Controlled-Release Oral Ketamine Dosage Forms for Dose Dumping Control

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Solution Overview

Problem

Existing oral formulations of ketamine fail to achieve satisfactory in vivo plasma levels and are prone to dose dumping and drug abuse, particularly when alcohol is consumed.

Innovation Solution

Development of a controlled release oral dosage form of ketamine that provides specific in vitro release profiles, minimizing dose dumping and drug abuse by using matrix-controlled, osmotic, and multi-particulate formulations.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Ease of operation

If oral formulations of ketamine are used, then the drug can be administered conveniently, but satisfactory in vivo plasma levels cannot be achieved

Engineering Contradiction:

Improveconvenience of administrationVSAvoidin vivo plasma level

Core Design Contradiction:

Ease of operationVSQuantity of substance

Solution Approach 1:

The patent modifies the release parameters of ketamine by using controlled-release formulations with specific dissolution profiles. The formulation controls the rate and extent of drug release to achieve therapeutic plasma levels while maintaining oral administration convenience.

Inventive Principle:

Principle #35Parameter changes

Solution Approach 2:

The patent employs composite formulation systems combining ketamine with controlled-release excipients and matrix materials. These composite materials enable sustained release profiles that maintain effective plasma concentrations over time while preserving oral dosing convenience.

Inventive Principle:

Principle #40Composite materials

2Ease of operation

If conventional oral formulations are used, then administration is simple, but dose dumping occurs when alcohol is consumed

Engineering Contradiction:

Improvesimplicity of administrationVSAvoidrelease control stability

Core Design Contradiction:

Ease of operationVSReliability

Solution Approach 1:

The controlled-release formulation is designed with preliminary protective measures against alcohol-induced dose dumping. The matrix structure and release-controlling excipients are selected to resist the disruptive effects of alcohol, maintaining reliable drug release even when alcohol is consumed.

Inventive Principle:

Principle #9Preliminary anti-action

Solution Approach 2:

The formulation parameters are specifically optimized to maintain release control stability in the presence of alcohol. This includes selecting excipients with appropriate hydrophobicity and cross-linking densities that prevent alcohol from accelerating drug release.

Inventive Principle:

Principle #35Parameter changes

3Device complexity

If conventional oral formulations are used, then the dosage form is simple, but drug abuse is facilitated

Engineering Contradiction:

Improvedosage form complexityVSAvoiddrug abuse risk

Core Design Contradiction:

Device complexityVSObject-affected harmful factors

Solution Approach 1:

The patent modifies the release parameters to prevent rapid absorption associated with abuse. The controlled-release profile with specific dissolution rates (e.g., Q60 between 10-40%) makes the drug less suitable for abuse while maintaining therapeutic efficacy, without significantly complicating the dosage form.

Inventive Principle:

Principle #35Parameter changes

4Reliability

If controlled release formulation is developed, then dose dumping is minimized, but formulation complexity increases

Engineering Contradiction:

Improverelease controlVSAvoidformulation complexity

Core Design Contradiction:

ReliabilityVSDevice complexity

Solution Approach 1:

The patent optimizes formulation parameters within practical ranges to achieve controlled release without excessive complexity. By selecting excipients and processing methods that balance performance and manufacturability, the formulation achieves reliable release control while remaining feasible for commercial production.

Inventive Principle:

Principle #35Parameter changes

Data Source

PatentUS12440456B2Method for treatment of depression with oral dosage forms of ketamine

Publication Date: 2025.10.14 KETABON GMBH

AI summary

The present invention relates to an oral dosage form for administration of ketamine and a method of preparing an oral dosage form for administration of ketamine, preferably once or twice a day.