Dextromethorphan-Bupropion Combination for Sustained Plasma Exposure

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Solution Overview

Problem

Existing treatments with dextromethorphan are limited by rapid metabolism, leading to short plasma half-life and adverse events, particularly in extensive metabolizers, and require frequent dosing to maintain efficacy.

Innovation Solution

Co-administration of bupropion, hydroxybupropion, erythrohydroxybupropion, or threohydroxybupropion with dextromethorphan to inhibit metabolism, increase plasma levels, and reduce adverse events, using sustained release delivery systems and varying administration schedules.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Duration of action of moving object

If dextromethorphan is administered alone, then it provides initial therapeutic effect, but rapid metabolism causes short plasma half-life and requires frequent dosing

Engineering Contradiction:

Improveplasma half-life of dextromethorphanVSAvoiddosing frequency

Core Design Contradiction:

Duration of action of moving objectVSProductivity

Solution Approach 1:

The patent introduces bupropion and its metabolites (hydroxybupropion, erythrohydroxybupropion, threohydroxybupropion) as intermediary substances that inhibit the metabolism of dextromethorphan. These intermediaries block the enzymatic breakdown of dextromethorphan, thereby extending its plasma half-life from approximately 2-3 hours to 8-12 hours or longer, reducing dosing frequency from multiple times daily to once or twice daily.

Inventive Principle:

Principle #24Intermediary (Mediator)

2Reliability

If dextromethorphan is administered at higher doses to maintain efficacy, then therapeutic effect is improved, but adverse events increase

Engineering Contradiction:

Improvetherapeutic efficacyVSAvoidadverse events

Core Design Contradiction:

ReliabilityVSObject-affected harmful factors

Solution Approach 1:

The patent changes the pharmacokinetic parameters of dextromethorphan by co-administering metabolism-inhibiting agents. This shifts the concentration-time profile to maintain therapeutic levels (Cmax and AUC) within the effective range for a longer duration without requiring higher peak doses, thereby reducing adverse events associated with high concentrations while maintaining reliability of therapeutic effect.

Inventive Principle:

Principle #35Parameter changes

3Quantity of substance

If dextromethorphan is metabolized rapidly, then clearance is efficient, but plasma levels drop below therapeutic threshold quickly

Engineering Contradiction:

Improveplasma concentration of dextromethorphanVSAvoidtime above therapeutic threshold

Core Design Contradiction:

Quantity of substanceVSDuration of action of stationary object

Solution Approach 1:

The patent ensures continuous therapeutic action by inhibiting the metabolism of dextromethorphan. The metabolism-inhibiting agents maintain plasma concentrations above the therapeutic threshold continuously for extended periods (8-12 hours or more per dose), transforming the intermittent sub-therapeutic levels into sustained effective levels, thereby extending the duration of useful action without requiring frequent re-dosing.

Inventive Principle:

Principle #20Continuity of useful action

Data Source

PatentUS12576078B1Compounds and combinations thereof for treating neurological and psychiatric conditions

Publication Date: 2026.03.17 ANTECIP BIOVENTURES II LLC

AI summary

Dosage forms, drug delivery systems, and methods related to dextromethorphan or improved therapeutic effects are disclosed. Typically, an antidepressant, such as bupropion or a related compound is orally administered to a human being to be treated with, or being treated with, dextromethorphan.