

### Claim 7 (depends on 1)

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

### Claim 8 (depends on 1)

The method of claim 1, wherein the method achieves an AUC0-12 of (S)-bupropion in the human being that is at least about 400 ng·hr/mL.

### Claim 9 (depends on 1)

The method of claim 1, wherein the method achieves an AUC0-12 of (S)-bupropion in the human being that is about 500 ng·hr/mL to about 900 ng·hr/mL.

### Claim 10 (depends on 1)

The method of claim 1, wherein the method achieves a Cmax of (S)-bupropion in the human being that is about 60 ng/mL to about 130 ng/mL.

### Claim 11 (depends on 1)

The method of claim 1, wherein the (S)-bupropion is in a dosage form, and wherein the dosage form is in a form of tablet, capsule, or syrup.

### Claim 12 (depends on 1)

The method of claim 1, wherein the (S)-bupropion is in a dosage form, and wherein the dosage form is a solid oral dosage form.

### Claim 13 (depends on 1)

The method of claim 1, wherein the (S)-bupropion is in a dosage form, and wherein the dosage form is orally administered to the human being under fasting conditions.

### Claim 14 (depends on 1)

The method of claim 1, wherein the (S)-bupropion is at least 97% enantiomerically pure.

### Claim 15 (depends on 1)

The method of claim 1, wherein the (S)-bupropion is at least 99% enantiomerically pure.

### Claim 16 (depends on 1)

The method of claim 1, wherein the (S)-bupropion is in a salt form.

### Claim 17 (depends on 1)

The method of claim 1, wherein the (S)-bupropion is in the free base form.

### Claim 18 (depends on 1)

The method of claim 1, which is effective in providing therapeutically effective plasma levels of (S)-bupropion.

### Claim 19 (depends on 1)

The method of claim 1, wherein orally administering the daily dose of the (S)-bupropion to the human being results in a reduction of adverse events associated with racemic bupropion.