Butorphanol Patch Adhesive Layer Composition

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Solution Overview

Problem

Patches containing butorphanol or its pharmaceutically acceptable salts often experience insufficient adhesion to the skin, particularly under warm water or high humidity conditions, necessitating improved skin permeability and adhesion resistance.

Innovation Solution

A patch design incorporating a backing layer and an adhesive layer with a specific blending ratio of rubber-based and silicone-based adhesive bases, along with butorphanol and/or its pharmaceutically acceptable salts, to enhance skin permeability and adhesion, even under challenging conditions.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Strength

If rubber-based adhesive base is used to achieve excellent adhesive strength, then adhesion to skin is improved, but adhesion deteriorates under warm water or high humidity conditions

Engineering Contradiction:
Improveadhesive strengthVSAvoidadhesion stability under water/humidity
Core Design Contradiction:
StrengthVSReliability

Solution Approach 1:

The patent combines rubber-based adhesive base and silicone-based adhesive base in a specific mass ratio (9.5:0.5 to 1.9:8.1) to create a composite adhesive system. The rubber-based component provides initial adhesive strength, while the silicone-based component maintains adhesion stability under water and humidity conditions, resolving the contradiction between strong adhesion and adhesion reliability.

Inventive Principle:
Principle #40Composite materials

Solution Approach 2:

The patent optimizes the mass ratio parameters of rubber-based and silicone-based adhesive bases to achieve the desired balance. By adjusting these compositional parameters within specific ranges, the adhesive system achieves both strong initial adhesion and maintained adhesion under challenging environmental conditions.

Inventive Principle:
Principle #35Parameter changes

2Duration of action of stationary object

If patch is designed for long-term skin application, then duration of action is improved, but skin permeability requirement increases

Engineering Contradiction:
Improvepatch application durationVSAvoidskin permeability
Core Design Contradiction:
Duration of action of stationary objectVSReliability

Solution Approach 1:

The patent optimizes the content ratio of butorphanol to adhesive bases within specific ranges to ensure sufficient drug loading for long-term application while maintaining effective skin permeability. This parameter optimization allows the patch to deliver adequate drug amounts over extended periods without compromising permeability.

Inventive Principle:
Principle #35Parameter changes

Solution Approach 2:

The silicone-based adhesive base component contributes to maintaining skin permeability during long-term application, while the rubber-based component ensures prolonged adhesion. The composite system addresses both the extended duration requirement and the permeability maintenance challenge.

Inventive Principle:
Principle #40Composite materials

3Object-affected harmful factors

If butorphanol content per unit area is reduced, then safety is improved, but skin permeability may be insufficient

Engineering Contradiction:
Improvedrug safetyVSAvoidskin permeability
Core Design Contradiction:
Object-affected harmful factorsVSReliability

Solution Approach 1:

The patent optimizes the butorphanol content parameters within specific ranges (3-20% by mass relative to total adhesive layer mass) to achieve the lowest effective dose that maintains sufficient skin permeability. This parameter optimization ensures safety by minimizing drug content while maintaining therapeutic effectiveness through enhanced permeability from the adhesive base combination.

Inventive Principle:
Principle #35Parameter changes

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 superior skin permeability and high-level adhesion with excellent water resistance and moisture resistance, maintaining effective adhesion and drug delivery performance.

Implementation Method 1

the adhesive layer contains at least one selected from the group consisting of butorphanol and pharmaceutically acceptable salts thereof, and contains a rubber-based adhesive base and a silicone-based adhesive base

Methodology Applied
Scientific EffectAdhesion: Adhesive

Implementation Method 2

the patch is required to exhibit superior skin permeability of butorphanol

Methodology Applied
Scientific EffectTransdermal absorption: Permeation

Data Source

PatentUS11202764B2Patch
Publication Date: 2021.12.21 HISAMITSU PHARM CO INC
  • US11202764B2 patent drawing
  • US11202764B2 patent drawing

AI summary

A patch comprises a backing layer and an adhesive layer, wherein the adhesive layer contains at least one selected from the group consisting of butorphanol and pharmaceutically acceptable salts thereof, and contains a rubber-based adhesive base and a silicone-based adhesive base, and a mass ratio of the rubber-based adhesive base to the silicone-based adhesive base (the mass of the rubber-based adhesive base:the mass of silicone-based adhesive base) in the adhesive layer is 9.5:0.5 to 1.9:8.1.