Asenapine Patch Using Sodium Diacetate for Skin Permeability
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Solution Overview
Problem
Conventional patches containing asenapine have low skin permeability, requiring large application areas and resulting in low use efficiency, and the incorporation of organic acids to enhance permeability leads to instability and variability in skin permeability over time.
Innovation Solution
A patch is developed with an adhesive agent layer containing sodium diacetate and asenapine or its pharmaceutically acceptable salt, where the sodium diacetate is generated by mixing sodium acetate with asenapine, achieving high skin permeability without the need for organic acids, thereby stabilizing the permeability and reducing variability.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Reliability
If organic acid and/or organic acid salt are incorporated to improve skin permeability, then skin permeability is improved, but production stability decreases due to volatilization of organic acid
Solution Approach 1:
The patent extracts and eliminates the volatile organic acid component from the formulation while retaining the beneficial skin permeability enhancement through the use of organic acid salt (sodium acetate) alone, thereby resolving the contradiction between improved permeability and production stability
Solution Approach 2:
The patent replaces the unstable volatile organic acid with a stable organic acid salt that does not volatilize, effectively substituting a short-lived unstable component with a long-lived stable alternative that maintains the desired pharmacological effect
2Reliability
If organic acid and/or organic acid salt are incorporated to improve skin permeability, then skin permeability is improved, but stability over time of skin permeability decreases
Solution Approach 1:
The patent removes the volatile organic acid component that causes degradation over time, relying solely on the stable organic acid salt to maintain consistent skin permeability enhancement throughout the product shelf life
Solution Approach 2:
The patent substitutes the time-unstable volatile organic acid with a time-stable organic acid salt, ensuring that the skin permeability enhancement effect remains consistent over the entire duration of product storage and use
3Reliability
If organic acid and/or organic acid salt are incorporated to improve skin permeability, then skin permeability is improved, but variation in skin permeability among preparations increases
Solution Approach 1:
The patent eliminates the volatile organic acid component that causes batch-to-batch variability, using only the stable organic acid salt to achieve consistent skin permeability enhancement across all pharmaceutical preparations
Solution Approach 2:
The patent changes the chemical form from volatile organic acid to non-volatile organic acid salt, fundamentally altering the physical-chemical parameters to eliminate variability while maintaining the skin permeability enhancement effect
4Reliability
If application area is increased to achieve therapeutically effective blood concentration, then blood concentration is improved, but use efficiency decreases
Solution Approach 1:
The patent changes the formulation parameters by incorporating organic acid salt, which enhances skin permeability and enables achievement of therapeutic blood concentrations with smaller application areas, thereby improving use efficiency
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 sustained high skin permeability of asenapine without incorporating organic acids, enhancing production stability and maintaining skin permeability over time, while reducing variations among pharmaceutical preparations.
Implementation Method 1
sodium diacetate is generated by mixing sodium acetate with asenapine
Data Source
AI summary
A method for producing a patch including a support layer, and an adhesive agent layer formed on the support layer and including sodium diacetate, a pressure-sensitive adhesive base agent, and asenapine and/or a pharmaceutically acceptable salt thereof. The sodium diacetate is generated from sodium acetate in the presence of the asenapine and/or salt thereof, a content of the asenapine and/or salt thereof in terms of free asenapine in the adhesive agent layer is in range of 3.0 to 20 mg, and when a content of the asenapine and/or salt thereof in terms of free asenapine in the adhesive agent layer is 6.4 mg and the patch is in contact with skin for 24 hours, Cmax of free asenapine is in range of 0.5 to 6.0 ng/mL and tmax of free asenapine is in range of 8 to 28 hr.