Rotigotine Patch Adhesive Skin Permeability

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Solution Overview

Problem

Conventional rotigotine-containing patches face challenges in achieving sufficient skin permeability despite the inclusion of known tackifiers and drug transdermal absorption promoters.

Innovation Solution

A patch design incorporating a backing layer and an adhesive agent layer with rotigotine, an alicyclic saturated hydrocarbon resin, and specific aliphatic alcohols such as lauryl alcohol, octyldodecanol, or oleyl alcohol, which enhances skin permeability of rotigotine.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If conventional tackifiers and transdermal absorption promoters are included in the patch, then the patch formulation is complete, but skin permeability of rotigotine is insufficient

Engineering Contradiction:
Improveskin permeability of rotigotineVSAvoidpatch formulation complexity
Core Design Contradiction:
ReliabilityVSDevice complexity

Solution Approach 1:

The patent changes the chemical parameters of the adhesive agent by specifying precise compositional ratios: rotigotine (5-15% by mass), alicyclic saturated hydrocarbon resin (40-80% by mass), and specific aliphatic alcohols (1-10% by mass). This parameter optimization resolves the contradiction by achieving sufficient skin permeability through controlled composition rather than adding more complex formulation elements.

Inventive Principle:
Principle #35Parameter changes

Solution Approach 2:

The patent creates a composite adhesive agent layer combining rotigotine, alicyclic saturated hydrocarbon resin, and specific aliphatic alcohols in defined proportions. This composite material approach allows the formulation to achieve both complete patch structure and sufficient skin permeability through synergistic material interaction, avoiding the need for additional complex components.

Inventive Principle:
Principle #40Composite materials

2Reliability

If the adhesive agent layer contains rotigotine and conventional additives, then the patch can be formulated, but skin permeability remains insufficient

Engineering Contradiction:
Improveskin permeability of rotigotineVSAvoidamount of conventional additives
Core Design Contradiction:
ReliabilityVSQuantity of substance

Solution Approach 1:

The patent reduces the quantity of conventional additives by replacing them with a specific combination of alicyclic saturated hydrocarbon resin and designated aliphatic alcohols. The compositional parameters are controlled to achieve sufficient skin permeability with fewer and more effective substances, directly addressing the contradiction between formulation completeness and permeability sufficiency.

Inventive Principle:
Principle #35Parameter changes

Solution Approach 2:

The patent employs specific aliphatic alcohols (lauryl alcohol, octyldodecanol, oleyl alcohol, or myristyl alcohol) that serve as effective but temporary absorption promoters. These substances facilitate rotigotine penetration during the therapeutic period and are not required long-term, resolving the contradiction by using substances that provide sufficient permeability without requiring large quantities or complex long-term formulation strategies.

Inventive Principle:
Principle #27Cheap short-living objects (Disposable)

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 particularly excellent skin permeability of rotigotine, improving drug absorption and maintaining adhesive properties.

Implementation Method 1

the adhesive agent layer contains rotigotine and/or a pharmaceutically acceptable salt thereof, and the adhesive agent layer further contains an alicyclic saturated hydrocarbon resin and at least one aliphatic alcohol selected from the group consisting of lauryl alcohol, octyldodecanol, oleyl alcohol, and myristyl alcohol

Methodology Applied
Scientific EffectDiffusion: Diffusion

Implementation Method 2

the matrix contains, as a base, a non-aqueous, acrylate-based or silicone-based polymer adhesive having a solubility of 5% (w/w) for rotigotine

Methodology Applied
Scientific EffectDissolution: Solvation

Implementation Method 3

a patch with excellent skin permeability of rotigotine

Methodology Applied
Scientific EffectTransdermal absorption: Permeation

Data Source

PatentEP3984598B1Rotigotine-containing patch
Publication Date: 2023.10.18 HISAMITSU PHARM CO INC
  • EP3984598B1 patent drawing

AI summary

The present invention provides a rotigotine-containing patch comprising: a backing layer; and an adhesive agent layer, wherein the adhesive agent layer contains rotigotine and/or a pharmaceutically acceptable salt thereof, and the adhesive agent layer further contains an alicyclic saturated hydrocarbon resin and at least one aliphatic alcohol selected from the group consisting of lauryl alcohol, octyldodecanol, oleyl alcohol, and myristyl alcohol.