Cyclohexane-hexol and N-acyl amino acid composition for trypsin inhibition

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Solution Overview

Problem

Current cosmetic solutions fail to effectively inhibit trypsin activity, leading to uneven skin tone and age spots due to unregulated melanin production and distribution, which are common issues in aging skin.

Innovation Solution

A topical cosmetic composition combining cyclohexane-1,2,3,4,5,6-hexol, N-acyl amino acids such as N-acyl Phenylalanine or N-acyl Tyrosine, and optionally vitamin B3 and 2-hexyldecan-1-ol, which inhibit trypsin activity when applied to the skin, thereby reducing melanin overproduction and improving skin tone.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If individual cosmetic components are used, then the formulation is simple, but the trypsin inhibition effectiveness is insufficient

Engineering Contradiction:
Improvetrypsin inhibition effectivenessVSAvoidcomposition complexity
Core Design Contradiction:
ReliabilityVSDevice complexity

Solution Approach 1:

The patent combines multiple active ingredients (cyclohexane-1,2,3,4,5,6-hexol, N-acyl amino acid compounds, and optionally vitamin B3 and 2-hexyldecan-1-ol) into a single cosmetic composition. This combination creates a synergistic effect that enhances trypsin inhibition effectiveness compared to individual components, while the formulation remains practical for topical application.

Inventive Principle:
Principle #5Merging (Combining)

Solution Approach 2:

The invention uses a composite cosmetic formulation incorporating multiple functional ingredients that work together to inhibit trypsin activity. The composite nature of the composition allows for enhanced biological activity and improved skin tone regulation while maintaining safety and tolerability through careful selection of complementary ingredients.

Inventive Principle:
Principle #40Composite materials

2Reliability

If trypsin activity is not inhibited, then the skin maintains natural functions, but melanin overproduction occurs leading to age spots and uneven skin tone

Engineering Contradiction:
Improveskin tone uniformityVSAvoidmelanin overproduction
Core Design Contradiction:
ReliabilityVSObject-affected harmful factors

Solution Approach 1:

The patent targets the harmful effect of trypsin-induced melanin overproduction by using N-acyl amino acid compounds that inhibit trypsin activity. This conversion of a harmful biological process (excessive melanin production leading to age spots) into a beneficial outcome (regulated melanin distribution and uniform skin tone) is achieved through the selective inhibition of trypsin, which is known to activate PAR-2 receptors that promote melanosome transfer.

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

3Reliability

If strong trypsin inhibitors are used, then age spots are reduced effectively, but skin irritation may increase

Engineering Contradiction:
Improveage spot reductionVSAvoidskin irritation
Core Design Contradiction:
ReliabilityVSObject-affected harmful factors

Solution Approach 1:

The patent optimizes the concentration and formulation parameters of the active ingredients to achieve effective trypsin inhibition while minimizing skin irritation. By carefully controlling the amount of N-acyl amino acid compounds and cyclohexane-1,2,3,4,5,6-hexol in the composition, the formulation achieves therapeutic effectiveness without causing excessive skin irritation or adverse reactions.

Inventive Principle:
Principle #35Parameter changes

Solution Approach 2:

The inclusion of vitamin B3 and 2-hexyldecan-1-ol as optional components may serve as intermediary substances that modulate the activity of the primary trypsin inhibitors. These additional ingredients can enhance the overall formulation's ability to inhibit trypsin while providing skin-conditioning benefits and reducing potential irritation, thereby serving as protective intermediaries between the active ingredients and the skin.

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 composition effectively inhibits trypsin activity, reducing the appearance of age spots and improving overall skin tone by regulating melanin distribution, providing a safer and more effective solution than individual components alone.

Implementation Method 1

The composition effectively inhibits trypsin activity, reducing the appearance of age spots and improving overall skin tone by regulating melanin distribution

Methodology Applied
Scientific EffectEnzyme inhibition: Enzyme

Data Source

PatentEP2640346B1Cosmetic compositions and methods for inhibiting or reducing trypsin activity based on cyclohexane-1,2,3,4,5,6-hexol and a n-acyl amino acid compound
Publication Date: 2016.02.10 PROCTER & GAMBLE CO
  • EP2640346B1 patent drawingFigure 1
  • EP2640346B1 patent drawingFigure 2
  • EP2640346B1 patent drawingFigure 3

AI summary

A cosmetic composition formulated for topical application to skin is provided. The composition includes a safe and effective amount of cyclohexane-1,2,3,4,5,6-hexol; a safe and effective amount of an N-acyl amino acid compound; and a dematologically acceptable vehicle.