Medicated Patch Using 5-Methyl-1-Phenyl-2-Pyridone for Skin Permeability

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Solution Overview

Problem

There is a lack of a medicated patch using 5-methyl-1-phenyl-2-(1H)-pyridone or its pharmaceutically acceptable salt that offers excellent skin permeability, sustained medicinal effect, adhesion, flexibility, and aggregability for the treatment of skin diseases such as hyperplastic scars, keloids, and fibrous skin diseases.

Innovation Solution

A medicated patch is developed with 5-methyl-1-phenyl-2-(1H)-pyridone as the active component, utilizing specific dissolving agents like peppermint oil and water-soluble or rubber-type polymers to enhance skin permeability and adhesion, with compositions optimized for aqueous or oil-based base materials.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If 5-methyl-1-phenyl-2-(1H)-pyridone is used as an active component in a medicated patch, then it provides therapeutic effect for skin diseases, but it exhibits poor solubility in aqueous base materials and inadequate skin permeability

Engineering Contradiction:
Improvetherapeutic effectVSAvoidsolubility in base material
Core Design Contradiction:
ReliabilityVSEase of manufacture

Solution Approach 1:

The patent changes the chemical parameters of the base material by selecting specific dissolving agents (propylene glycol, butylene glycol, isopropyl myristate, ethylene glycol salicylate, propylene carbonate) that are compatible with 5-methyl-1-phenyl-2-(1H)-pyridone. This parameter change enables the active component to dissolve effectively in the base material, resolving the solubility issue while maintaining therapeutic efficacy.

Inventive Principle:
Principle #35Parameter changes

Solution Approach 2:

The patent creates a composite base material system combining multiple components including dissolving agents, adhesive polymers, and the active component 5-methyl-1-phenyl-2-(1H)-pyridone. This composite approach allows each component to contribute its specific properties, achieving both solubility and skin permeability enhancement simultaneously.

Inventive Principle:
Principle #40Composite materials

2Ease of manufacture

If conventional base materials are used for the medicated patch, then manufacturing is simplified, but the patch exhibits inadequate adhesion, flexibility, and aggregability

Engineering Contradiction:
Improvemanufacturing simplicityVSAvoidadhesion and flexibility
Core Design Contradiction:
Ease of manufactureVSReliability

Solution Approach 1:

The patent develops a composite adhesive polymer system combining polyisobutylene, styrene-isoprene-styrene block copolymer, and other polymers in specific ratios. This composite material provides superior adhesion, flexibility, and aggregability compared to conventional single-component base materials, while remaining manufacturable through standard patch fabrication processes.

Inventive Principle:
Principle #40Composite materials

Solution Approach 2:

The patent optimizes the compositional parameters of the base material by specifying precise weight ratios of different polymers and dissolving agents. This parameter optimization ensures the patch achieves the required mechanical properties (adhesion, flexibility) while maintaining ease of manufacture through controlled formulation rather than complex processing.

Inventive Principle:
Principle #35Parameter changes

3Reliability

If the active component concentration is increased to enhance therapeutic effect, then medicinal efficacy improves, but skin permeability and sustained release characteristics deteriorate

Engineering Contradiction:
Improvemedicinal efficacyVSAvoidsustentation of medicinal effect
Core Design Contradiction:
ReliabilityVSDuration of action of moving object

Solution Approach 1:

The patent optimizes the concentration parameter of 5-methyl-1-phenyl-2-(1H)-pyridone within a specific range (0.1-30 mass%) and adjusts the composition of dissolving agents and base materials accordingly. This parameter optimization ensures adequate therapeutic effect while maintaining proper skin permeability and sustained release characteristics through balanced formulation.

Inventive Principle:
Principle #35Parameter changes

Solution Approach 2:

The dissolving agents (propylene glycol, butylene glycol, isopropyl myristate, etc.) act as intermediaries between the active component and the skin. These intermediaries facilitate controlled permeation and sustained release of the active component, allowing therapeutic efficacy to be maintained over time without requiring excessive drug concentration.

Inventive Principle:
Principle #24Intermediary (Mediator)

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 medicated patch achieves high skin permeability and sustained medicinal effect, effectively treating skin diseases like hypertrophic scars and keloids without systemic diffusion, ensuring localized administration and minimizing side effects.

Implementation Method 1

solubility of 5-methyl-1-phenyl-2-(1H)-pyridone to an aqueous base material is improved by selecting, as a dissolving agent, peppermint oil, oleyl alcohol, isopropanol, propylene glycol, butylene glycol, N-methyl-pyrrolidone, diethylene glycol monoethyl ether, triacetine, glycerin, crotamiton, macrogol, isopropyl myristate, glycerin triethyl hexanoate, diisopropyl sebacate, diethyl sebacate, diisopropyl adipate, triethyl citrate, ethylene glycol salicylate, propylene carbonate and medium-chain fatty acid triglycerides

Methodology Applied
Scientific EffectDissolution: Solvation

Implementation Method 2

a medicated patch including a percutaneously absorbable preparation layer, which is effective for the prophylaxis and treatment of skin diseases... provides fine skin permeability of the active component

Methodology Applied
Scientific EffectPercutaneous absorption: Permeation

Implementation Method 3

an aqueous-type medicated patch including 5-methyl-1-phenyl-2-(1H)-pyridone having preferable adhesion, flexibility and/or aggregability for medicated patches

Methodology Applied
Scientific EffectAdhesion: Adhesive

Data Source

PatentUS8287900B2Medicated patch comprising 5-methyl-1-phenyl-2-(1H)-pyridone
Publication Date: 2012.10.16 LEAD CHEM CO LTD
  • US8287900B2 patent drawing
  • US8287900B2 patent drawing
  • US8287900B2 patent drawing

AI summary

There is provided a medicated patch including 5-methyl-1-phenyl-2-(1H)-pyridone. A medicated patch comprising a percutaneously absorbable preparation layer, wherein the percutaneously absorbable preparation layer includes 5-methyl-1-phenyl-2-(1H)-pyridone or a pharmaceutically acceptable salt thereof as an active component, a dissolving agent and an aqueous base material (or a rubber-type base material), and the active component is contained in an amount of 0.1 to 30 mass % relative to the total amount of the percutaneously absorbable preparation layer.