Ketamine Transdermal Patch Using Hydroxyl Adhesive
Find Innovative SolutionsGenerate Solutions
Solution Overview
Problem
Transdermal therapeutic systems (TTS) for ketamine administration face challenges in achieving optimal active ingredient flux and utilization, stability, and simplicity in design and production, particularly due to limitations in molecular transport through the skin and the need for crystallization inhibitors.
Innovation Solution
A TTS design featuring a backing layer impermeable to the active ingredient and a matrix layer with a pressure-sensitive adhesive containing free hydroxyl groups, which includes ketamine or its pharmaceutically acceptable salt, optimizing flux and stability without the use of crystallization inhibitors and crosslinking agents, and incorporating penetration enhancers for enhanced skin permeation.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Stability of the object's composition
If a pressure sensitive adhesive comprising free carboxyl groups and crystallization inhibitors is used (prior art), then the ketamine can be stabilized, but the flux of active ingredient and utilization of ketamine in the matrix layer are suboptimal
Solution Approach 1:
The patent changes the chemical parameter of the adhesive from free carboxyl groups to free hydroxyl groups. This parameter change fundamentally alters the interaction with ketamine, enabling both high stability and high flux without requiring crystallization inhibitors. The hydroxyl groups provide a different molecular environment that maintains ketamine in a stable amorphous state while optimizing its transdermal flux.
Solution Approach 2:
The patent extracts and eliminates the crystallization inhibitors from the formulation. By using adhesives with free hydroxyl groups instead of free carboxyl groups, the system achieves stability without these additional components, simplifying the formulation and removing potential sources of suboptimal flux associated with inhibitor presence.
2Stability of the object's composition
If crystallization inhibitors are used to stabilize ketamine, then the ketamine remains stable, but the design and production become more complex
Solution Approach 1:
The patent removes crystallization inhibitors from the formulation by using adhesives with free hydroxyl groups. This extraction of unnecessary components simplifies the design and production process while maintaining ketamine stability, directly addressing the complexity issue.
Solution Approach 2:
By changing the adhesive chemistry from carboxyl-based to hydroxyl-based, the patent eliminates the need for crystallization inhibitors, thereby simplifying the overall system design and production without compromising stability.
3Productivity
If the molecular transport of ingredients via the skin is enhanced, then the flux of active ingredient increases, but the stability of ketamine may be compromised
Solution Approach 1:
The patent changes the fundamental chemical parameter of the adhesive matrix from carboxyl groups to hydroxyl groups. This parameter change creates a unique environment that simultaneously optimizes both flux and stability, resolving the typical trade-off between these two parameters.
Solution Approach 2:
The patent uses a composite approach by combining the pressure sensitive adhesive with free hydroxyl groups and ketamine in a specific formulation. This composite material system achieves synergistic effects where the hydroxyl-containing adhesive provides both the necessary flux enhancement and stability maintenance.
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 solution achieves a high and sustained flux of ketamine, optimal utilization, and chemical and physical stability, with improved skin tolerance and adhesive strength, while maintaining a simple and economically advantageous production process.
Implementation Method 1
the molecular transport of ingredients via the skin poses a limiting factor
Implementation Method 2
The at least one pressure sensitive adhesive comprises free hydroxyl groups
Implementation Method 3
a backing layer which is not permeable for the active ingredient
Data Source
AI summary
The present invention concerns a transdermal therapeutic system, comprising a backing layer, which is not permeable for the active ingredient, and a matrix layer on one side of the backing layer, wherein the matrix layer contains at least one pressure sensitive adhesive and ketamine or a pharmaceutically acceptable salt or solvate thereof, wherein the at least one pressure sensitive adhesive has free hydroxyl groups, as well as its use as medicament, in particular for the treatment of depression and pain.