# US 2025/0367142 A1 · Bupropion as a modulator of drug activity

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- Number: US 2025/0367142 A1
- Document ID: US20250367142A1
- Status: Published application
- Kind: A1
- Application number: 19/308,044
- Filed: 2025-08-22
- Published: 2025-12-04
- Earliest claimed: 2013-11-05
- Assignees: Antecip Bioventures II LLC
- Applicants: Antecip Bioventures II LLC
- Inventors: Herriot Tabuteau
- Web page: https://patentgrep.com/patent/US20250367142A1

## CPC

- A61K 31/138: Aryloxyalkylamines, e.g. propranolol, tamoxifen, phenoxybenzamine (atenolol A61K31/165; pindolol A61K31/404; timolol A61K31/5377)
- A61K 9/0053: {Mouth and digestive tract, i.e. intraoral and peroral administration}
- A61K 31/137: Arylalkylamines, e.g. amphetamine, epinephrine, salbutamol, ephedrine {or methadone}
- A61K 31/485: Morphinan derivatives, e.g. morphine, codeine
- A61P 25/24: Antidepressants
- A61K 9/2054: {Cellulose; Cellulose derivatives, e.g. hydroxypropyl methylcellulose}
- 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

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

### Claim 1

A method of treating nicotine addiction associated with smoking tobacco comprising administering a combination of a therapeutically effective amount of bupropion, or a pharmaceutically acceptable salt thereof, and a therapeutically effective amount of dextromethorphan, or a pharmaceutically acceptable salt thereof, daily for at least 21 consecutive days to a person suffering from nicotine addiction, wherein the person is an ad-lib tobacco smoker, wherein the combination is in a single dosage form and there are no other therapeutically active agents in the dosage form, wherein the dosage form is administered to the person once daily for three days, followed by twice daily, and wherein the method is more effective than administering the same amount of bupropion, or a pharmaceutically acceptable salt thereof, alone.

### Claim 2 (depends on 1)

The method of claim 1, wherein the combination of bupropion, or a pharmaceutically acceptable salt thereof, and dextromethorphan, or a pharmaceutically acceptable salt thereof, is administered to the person daily for at least 42 consecutive days.

### Claim 3 (depends on 1)

The method of claim 1, wherein the bupropion is in a salt form.

### Claim 4 (depends on 1)

The method of claim 1, wherein the bupropion is bupropion hydrochloride.

### Claim 5 (depends on 1)

The method of claim 1, wherein the dextromethorphan is in a salt form.

### Claim 6 (depends on 1)

The method of claim 1, wherein the dextromethorphan is dextromethorphan hydrobromide.

### Claim 7 (depends on 4)

The method of claim 4, wherein the therapeutically effective amount of bupropion hydrochloride is about 105 mg.

### Claim 8 (depends on 1)

The method of claim 1, wherein the weight ratio of dextromethorphan, or a pharmaceutically acceptable salt thereof, to bupropion, or a pharmaceutically acceptable salt thereof, is about 0.1 to about 0.5.

### Claim 9 (depends on 1)

The method of claim 1, wherein the weight ratio of dextromethorphan, or a pharmaceutically acceptable salt thereof, to bupropion, or a pharmaceutically acceptable salt thereof, is about 0.4 to about 0.5.

### Claim 10 (depends on 1)

The method of claim 1, wherein, to the person addicted to nicotine, the method is more effective than administering dextromethorphan, or a pharmaceutically acceptable salt thereof, alone.

### Claim 11 (depends on 4)

The method of claim 4, wherein about 105 mg of bupropion hydrochloride is administered to the person once daily for three days, followed by administering 105 mg of bupropion hydrochloride twice daily to the person for at least 21 days.

### Claim 12 (depends on 11)

The method of claim 11, wherein, to the person addicted to nicotine, the method is more effective, as measured on day 24 of treatment, than a control method, wherein the control method consists of administering 105 mg of bupropion hydrochloride alone to the person once daily for three days, followed by administering 105 mg of bupropion hydrochloride alone twice daily to the person for 21 days.

### Claim 13 (depends on 4)

The method of claim 4, wherein about 105 mg of bupropion hydrochloride is administered to the person once daily for three days, followed by administering 105 mg of bupropion hydrochloride twice daily to the person for at least 39 days.

### Claim 14 (depends on 13)

The method of claim 13, wherein, to the person addicted to nicotine, the method is more effective, as measured on day 42 of treatment, than a control method, wherein the control method consists of administering 105 mg of bupropion hydrochloride alone to the person once daily for three days, followed by administering 105 mg of bupropion hydrochloride alone twice daily to the person for 39 days.

### Claim 15 (depends on 1)

The method of claim 1, wherein bupropion, or a pharmaceutically acceptable salt thereof, has an enantiomeric excess of the R-enantiomer that is at least 90%.

### Claim 16 (depends on 1)

The method of claim 1, wherein bupropion, or a pharmaceutically acceptable salt thereof, has an enantiomeric excess of the S-enantiomer that is at least 90%.

### Claim 17 (depends on 1)

The method of claim 1, wherein bupropion, or a pharmaceutically acceptable salt thereof, is deuterium enriched.

### Claim 18 (depends on 1)

The method of claim 1, wherein dextromethorphan, or a pharmaceutically acceptable salt thereof, is deuterium enriched.

### Claim 19 (depends on 6)

The method of claim 6, wherein the therapeutically effective amount of dextromethorphan hydrobromide is about 45 mg.

### Claim 20

A method of treating nicotine addiction associated with smoking tobacco comprising administering a combination of about 105 mg bupropion hydrochloride and about 45 mg dextromethorphan hydrobromide daily for at least 21 consecutive days to a person suffering from nicotine addiction, wherein the person is an ad lib tobacco smoker, wherein the combination is in a single dosage form and there are no other therapeutically active agents in the dosage form, wherein the dosage form is administered to the person once daily for three days, followed by twice daily, and wherein the method is more effective than administering the same amount of the bupropion alone.
