Extended-Release Ketamine Tablet Using a PEO Matrix

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Solution Overview

Problem

Existing treatments for treatment-resistant depression and anxiety disorders, such as injected ketamine, are associated with significant side effects like dissociative symptoms and require frequent administration, which can be cumbersome.

Innovation Solution

Development of an oral, extended-release ketamine tablet using a hydrophilic polymeric matrix, primarily polyethylene oxide (PEO), to provide a prolonged release profile minimizing side effects and allowing for less frequent dosing.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Speed

If injected ketamine is used to treat treatment-resistant depression and anxiety disorders, then rapid onset antidepressant effects are achieved, but dissociative symptoms and cardiovascular side effects occur

Engineering Contradiction:

Improveonset speed of antidepressant effectVSAvoiddissociative symptoms and cardiovascular side effects

Core Design Contradiction:

SpeedVSObject-affected harmful factors

Solution Approach 1:

The patent uses a hydrophilic polymeric matrix as an intermediary delivery system that modifies the release kinetics of ketamine. The matrix acts as a mediator between the drug and the body, controlling the rate of release to avoid rapid absorption while maintaining therapeutic effectiveness. This resolves the contradiction by providing rapid onset through optimized release kinetics without the harmful effects of rapid intravenous administration.

Inventive Principle:

Principle #24Intermediary (Mediator)

Solution Approach 2:

The patent changes the physical and chemical parameters of ketamine delivery by using a hydrophilic polymeric matrix with specific molecular weights and compositions. By adjusting parameters such as polymer molecular weight, drug-polymer ratio, and matrix porosity, the system achieves controlled release that provides rapid antidepressant effects while minimizing dissociative symptoms and cardiovascular side effects.

Inventive Principle:

Principle #35Parameter changes

2Reliability

If injected ketamine is administered to achieve therapeutic effects, then antidepressant activity is achieved, but frequent administration is required which is cumbersome

Engineering Contradiction:

Improvetherapeutic effectivenessVSAvoidtime required for frequent administration

Core Design Contradiction:

ReliabilityVSLoss of time

Solution Approach 1:

The patent implements continuous release of ketamine through the hydrophilic polymeric matrix system. The matrix provides sustained release of the drug over an extended period, maintaining therapeutic levels continuously without requiring frequent dosing. This resolves the contradiction by ensuring reliable therapeutic effectiveness while eliminating the time loss associated with frequent administration.

Inventive Principle:

Principle #20Continuity of useful action

3Object-affected harmful factors

If oral ketamine formulation is developed to minimize side effects, then dissociative symptoms are reduced, but prolonged release profile is required for optimal effect

Engineering Contradiction:

Improvedissociative symptomsVSAvoidrelease duration of ketamine

Core Design Contradiction:

Object-affected harmful factorsVSDuration of action of moving object

Solution Approach 1:

The patent optimizes the physical and chemical parameters of the hydrophilic polymeric matrix to achieve the desired release profile. By selecting specific molecular weights of PEO (2 million to 7 million), adjusting the drug-polymer ratio, and controlling matrix porosity, the system achieves prolonged release that minimizes dissociative symptoms while maintaining therapeutic effectiveness throughout the dosing interval.

Inventive Principle:

Principle #35Parameter changes

4Strength

If high concentration of PEO is used to create hard crush-resistant tablets, then tablet durability is improved, but manufacturing complexity increases

Engineering Contradiction:

Improvetablet hardness and crush resistanceVSAvoidmanufacturing process simplicity

Core Design Contradiction:

StrengthVSEase of manufacture

Solution Approach 1:

The patent optimizes the concentration of PEO in the matrix to achieve the minimum necessary tablet hardness and crush resistance. By carefully controlling the drug-polymer ratio and using appropriate granulation and compression parameters, the system produces durable tablets that are resistant to crushing during handling and administration, while keeping the manufacturing process relatively simple and scalable.

Inventive Principle:

Principle #35Parameter changes

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 prolonged release of ketamine and norketamine, reducing side effects and enabling once or twice-daily administration, effectively treating treatment-resistant depression and anxiety disorders with improved patient compliance and reduced adverse reactions.

Implementation Method 1

a core comprising: i) 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 EffectPolymer matrix controlled release:

Implementation Method 2

The formulation demonstrated linear in vitro dissolution over 10-12 hours

Methodology Applied

Scientific EffectDiffusion: Diffusion

Implementation Method 3

using a hydrophilic polymeric matrix approach. Polyethylene oxide (PEO) is one of a number of hydrophilic polymers used in controlled drug delivery formulations

Methodology Applied

Scientific EffectErosion:

Data Source

PatentUS20260034065A1Extended release pharmaceutical formulation

Publication Date: 2026.02.05 DOUGLAS PHARMA

AI summary

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