Bupropion Modulation of Dextromethorphan Metabolism in Extensive Metabolizers

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Solution Overview

Problem

Existing methods fail to effectively increase dextromethorphan plasma levels and reduce adverse events or metabolic breakdown in human beings, particularly in extensive metabolizers, leading to inefficiencies and side effects.

Innovation Solution

Co-administration of bupropion, hydroxybupropion, erythrohydroxybupropion, or threohydroxybupropion, or their prodrugs, with dextromethorphan to inhibit metabolism and enhance plasma levels, thereby reducing dextrorphan levels and improving therapeutic efficacy.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Quantity of substance

If dextromethorphan is administered alone to extensive metabolizers, then the drug is rapidly metabolized, but plasma levels decrease and therapeutic efficacy is reduced

Engineering Contradiction:

Improvedextromethorphan plasma levelVSAvoidmetabolic breakdown rate

Core Design Contradiction:

Quantity of substanceVSProductivity

Solution Approach 1:

Bupropion is introduced as an intermediary substance that inhibits the metabolism of dextromethorphan. By co-administering bupropion with dextromethorphan, the metabolic breakdown of dextromethorphan is inhibited, thereby increasing and maintaining dextromethorphan plasma levels in extensive metabolizers.

Inventive Principle:

Principle #24Intermediary (Mediator)

2Reliability

If dextromethorphan plasma levels are increased to improve therapeutic efficacy, then adverse events and side effects increase

Engineering Contradiction:

Improvetherapeutic efficacyVSAvoidadverse events

Core Design Contradiction:

ReliabilityVSObject-affected harmful factors

Solution Approach 1:

The pharmacokinetic parameters of dextromethorphan are modified by changing the metabolic environment through bupropion co-administration. This changes the plasma concentration-time profile of dextromethorphan, achieving therapeutic efficacy while controlling adverse events through optimized drug levels.

Inventive Principle:

Principle #35Parameter changes

3Duration of action of moving object

If dextromethorphan is administered multiple times to maintain therapeutic levels, then the frequency of administration increases, but this leads to accumulation of adverse effects

Engineering Contradiction:

Improveduration of therapeutic effectVSAvoidaccumulation of adverse effects

Core Design Contradiction:

Duration of action of moving objectVSObject-generated harmful factors

Solution Approach 1:

Bupropion provides continuous inhibition of dextromethorphan metabolism, allowing for fewer administration doses while maintaining stable plasma levels. This continuous metabolic inhibition extends the duration of therapeutic effect and reduces the frequency of dosing, thereby minimizing accumulation of adverse effects.

Inventive Principle:

Principle #20Continuity of useful action

Applied Scientific Principles

This section explains which scientific principles are used to turn an abstract innovation direction into a practical engineering solution.

Function Achieved in This Case

The co-administration significantly increases dextromethorphan plasma levels, decreases metabolic breakdown, and reduces adverse events, providing sustained therapeutic effects and improved treatment outcomes.

Implementation Method 1

Co-administration of bupropion, hydroxybupropion, erythrohydroxybupropion, or threohydroxybupropion, or their prodrugs, with dextromethorphan to inhibit metabolism and enhance plasma levels

Methodology Applied

Scientific EffectMetabolic inhibition:

Implementation Method 2

The co-administration significantly increases dextromethorphan plasma levels, decreases metabolic breakdown, and reduces adverse events

Methodology Applied

Scientific EffectMetabolic breakdown: Decomposition (biological)

Data Source

PatentUS20250345294A1Bupropion as a modulator of drug activity

Publication Date: 2025.11.13 ANTECIP BIOVENTURES II LLC

AI summary

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.