2-O-α-D-Glucosyl-L-Ascorbic Acid for Stable Skin Turnover

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Solution Overview

Problem

Current external dermal agents for anti-aging only partially address skin issues like wrinkles, fine wrinkles, and saggings, and there is a need for a novel approach that improves skin turnover and inhibits glycation, which contributes to skin aging.

Innovation Solution

A dermal composition containing 2-O-α-D-glucosyl-L-ascorbic acid or its sodium salt, which is stable and effectively released in the skin to enhance skin turnover and inhibit glycation, thereby improving skin health and appearance.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If conventional external dermal agents are used for anti-aging, then some skin issues are addressed, but skin turnover is not sufficiently improved and glycation inhibition is insufficient

Engineering Contradiction:
Improveanti-aging effectivenessVSAvoidskin turnover rate
Core Design Contradiction:
ReliabilityVSProductivity

Solution Approach 1:

The patent uses 2-O-α-D-glucosyl-L-ascorbic acid as an intermediary compound that bridges the gap between stable vitamin C delivery and effective skin turnover improvement. This glycosylated derivative acts as a mediator that is stable enough for topical application yet effectively converts to active L-ascorbic acid in the skin, thereby improving turnover without the instability issues of pure L-ascorbic acid.

Inventive Principle:
Principle #24Intermediary (Mediator)

Solution Approach 2:

The patent changes the chemical parameter of vitamin C by glycosylation at the 2-O position, transforming L-ascorbic acid into 2-O-α-D-glucosyl-L-ascorbic acid. This parameter change enhances stability for topical application while maintaining the ability to improve skin turnover and inhibit glycation, thus resolving the contradiction between stability and effectiveness.

Inventive Principle:
Principle #35Parameter changes

2Productivity

If L-ascorbic acid is used to improve skin turnover, then turnover rate increases, but stability and ease of application decrease

Engineering Contradiction:
Improveskin turnover rateVSAvoidcompound stability
Core Design Contradiction:
ProductivityVSStability of the object's composition

Solution Approach 1:

The patent employs 2-O-α-D-glucosyl-L-ascorbic acid as a stable intermediary that can be topically applied and then converts to active L-ascorbic acid in the skin. This intermediary form maintains stability during storage and application while releasing the active form where needed, thus resolving the stability-effectiveness contradiction.

Inventive Principle:
Principle #24Intermediary (Mediator)

Solution Approach 2:

The patent performs preliminary glycosylation of L-ascorbic acid to create a stable derivative before topical application. This preliminary chemical modification prepares the compound for stable storage and application, with the understanding that it will convert to the active form in the skin, thus advance-solving the stability problem.

Inventive Principle:
Principle #10Preliminary action

3Reliability

If AGEs accumulate in skin tissues, then skin aging increases, but detecting and measuring the extent of glycation is difficult

Engineering Contradiction:
Improveanti-aging effectVSAvoidglycation level measurement
Core Design Contradiction:
ReliabilityVSDifficulty of detecting and measuring

Solution Approach 1:

The patent incorporates ingredients that inhibit glycation pathways, creating a feedback mechanism that prevents AGE accumulation before it occurs. By targeting the glycation process itself rather than just treating symptoms, the composition provides measurable prevention effects that can be assessed through skin quality improvements.

Inventive Principle:
Principle #23Feedback

Solution Approach 2:

The patent converts the harmful glycation process into a beneficial target for intervention by using ingredients that specifically inhibit glycation. Instead of dealing with the consequence of AGE accumulation, the composition prevents the harmful process itself, turning the problem of glycation into an opportunity for targeted prevention.

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

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 prevents or improves wrinkles, fine wrinkles, and saggings by enhancing skin turnover and maintaining skin barrier function, while inhibiting glycation, leading to improved skin health and a more youthful appearance.

Implementation Method 1

2-O-α-D-glucosyl-L-ascorbic acid or a sodium salt thereof, which is stable and effectively released in the skin

Methodology Applied
Scientific EffectHydrolysis: Hydrolysis

Implementation Method 2

inhibiting glycation, which contributes to skin aging

Methodology Applied
Scientific EffectGlycation inhibition:

Data Source

PatentEP3398585B1External dermal composition for Anti-ageing and method for producing the same
Publication Date: 2020.02.26 HAYASHIBARA CO LTD
  • EP3398585B1 patent drawingFigure 1~2
  • EP3398585B1 patent drawingFigure 3A~3B
  • EP3398585B1 patent drawingFigure 4A~4D

AI summary

Provided is a use of one or more members selected from the groupconsisting of L-ascorbic acid, an L-ascorbic acid derivative, and a salt thereof as a effective ingredient(s) in an external dermal composition for anti-ageing, which composition further comprises an aqueous medium as a base material. The L-ascorbic acid derivative may be a glycosyl-, acyl-, or phosphorylated-derivative of L-ascorbic acid. Further provided is a method for producing an external dermal composition for anti-ageing or a skin care comprising the external dermal composition.