Capsaicin Transdermal Patch Saturated Matrix Release
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Solution Overview
Problem
Existing transdermal patches with low-dose capsaicin do not achieve a consistent, prolonged release of the active ingredient over 4 to 24 hours, leading to variable pain-relieving effects.
Innovation Solution
A transdermal patch comprising a silicone matrix with capsaicin in a saturated solution and solid form, along with a liquid excipient that controls solubility, ensuring a uniform release of capsaicin with near zero-order kinetics for at least 4 to 12 hours.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Duration of action of moving object
If a transdermal patch uses low-dose capsaicin with traditional release mechanisms, then the patch structure is simpler, but the release of active ingredient is not consistent or prolonged
Solution Approach 1:
The patent changes the physical-chemical parameters of the capsaicin formulation by using a saturated solution combined with solid capsaicin particles. This parameter change enables the system to maintain constant release kinetics (near zero-order) over extended periods (4-24 hours), resolving the contradiction between prolonged duration and release consistency.
Solution Approach 2:
The patent employs a composite formulation consisting of capsaicin in saturated solution combined with solid capsaicin particles within the transdermal matrix. This composite structure provides both immediate availability (from solution) and sustained release (from solid particles dissolving), achieving consistent prolonged release without complex multilayer structures.
2Duration of action of moving object
If a transdermal patch uses multiple layers with increasing capsaicin concentrations to achieve prolonged release, then the release duration is extended, but the manufacturing complexity increases
Solution Approach 1:
Instead of varying concentration across multiple layers, the patent maintains uniform saturated solution concentration throughout the matrix and relies on the dissolution kinetics of solid particles to extend release duration. This approach achieves prolonged release (4-24 hours) while simplifying manufacturing, as it eliminates the need for precise concentration gradients and complex multilayer assembly.
Solution Approach 2:
The patent extracts the release-control function from the structural complexity of multiple layers and concentrates it in the phase distribution between saturated solution and solid particles. This extraction allows prolonged release to be achieved through a simpler single-layer structure with uniform composition.
3Reliability
If a transdermal patch uses a membrane-controlled system to achieve consistent release kinetics, then the release profile is more controlled, but the patch cannot be cut and dose rate cannot be changed
Solution Approach 1:
The patent achieves consistent near zero-order release kinetics through the thermodynamic equilibrium of saturated solution and dissolving solid particles, rather than through membrane control. This parameter-based control mechanism does not rely on a rate-limiting membrane, allowing the patch to be cut to size while maintaining proportional release rates, thus providing both reliability and adaptability.
4Adaptability or versatility
If a transdermal patch uses adhesive polymer dispersion systems to allow cutting and dose adjustment, then the patch is more versatile, but the kinetics of drug release are not optimal
Solution Approach 1:
The patent combines the versatility of adhesive polymer dispersion systems with the release-control mechanism of saturated solution-solid particle equilibria. The adhesive matrix allows cutting and dose adjustment, while the capsaicin phase distribution ensures optimal near zero-order kinetics, resolving the contradiction between versatility and release consistency.
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 patch achieves a stable, prolonged release of capsaicin, providing effective pain relief for an extended period without the need for increasing concentrations in each layer or a membrane for regulation.
Implementation Method 1
an excipient, preferably a liquid excipient, which controls the solubility of the active ingredient in dissolved form in the matrix
Implementation Method 2
the saturated solution of the active ingredient in the matrix
Implementation Method 3
the active ingredient leaving the matrix during administration through the skin is replaced by the dissolution of the active ingredient dispersed in the form of a pure substance
Implementation Method 4
transdermal preparations are able to deliver their active ingredient content—with appropriate release kinetics—into the skin, or into the human body through the skin
Implementation Method 5
The two characteristics are well combined in 'micro-reservoir' type systems, but these are expensive to produce. This type of TTS is thicker than the others and release is controlled by diffusion through the polymer matrix
Data Source
AI summary
The invention relates to a topical, preferably transdermal preparation and patch, which can deliver its active ingredient content into the skin with near zero-order kinetics, as well as a method for their production. The active ingredient is preferably an NSAID or a capsaicinoid. In particular, the invention relates to a transdermal patch comprising a low dose of capsaicin, which, when placed on the skin, ensures the release of the active ingredient over a long period of time, preferably for 4 to 24 hours, more preferably for 6-12 hours, with near zero-order kinetics. The invention further relates to the production of these preparations. The invention further relates to the use of these preparations to relieve pain, preferably acute pain, and/or chronic inflammatory and neuropathic pain, and as a warm-up patch during sports activities.