# US 2022/0031691 A9 · Bupropion as a modulator of drug activity

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- Number: US 2022/0031691 A9
- Document ID: US20220031691A9
- Status: Published application
- Kind: A9
- Application number: 16/950,838
- Filed: 2020-11-17
- Published: 2022-02-03
- Earliest claimed: 2013-11-05
- Assignees: Antecip Bioventures II LLC
- Applicants: Antecip Bioventures II LLC
- Inventors: Herriot Tabuteau
- Web page: https://patentgrep.com/patent/US20220031691A9

## CPC

- A61K 31/485: Morphinan derivatives, e.g. morphine, codeine
- A61K 9/0053: {Mouth and digestive tract, i.e. intraoral and peroral administration}
- A61K 31/135: having aromatic rings {, e.g. ketamine, nortriptyline (methadone A61K31/137)}
- A61K 31/137: Arylalkylamines, e.g. amphetamine, epinephrine, salbutamol, ephedrine {or methadone}
- A61K 31/15: Oximes (>C=N—O—); Hydrazines (>N—N<); Hydrazones (>N—N=) {; Imines (C—N=C)}
- A61K 31/343: condensed with a carbocyclic ring, e.g. coumaran, bufuralol, befunolol, clobenfurol, amiodarone
- A61K 31/381: having five-membered rings
- 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)

## 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 treatment resistant depression, comprising administering a drug combination once a day or twice a day to a human being in need thereof for at least 8 consecutive days, wherein the human being is an extensive metabolizer of dextromethorphan or an intermediate metabolizer of dextromethorphan, wherein the drug combination comprises: about 100 mg to about 110 mg of bupropion hydrochloride, or a molar equivalent amount of a bupropion in the free base form or another salt form; and about 40 mg to about 50 mg of dextromethorphan hydrobromide, or a molar equivalent amount of a dextromethorphan in the free base form or another salt form; wherein the drug combination is orally administered in a single dosage form comprising the bupropion and the dextromethorphan as the only therapeutically active compounds, which provides immediate release of dextromethorphan and sustained release of bupropion; and wherein the method results in the human being experiencing a therapeutic effect.

### Claim 2 (depends on 1)

The method of claim 1, wherein after orally administering the dosage form, the human being experiences an improvement in a depressive symptom as compared to baseline.

### Claim 3 (depends on 1)

The method of claim 1, wherein orally administering the dosage form is more effective in treating treatment resistant depression than orally administering a placebo.

### Claim 4 (depends on 1)

The method of claim 1, wherein orally administering the dosage form is more effective in treating treatment resistant depression than orally administering the same amount of the dextromethorphan alone.

### Claim 5 (depends on 1)

The method of claim 1, wherein the dosage form is orally administered once daily.

### Claim 6 (depends on 1)

The method of claim 1, wherein the dosage form is orally administered twice daily.

### Claim 7 (depends on 1)

The method of claim 1, wherein the dosage form is orally administered for at least 14 consecutive days.

### Claim 8 (depends on 1)

The method of claim 1, wherein the dosage form is orally administered for at least 30 consecutive days.

### Claim 9 (depends on 1)

The method of claim 1, wherein the dosage form has a weight ratio of the dextromethorphan to the bupropion that is about 0.3 to about 0.5.

### Claim 10 (depends on 1)

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

### Claim 11 (depends on 1)

The method of claim 1, wherein the dosage form is orally administered once a day for 2 days and twice a day thereafter.

### Claim 12 (depends on 1)

The method of claim 1, wherein the dosage form is orally administered once a day for 3 days and twice a day thereafter.

### Claim 13 (depends on 1)

The method of claim 1, wherein orally administering the dosage form is more effective than orally administering a placebo in reducing anxiety.

### Claim 14 (depends on 1)

The method of claim 1, wherein orally administering the dosage form is more effective than orally administering a placebo in improving concentration, reducing mental slowing, or a combination thereof.

### Claim 15 (depends on 1)

The method of claim 1, wherein orally administering the dosage form is more effective than orally administering a placebo in improving mood, reducing feelings of intense sadness, reducing despair, reducing pessimistic worry, or a combination thereof.

### Claim 16 (depends on 1)

The method of claim 1, wherein orally administering the dosage form is more effective than orally administering a placebo in reducing agitation, irritability, restlessness, or a combination thereof.

### Claim 17 (depends on 1)

The method of claim 1, wherein orally administering the dosage form is more effective than orally administering a placebo in reducing guilt, feelings of worthlessness, self-deprecation, or a combination thereof.

### Claim 18 (depends on 1)

The method of claim 1, wherein orally administering the dosage form is more effective than orally administering a placebo in reducing anger, reckless behavior, suicidal thoughts or attempts, or a combination thereof.

### Claim 19 (depends on 1)

The method of claim 1, wherein orally administering the dosage form is more effective than orally administering a placebo in reducing insomnia.

### Claim 20 (depends on 1)

The method of claim 1, wherein orally administering the dosage form is more effective than orally administering a placebo in reducing anorexia, appetite loss, weight loss, or a combination thereof.

### Claim 21 (depends on 1)

The method of claim 1, wherein orally administering the dosage form is more effective than orally administering a placebo in reducing weight gain.

### Claim 22 (depends on 1)

The method of claim 1, wherein orally administering the dosage form is more effective than orally administering a placebo in reducing decreased energy, fatigue, decreased libido, or a combination thereof.

### Claim 23 (depends on 1)

The method of claim 1, wherein orally administering the dosage form is more effective than orally administering a placebo in reducing aches, pains, headaches, cramps, or a combination thereof.

### Claim 24 (depends on 1)

The method of claim 1, wherein orally administering the dosage form is more effective than orally administering a placebo in reducing digestive issues.

### Claim 25 (depends on 1)

The method of claim 1, wherein orally administering the dosage form is more effective than orally administering a placebo in reducing abnormal hormonal circadian rhythms.
