Transdermal Adhesive Plasticity via 4E Indolone

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Solution Overview

Problem

Transdermal preparations face challenges in achieving suitable tackiness and maintaining sufficient transdermal absorption of physiologically active compounds, particularly with the known decomposition product 4-ethylene-2(3H)-indolone (4E indolone) lacking specific usage.

Innovation Solution

Incorporating 4E indolone into the adhesive layer of transdermal preparations, along with a physiologically active compound like ropinirole, enhances the plasticity and tackiness of the adhesive layer while maintaining effective transdermal absorption properties.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Ease of operation

If 4E indolone is included in the adhesive layer to improve plasticity and tackiness, then the adhesive properties are improved, but the transdermal absorption property may be compromised

Engineering Contradiction:

ImprovetackinessVSAvoidtransdermal absorption property

Core Design Contradiction:

Ease of operationVSReliability

Solution Approach 1:

The patent converts 4E indolone, which was previously considered merely a decomposition product without specific usage, into a beneficial plasticizing agent for the adhesive layer. By incorporating 4E indolone at controlled concentrations (0.01-5 mass%), the invention improves adhesive plasticity and tackiness while maintaining sufficient transdermal absorption of physiologically active compounds, thus transforming a previously useless or potentially harmful substance into a valuable functional component.

Inventive Principle:

Principle #22Blessing in disguise (Convert harm into benefit)

2Ease of operation

If the adhesive layer is made more plastic to improve tackiness, then application ease is improved, but the transdermal absorption property may deteriorate

Engineering Contradiction:

ImproveplasticityVSAvoidtransdermal absorption property

Core Design Contradiction:

Ease of operationVSReliability

Solution Approach 1:

The patent employs parameter changes by precisely controlling the concentration of 4E indolone in the adhesive layer (0.01-5 mass%). This quantitative parameter adjustment optimizes the balance between plasticity improvement and maintenance of transdermal absorption properties. The specific concentration range was determined to achieve sufficient plasticizing effect while preventing excessive dilution or interference with the transdermal absorption of the physiologically active compound.

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 inclusion of 4E indolone improves the adhesive layer's plasticity and tackiness, ensuring a transdermal preparation with sustained absorption of physiologically active compounds, as demonstrated by improved adhesion strength and permeation rates in skin permeation tests.

Implementation Method 1

4E indolone exerted an excellent plasticizing action on the adhesive layer of the transdermal preparation

Methodology Applied

Scientific EffectPlasticizing action:

Implementation Method 2

maintain a sufficient transdermal absorption property of physiologically active compounds

Methodology Applied

Scientific EffectTransdermal absorption: Permeation

Data Source

PatentUS9238025B2Transdermal preparation comprising a ropinirole derivative

Publication Date: 2016.01.19 HISAMITSU PHARM CO INC

AI summary

The present invention relates to a transdermal preparation having a backing and an adhesive layer laminated on the backing, wherein the adhesive layer contains 4-ethylene-2(3H)-indolone and a physiologically active compound, and wherein the 4-ethylene-2(3H)-indolone is present in an amount from 0.001 to 4 mass % of the total mass of components of the adhesive layer.