Extended-Release Ketamine Tablet With PEO Matrix for Lower Side Effects

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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 with high molecular weight 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 ketamine's release profile. The matrix acts as a mediator between the drug and the patient's body, controlling the rate and pattern of drug release to achieve rapid therapeutic effects while minimizing peak-related side effects.

Inventive Principle:

Principle #24Intermediary (Mediator)

Solution Approach 2:

The patent implements periodic action through its multi-phase release mechanism that delivers ketamine in controlled bursts or phases rather than as a single peak. This allows the drug to maintain therapeutic levels while reducing the intensity and duration of peak concentrations that cause dissociative symptoms.

Inventive Principle:

Principle #19Periodic action

2Reliability

If injected ketamine is administered frequently to maintain therapeutic effect, then treatment efficacy is maintained, but administration burden and time consumption increase

Engineering Contradiction:

Improvemaintenance of therapeutic effectVSAvoidtime consumption for frequent administration

Core Design Contradiction:

ReliabilityVSLoss of time

Solution Approach 1:

The patent achieves continuity of useful action through its extended-release formulation that maintains therapeutic ketamine levels in the body over an extended period. The hydrophilic polymeric matrix continuously releases the drug, eliminating the need for frequent re-administration and maintaining reliable therapeutic effects throughout the day.

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 achieving prolonged release profile becomes challenging

Engineering Contradiction:

Improvedissociative symptomsVSAvoidformulation complexity for prolonged release

Core Design Contradiction:

Object-affected harmful factorsVSDevice complexity

Solution Approach 1:

The patent applies parameter changes by systematically varying the composition, molecular weight, and crosslinking density of the hydrophilic polymeric matrix to optimize release kinetics. By adjusting these parameters, the formulation achieves prolonged release while maintaining manufacturability and avoiding excessive complexity.

Inventive Principle:

Principle #35Parameter changes

Solution Approach 2:

The patent uses composite materials by combining ketamine with a hydrophilic polymeric matrix that exhibits specific rheological properties. This composite formulation leverages the synergistic interactions between the drug and polymer to achieve controlled release, utilizing the polymer's water solubility and swellability characteristics for prolonged drug delivery.

Inventive Principle:

Principle #40Composite materials

4Duration of action of moving object

If high molecular weight PEO is used to create extended release profile, then release duration is extended, but tablet hardness and crush resistance may be compromised

Engineering Contradiction:

Improverelease duration of ketamineVSAvoidtablet hardness and crush resistance

Core Design Contradiction:

Duration of action of moving objectVSStrength

Solution Approach 1:

The patent applies local quality by creating distinct regions within the tablet with different functional properties. The hydrophilic polymeric matrix provides the extended-release function in specific areas, while other components or structural features provide mechanical strength and crush resistance, allowing each region to optimize its specific function without compromising the other.

Inventive Principle:

Principle #3Local quality

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 therapeutic effect with reduced side effects and allows for once or twice-daily administration, providing sustained relief for treatment-resistant depression and anxiety disorders over several days.

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 EffectDiffusion: Diffusion