Acrylic Adhesive Patch for Serotonin Antagonists

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Solution Overview

Problem

Current transdermal absorption-type patches for serotonin receptor antagonists face challenges in achieving rapid onset of drug efficacy, sufficient transdermal absorbability, and rapid drug elimination, while also causing skin irritation and having long transdermal absorption delay times.

Innovation Solution

A transdermal patch comprising a non-functional acrylic adhesive, a water-soluble organic amine, and a fatty acid ester, which allows for a serotonin receptor antagonist to be administered once daily, with a serotonin receptor antagonist such as ramosetron, granisetron, or palonosetron, achieving a short transdermal absorption delay time and maximum permeation rate within a short time.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Duration of action of stationary object

If an adhesive containing a hydroxyl group is used to enable long-term skin application (24 hours or more), then the duration of action is improved, but the initial adhesive power becomes too strong causing skin irritation and the transdermal absorbability is insufficient

Engineering Contradiction:
Improveduration of skin applicationVSAvoidskin irritation
Core Design Contradiction:
Duration of action of stationary objectVSObject-affected harmful factors

Solution Approach 1:

The patent removes the hydroxyl group functional group from the acrylic adhesive to eliminate the harmful effect of strong initial adhesion that causes skin irritation and peeling of the horny layer, while maintaining long-term skin application capability through alternative adhesive formulations

Inventive Principle:
Principle #2Taking out (Extraction)

Solution Approach 2:

The patent changes the chemical structure parameters of the acrylic adhesive by eliminating the hydroxyl group, thereby altering the adhesive properties to reduce initial adhesion strength and improve transdermal absorbability while maintaining sufficient holding power for extended wear

Inventive Principle:
Principle #35Parameter changes

2Duration of action of stationary object

If a transdermal patch with continuous drug release is used, then the duration of action is improved, but the rapid onset of drug efficacy is insufficient for once-daily administration

Engineering Contradiction:
Improvecontinuous drug releaseVSAvoidonset of drug efficacy
Core Design Contradiction:
Duration of action of stationary objectVSSpeed

Solution Approach 1:

The patent incorporates an absorption enhancer in the adhesive formulation that pre-prepares the skin barrier for drug penetration, enabling both rapid onset of efficacy and sustained continuous release throughout the 24-hour wear period

Inventive Principle:
Principle #10Preliminary action

Solution Approach 2:

The patent uses a composite adhesive system combining acrylic adhesive with absorption enhancers that work synergistically to achieve both rapid initial drug penetration and sustained continuous release, satisfying the requirements for once-daily administration

Inventive Principle:
Principle #40Composite materials

3Duration of action of stationary object

If an adhesive with strong holding power is used to maintain long-term skin application, then the duration of action is improved, but the peeling of the horny layer occurs simultaneously with formulation peeling causing strong skin irritation

Engineering Contradiction:
Improveholding powerVSAvoidskin irritation from peeling
Core Design Contradiction:
Duration of action of stationary objectVSObject-affected harmful factors

Solution Approach 1:

The patent removes the hydroxyl group from the acrylic adhesive that is responsible for the strong initial adhesion causing horny layer peeling, thereby eliminating the harmful peeling effect while maintaining sufficient holding power through alternative adhesive mechanisms

Inventive Principle:
Principle #2Taking out (Extraction)

Solution Approach 2:

The patent creates different adhesive properties at different stages: reduced initial adhesion to prevent horny layer damage, while maintaining sufficient holding power for long-term wear, achieving spatial and temporal differentiation of adhesive 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 enables efficient and continuous transdermal absorption of serotonin receptor antagonists, reducing skin irritation and improving patient quality of life by achieving rapid drug efficacy and rapid elimination from the bloodstream, suitable for once-daily administration.

Implementation Method 1

a transdermal absorption-type patch which enables efficient and continuous absorption of a serotonin receptor antagonist used as a therapeutic drug for nausea and vomiting from a skin

Methodology Applied
Scientific EffectTransdermal absorption: Permeation

Implementation Method 2

an adhesive containing a serotonin receptor antagonist in an effective amount for antiemetic activity and an absorption enhancer

Methodology Applied
Scientific EffectAbsorption enhancement: Absorption (physical)

Data Source

PatentEP2730290B1Adhesive skin patch containing serotonin receptor antagonist drug
Publication Date: 2019.09.18 TEIKOKU SEIYAKU CO LTD
  • EP2730290B1 patent drawingFigure 1~2

AI summary

Provided is a transdermal absorption-type patch containing a serotonin receptor antagonist, which has a short transdermal absorption delay time (lag time), and in which the maximum transdermal permeation rate of the drug can be reached within a short time and the drug can disappear from circulating blood rapidly. That is, provided is a patch containing a serotonin receptor antagonist, wherein the patch contains an adhesive layer comprising a non-functional acrylic adhesive, a water-soluble organic amine, a fatty acid ester, and a serotonin receptor antagonist such as granisetron as an active ingredient.