Oral Extended-Release Ketamine Tablet for Reduced Dissociation

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Solution Overview

Problem

Existing treatments for treatment-resistant depression and anxiety disorders, such as injected ketamine, are associated with dissociative symptoms and require frequent administration, which can be inconvenient and time-consuming.

Innovation Solution

Development of an oral, extended-release ketamine tablet using a hydrophilic polymeric matrix, primarily polyethylene oxide, to provide a controlled release profile minimizing dissociative side effects while ensuring rapid treatment response.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Speed

If intravenous ketamine is administered, then rapid antidepressant effect is achieved, but dissociative side effects and increased heart rate/blood pressure occur

Engineering Contradiction:

Improveonset speed of antidepressant effectVSAvoiddissociative side effects and cardiovascular effects

Core Design Contradiction:

SpeedVSObject-affected harmful factors

Solution Approach 1:

The patent segments the rapid release of ketamine into controlled portions over time using a hydrophilic polymeric matrix. The matrix structure divides the drug release process into multiple phases, allowing therapeutic effects to occur while avoiding peak concentrations that cause dissociative side effects.

Inventive Principle:

Principle #1Segmentation

Solution Approach 2:

The patent implements periodic action through extended-release formulation that delivers ketamine at controlled intervals over 10-12 hours. This periodic release pattern maintains therapeutic blood levels while avoiding the continuous high concentration that produces adverse effects.

Inventive Principle:

Principle #19Periodic action

2Ease of operation

If oral ketamine formulation is developed, then patient comfort and ease of administration are improved, but drug absorption and efficacy may be reduced

Engineering Contradiction:

Improveease of administrationVSAvoiddrug absorption reliability

Core Design Contradiction:

Ease of operationVSReliability

Solution Approach 1:

The patent uses composite materials by combining ketamine with a hydrophilic polymeric matrix system. This composite formulation ensures reliable oral absorption while maintaining the drug's therapeutic properties, bridging the gap between ease of administration and absorption reliability.

Inventive Principle:

Principle #40Composite materials

Solution Approach 2:

The patent applies parameter changes by modifying the physical and chemical properties of ketamine through the polymeric matrix system. This changes the release kinetics and absorption characteristics, ensuring reliable oral bioavailability while maintaining therapeutic efficacy.

Inventive Principle:

Principle #35Parameter changes

3Strength

If high concentration of PEO is used in tablet formulation, then tablet hardness and crush resistance are improved, but drug release rate may be reduced

Engineering Contradiction:

Improvetablet hardnessVSAvoiddrug release rate

Core Design Contradiction:

StrengthVSSpeed

Solution Approach 1:

The patent applies dynamics by creating a time-dependent release system where the PEO matrix progressively hydrates and swells over time. This dynamic process allows the tablet to maintain high hardness initially while gradually increasing drug release rate as the matrix hydrates, achieving both strength and controlled release.

Inventive Principle:

Principle #15Dynamics

Solution Approach 2:

The patent utilizes phase transitions of the hydrophilic PEO matrix as it transitions from dry solid to hydrated gel state. This phase transition enables the tablet to maintain structural integrity while progressively releasing the drug, balancing hardness and release rate.

Inventive Principle:

Principle #36Phase transitions

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 tablet achieves a rapid treatment response with minimal dissociative side effects and allows for convenient once or twice-daily administration, effectively alleviating symptoms of treatment-resistant depression and anxiety disorders over several days.

Implementation Method 1

a therapeutically effective amount of an active agent selected from the group consisting of ketamine, norketamine, pharmaceutically acceptable salts thereof, and combinations thereof; ii) at least one high molecular weight polyethylene oxide (PEO) that is cured

Methodology Applied

Scientific EffectHydrophilic polymer dissolution:

Implementation Method 2

provides a prolonged release profile to minimize dissociative side effects while maintaining rapid treatment response

Methodology Applied

Scientific EffectDrug diffusion through polymer matrix: Diffusion

Implementation Method 3

a coating on said core, wherein said tablet is crush resistant and has a breaking strength of at least about 200 N

Methodology Applied

Scientific EffectPhysical barrier protection: Physical Containment

Data Source

PatentUS12611386B2Extended release pharmaceutical formulation

Publication Date: 2026.04.28 DOUGLAS PHARMA

AI summary

The disclosure provides a dosing regimen utilizing an oral extended release formulation for the treatment of treatment-resistant depression and treatment-resistant anxiety.