Ropinirole Adhesive Patch Skin Permeability and Adhesion Balance

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Solution Overview

Problem

Conventional ropinirole transdermal patches face challenges in achieving sufficient skin permeability and adhesiveness due to the skin permeability of ropinirole acid addition salts being reduced, and adjusting the content to improve permeation complicates adhesive properties.

Innovation Solution

A ropinirole-containing patch with an adhesive agent layer containing 5-13.2% free ropinirole by mass, combined with specific compounds like benzyl alcohol and isopropyl palmitate, and a rubber-based adhesive, along with sodium hydroxide, to enhance skin permeability and adhesiveness, and storing it with a deoxidizer for stability.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Quantity of substance

If the content of ropinirole acid addition salt in the adhesive agent layer is increased to improve skin permeability, then the amount of ropinirole permeated through the skin increases, but the adhesive properties deteriorate and adhesiveness is reduced

Engineering Contradiction:
Improveamount of ropinirole permeatedVSAvoidadhesive properties
Core Design Contradiction:
Quantity of substanceVSReliability

Solution Approach 1:

The patent optimizes the content parameter of ropinirole acid addition salt in the adhesive agent layer to a specific range (0.1-5% by mass). This parameter change resolves the contradiction by finding the optimal concentration that provides sufficient ropinirole permeation while maintaining adhesive properties. The specified content range balances drug delivery effectiveness with adhesive performance.

Inventive Principle:
Principle #35Parameter changes

2Quantity of substance

If ropinirole in free form is used to improve skin permeability, then the skin permeability of ropinirole is enhanced, but the adhesive agent layer loses aggregation ability and adhesiveness is reduced

Engineering Contradiction:
Improveskin permeability of ropiniroleVSAvoidaggregation ability of adhesive agent layer
Core Design Contradiction:
Quantity of substanceVSStability of the object's composition

Solution Approach 1:

The patent specifies using ropinirole acid addition salt instead of free ropinirole, and optimizes its content parameter to 0.1-5% by mass in the adhesive agent layer. This parameter change resolves the contradiction by providing sufficient ropinirole permeation while maintaining the aggregation ability and adhesive properties of the adhesive agent layer.

Inventive Principle:
Principle #35Parameter changes

3Quantity of substance

If the content of ropinirole acid addition salt is adjusted to achieve sufficient ropinirole permeation, then the skin permeability improves, but the adhesiveness of the patch is reduced

Engineering Contradiction:
Improveropinirole permeation amountVSAvoidadhesiveness of patch
Core Design Contradiction:
Quantity of substanceVSStrength

Solution Approach 1:

The patent optimizes the content parameter of ropinirole acid addition salt to a specific range (0.1-5% by mass) in the adhesive agent layer. This parameter change simultaneously achieves sufficient ropinirole permeation and maintains adequate adhesiveness of the patch.

Inventive Principle:
Principle #35Parameter changes

Solution Approach 2:

The patent uses a composite adhesive agent layer containing both ropinirole acid addition salt and adhesive base. This composite material approach allows the system to achieve both drug permeation function and adhesive function simultaneously, resolving the contradiction between permeation effectiveness and adhesive strength.

Inventive Principle:
Principle #40Composite materials

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 excellent skin permeability and adhesiveness while maintaining ropinirole stability over time, ensuring a sufficient amount of ropinirole is permeated through the skin effectively.

Implementation Method 1

a metal salt produced by a reaction of a ropinirole acid addition salt and a metal-ion containing desalting agent

Methodology Applied
Scientific EffectChemical reaction (desalting): Chemical Bonding

Implementation Method 2

the skin permeability of ropinirole still has not been sufficient, making it difficult to keep the ropinirole concentration in the plasma at a sufficiently high level

Methodology Applied
Scientific EffectPermeation: Permeation

Implementation Method 3

by sealing and storing such a ropinirole-containing patch together with a deoxidizer, the ropinirole stability over time is further improved

Methodology Applied
Scientific EffectOxidation prevention: Oxidation

Data Source

PatentEP2716286B1Ropinirole-containing adhesive patch and packaging therefor
Publication Date: 2017.07.12 HISAMITSU PHARM CO INC
  • EP2716286B1 patent drawingFigure 1
  • EP2716286B1 patent drawingFigure 2
  • EP2716286B1 patent drawingFigure 3

AI summary

A ropinirole-containing patch comprises an adhesive agent layer and a support layer, the adhesive agent layer containing ropinirole and/or a pharmaceutically acceptable salt thereof, wherein a content of the ropinirole, and/or the pharmaceutically acceptable salt thereof in terms of free ropinirole in the adhesive agent layer is 5 to 13.2% by mass relative to a total mass of the adhesive agent layer.