# US 12,109,178 B2 · Bupropion as a modulator of drug activity

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- Number: US 12,109,178 B2
- Document ID: US12109178B2
- Status: Granted
- Kind: B2
- Application number: 17/821,342
- Filed: 2022-08-22
- Published: 2023-02-09
- Granted: 2024-10-08
- Earliest claimed: 2013-11-05
- Assignees: Antecip Bioventures II LLC
- Applicants: Antecip Bioventures II LLC
- Inventors: Herriot Tabuteau
- Web page: https://patentgrep.com/patent/US12109178B2

## CPC

- A61K 9/2054: {Cellulose; Cellulose derivatives, e.g. hydroxypropyl methylcellulose}
- 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: 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 major depressive disorder, comprising orally administering a dosage form once a day or twice a day to a human patient in need thereof, wherein the dosage form contains about 40 mg to about 50 mg of a dextromethorphan salt, or a molar equivalent amount of the free base form of dextromethorphan, and about 100 mg to about 110 mg of bupropion hydrochloride, or a molar equivalent amount of another salt form or the free base form of bupropion.

### Claim 2 (depends on 1)

The method of claim 1, wherein the dosage form contains about 45 mg of the dextromethorphan salt.

### Claim 3 (depends on 1)

The method of claim 1, wherein the dosage form is orally administered once a day for three days, and after three days, the dosage form is orally administered twice a day.

### Claim 4 (depends on 1)

The method of claim 1, wherein the dosage form contains about 105 mg of bupropion hydrochloride.

### Claim 5 (depends on 4)

The method of claim 4, wherein the dosage form contains about 45 mg of the dextromethorphan salt.

### Claim 6 (depends on 5)

The method of claim 5, wherein the dosage form is orally administered once a day for three days, and after three days, the dosage form is orally administered twice a day.

### Claim 7 (depends on 6)

The method of claim 6, wherein the dosage form provides sustained release of bupropion and immediate release of dextromethorphan.

### Claim 8 (depends on 7)

The method of claim 7, wherein the dosage form is in the form of a tablet.

### Claim 9 (depends on 8)

The method of claim 8, wherein the tablet further contains magnesium stearate.

### Claim 10 (depends on 9)

The method of claim 9, wherein the tablet further contains microcrystalline cellulose.

### Claim 11 (depends on 1)

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

### Claim 12 (depends on 11)

The method of claim 11, wherein the dosage form contains about 45 mg of dextromethorphan hydrobromide.

### Claim 13 (depends on 12)

The method of claim 12, wherein the dosage form contains about 105 mg of bupropion hydrochloride.

### Claim 14 (depends on 13)

The method of claim 13, wherein the dosage form is orally administered once a day for three days, and after three days, the dosage form is orally administered twice a day.

### Claim 15 (depends on 14)

The method of claim 14, wherein the dosage form provides sustained release of bupropion and immediate release of dextromethorphan.

### Claim 16 (depends on 15)

The method of claim 15, wherein the dosage form is in the form of a tablet.

### Claim 17 (depends on 16)

The method of claim 16, wherein the tablet further contains magnesium stearate.

### Claim 18 (depends on 17)

The method of claim 17, wherein the tablet further contains microcrystalline cellulose.