Asenapine Patch Adhesive Cold Flow Control

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Solution Overview

Problem

Asenapine-containing patches with silicone-based pressure-sensitive adhesive bases experience cold flow issues, leading to decreased skin permeability and stability, making it difficult to maintain the medicinal effect and administration form over time.

Innovation Solution

A patch with a pressure-sensitive adhesive layer containing asenapine and a silicone-based adhesive base, where the loss tangent is adjusted to 0.75 to 1.5 and viscosity is 3,000 to 60,000 Pa·s at 90° C, combining high-tack, medium-tack, and low-tack amine-compatible silicone-based adhesives to suppress cold flow and enhance adhesiveness and stability.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If a silicone-based pressure-sensitive adhesive base is used to enhance skin permeability, then skin permeability is improved, but cold flow occurs during storage or application leading to decreased stability and handleability

Engineering Contradiction:
Improveskin permeabilityVSAvoidtemporal stability
Core Design Contradiction:
ReliabilityVSStability of the object's composition

Solution Approach 1:

The invention changes the rheological parameters of the pressure-sensitive adhesive by controlling the loss tangent (tan δ) within 0.5 to 2.0 and viscosity at 90°C within 1,000 to 100,000 Pa·s. This parameter optimization allows the adhesive to maintain appropriate softness for skin permeability while suppressing cold flow during storage, resolving the contradiction between reliability and stability

Inventive Principle:
Principle #35Parameter changes

Solution Approach 2:

The invention uses a composite pressure-sensitive adhesive system combining silicone-based adhesive with specific additives and modifiers. This composite formulation maintains the high skin permeability of silicone while incorporating components that reduce cold flow tendency, thereby achieving both improved reliability and enhanced stability

Inventive Principle:
Principle #40Composite materials

2Reliability

If a silicone-based pressure-sensitive adhesive base is used to enhance skin permeability, then skin permeability is improved, but cold flow causes the pressure-sensitive adhesive layer to protrude and adhere to packaging material, decreasing handleability

Engineering Contradiction:
Improveskin permeabilityVSAvoidhandleability
Core Design Contradiction:
ReliabilityVSEase of operation

Solution Approach 1:

By optimizing the loss tangent (tan δ) to 0.5-2.0 and viscosity at 90°C to 1,000-100,000 Pa·s, the invention adjusts the adhesive's flow characteristics to prevent excessive protrusion during application while maintaining skin permeability. The controlled rheological properties ensure the adhesive remains manageable and does not adhere excessively to packaging materials

Inventive Principle:
Principle #35Parameter changes

Solution Approach 2:

The invention applies preliminary anti-action by formulating the pressure-sensitive adhesive with cold-flow suppressing components before application. This preventive approach counteracts the tendency to protrude and adhere to packaging materials, maintaining ease of operation throughout storage and application processes

Inventive Principle:
Principle #9Preliminary anti-action

3Stability of the object's composition

If cold flow is suppressed by adjusting loss tangent and viscosity, then stability and handleability are improved, but skin permeability may decrease

Engineering Contradiction:
Improvetemporal stabilityVSAvoidskin permeability
Core Design Contradiction:
Stability of the object's compositionVSReliability

Solution Approach 1:

The invention identifies and optimizes specific rheological parameters (loss tangent: 0.5-2.0, viscosity at 90°C: 1,000-100,000 Pa·s) that simultaneously achieve cold flow suppression and maintain skin permeability. This precise parameter control resolves the contradiction by finding the optimal range where both stability and permeability are satisfied

Inventive Principle:
Principle #35Parameter changes

Solution Approach 2:

The invention applies local quality by creating different functional zones within the pressure-sensitive adhesive layer. The adhesive formulation provides localized properties: regions with higher elasticity for cold flow suppression and regions with appropriate viscosity for maintaining skin permeability, achieving both objectives through spatially differentiated characteristics

Inventive Principle:
Principle #3Local quality

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 effectively suppresses cold flow, maintaining stability and adhesiveness, ensuring sustained medicinal effects and appropriate administration form by controlling the loss tangent and viscosity of the adhesive layer.

Implementation Method 1

Cold flow is a phenomenon in which a pressure-sensitive adhesive flows/deforms at room temperature during storage or application

Methodology Applied
Scientific EffectCold flow: Creep

Implementation Method 2

by adjusting loss tangent (tan δ) of a pressure-sensitive adhesive layer within a predetermined range to suppress the cold flow

Methodology Applied
Scientific EffectViscoelasticity: Viscoelasticity

Implementation Method 3

the patch has excellent adhesiveness and handleability

Methodology Applied
Scientific EffectAdhesion: Adhesive

Data Source

PatentUS11850311B2Asenapine-containing adhesive patch
Publication Date: 2023.12.26 HISAMITSU PHARM CO INC

AI summary

An object of the present invention is to provide an asenapine-containing patch having excellent adhesiveness and handleability, which can persistently provide sufficient medicinal effects by suppressing cold flow during storage or application while enhancing skin permeability using a silicone-based pressure-sensitive adhesive base, and thereby maintaining the stability of the drug in the patch during storage, and maintaining an appropriate administration form for a long period of time. The present invention relates to a patch having a support and a pressure-sensitive adhesive layer, wherein the pressure-sensitive adhesive layer comprises asenapine and a silicone-based pressure-sensitive adhesive base, and the loss tangent (tan δ) of the pressure-sensitive adhesive layer is 0.75 to 1.5 at 1.0 Hz.