Asenapine Patch Adhesive Layer Formulation for Permeability and Adhesion
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Solution Overview
Problem
Conventional patches containing asenapine with a rubber-based adhesive agent face challenges in maintaining sufficient skin permeability and adhesion force, as the incorporation of asenapine and rubber-based adhesive agents can decrease the adhesion force of the adhesive layer.
Innovation Solution
A patch design incorporating free asenapine, a maleic acid alkali salt, and a rubber-based adhesive agent, specifically styrene-isoprene-styrene block copolymers or polyisobutylene, in the adhesive layer, which maintains a strong adhesion force while enhancing skin permeability and release of asenapine.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Reliability
If asenapine and rubber-based adhesive agent are incorporated into the adhesive agent layer, then the skin permeability of asenapine is improved, but the adhesion force of the adhesive agent layer is decreased
Solution Approach 1:
The patent applies parameter changes by carefully controlling the content ratio of asenapine to rubber-based adhesive agent within 1:1 to 1:9 by mass, and maintaining asenapine content at 0.1-10% by mass in the adhesive agent layer. These specific parameter ranges optimize both skin permeability and adhesion force, resolving the contradiction between improved drug delivery and maintained adhesive strength.
2Reliability
If asenapine is released from the adhesive agent layer, then the plasma concentration of asenapine can be maintained at therapeutically effective level, but the adhesion force of the adhesive agent layer is decreased
Solution Approach 1:
The patent resolves this contradiction by optimizing the release parameters through controlled asenapine content (0.1-10% by mass) and specific ratio to rubber-based adhesive agent (1:1 to 1:9). These parameter changes enable sufficient drug release for therapeutic plasma concentration while maintaining adequate adhesion force through the balanced formulation.
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 balance of strong adhesion and effective skin permeability of asenapine, preventing a decrease in adhesion force and ensuring therapeutic plasma concentrations, while minimizing skin irritation and local adverse effects.
Implementation Method 1
the skin permeability of asenapine is not sufficient, so that it is difficult to keep the plasma concentration of asenapine at a therapeutically effective level
Implementation Method 2
the adhesion force of an adhesive agent layer is decreased in the case where asenapine and the rubber-based adhesive agent are incorporated into the adhesive agent layer
Data Source
AI summary
In a patch comprising a support layer and an adhesive agent layer, the adhesive agent layer comprises free asenapine, a maleic acid alkali salt, and a rubber-based adhesive agent.