Oral Ketamine Tablet Extended Release Matrix
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Solution Overview
Problem
Current treatments for treatment-resistant depression (TRD) and anxiety disorders, such as Post-Traumatic Stress Disorder (PTSD), Obsessive Compulsive Disorder (OCD), Generalized Anxiety Disorder (GAD), and Social Anxiety Disorder, using injected ketamine are limited by significant side effects like dissociative symptoms and require invasive administration methods.
Innovation Solution
Development of an oral, extended-release ketamine tablet formulation using a hydrophilic polyethylene oxide matrix that provides a prolonged release profile, minimizing dissociative symptoms and improving administration convenience, with a coating that enhances tablet hardness and stability, allowing for once or twice-daily dosing without significant side effects.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Speed
If injected ketamine is used to treat treatment-resistant depression and anxiety disorders, then rapid antidepressant effects are achieved, but dissociative symptoms and cardiovascular side effects occur
Solution Approach 1:
The patent segments the rapid onset effect from the harmful side effects by using an extended-release formulation that delivers ketamine gradually over time. The composition includes ketamine combined with a fast-absorbing carrier (such as benzyl alcohol, ethanol, or propylene glycol) that enables rapid initial absorption for quick therapeutic effect, while the extended-release mechanism prevents the sudden high peak concentrations that cause dissociative symptoms and cardiovascular side effects.
Solution Approach 2:
The patent changes the pharmacokinetic parameters of ketamine delivery by using an extended-release formulation with specific absorption characteristics. The composition is designed to achieve a rapid initial absorption phase followed by a prolonged release phase, maintaining ketamine levels in a therapeutic window that avoids the harmful effects associated with high peak concentrations while preserving the rapid onset of antidepressant activity.
2Reliability
If injected ketamine is administered, then antidepressant effects are achieved, but invasive administration and time-consuming procedures are required
Solution Approach 1:
The patent replaces the mechanical injection system with an oral administration system. Instead of using needles and syringes for intravenous or intramuscular injection, the invention delivers ketamine through an oral composition that is absorbed rapidly into the bloodstream, eliminating the need for invasive procedures and making administration as simple as taking a pill or liquid formulation.
3Reliability
If standard ketamine formulations are used, then therapeutic effects are achieved, but abuse potential and dissociative symptoms increase
Solution Approach 1:
The patent applies dynamic delivery by designing an extended-release formulation that adjusts ketamine release over time. The composition provides a rapid initial absorption phase for immediate therapeutic effect, followed by a controlled prolonged release phase that maintains therapeutic levels while avoiding the sudden high concentrations that produce dissociative symptoms and increase abuse potential. This dynamic release profile optimizes the therapeutic window and minimizes harmful effects.
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 oral ketamine tablet formulation effectively treats TRD and anxiety disorders with reduced side effects, providing sustained antidepressant and anxiolytic effects for several days with minimal dissociative symptoms, and can be administered orally, offering improved patient convenience and tolerability compared to injected ketamine.
Implementation Method 1
The formulation demonstrated linear in vitro dissolution over 10-12 hours. Elimination half-life estimates for ketamine and norketamine for this formulation are much longer that previously reported for tablets.
Implementation Method 2
tablets formulations based on a high concentration of PEO are able to be annealed (heated) to give tablets of very high hardness that are resistant to crushing.
Data Source
AI summary
The invention provides an oral extended release formulation for the treatment of treatment-resistant depression and treatment-resistant anxiety.