Stable Ascorbic Acid Derivatives for Low-Discoloration Cosmetics

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Solution Overview

Problem

Existing ascorbic acid derivatives and salts used in cosmetics suffer from instability, discoloration, odor generation, and short-lived activity, limiting their effectiveness and stability over time.

Innovation Solution

Development of a novel ascorbic acid derivative or salt represented by formula (I), where R1 and R2 are specific groups, including hydroxyisobutyl, which enhances stability, reduces discoloration and odor, and maintains high physiological activity, achieved through regiospecific etherification of ascorbic acid's hydroxyl groups.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Stability of the object's composition

If ascorbic acid derivatives or salts are used to improve stability over time, then stability is improved, but discoloration and odor generation occur over time

Engineering Contradiction:

Improvestability over timeVSAvoiddiscoloration and odor generation

Core Design Contradiction:

Stability of the object's compositionVSObject-generated harmful factors

Solution Approach 1:

The patent modifies the chemical structure of ascorbic acid derivatives by changing specific parameters (introducing hydroxyisobutyl groups at specific positions) to achieve both improved stability and reduced discoloration/odor. This structural parameter change resolves the contradiction by creating a derivative that maintains the beneficial properties while eliminating the harmful effects.

Inventive Principle:

Principle #35Parameter changes

Solution Approach 2:

The patent creates a composite molecular structure by combining ascorbic acid core with hydroxyisobutyl side chains at specific positions. This composite structure provides both the stability benefits of the modified molecule and the beneficial properties of the ascorbic acid framework, while the specific configuration prevents discoloration and odor.

Inventive Principle:

Principle #40Composite materials

2Stability of the object's composition

If ascorbic acid derivatives are used to improve stability, then stability is improved, but activity duration is short

Engineering Contradiction:

Improvestability over timeVSAvoidactivity duration in body

Core Design Contradiction:

Stability of the object's compositionVSDuration of action of moving object

Solution Approach 1:

The patent changes the molecular parameters by introducing hydroxyisobutyl groups that modify the pharmacokinetic properties of ascorbic acid derivatives. This structural modification extends the duration of action in the body while maintaining stability, resolving the contradiction between stability improvement and short activity duration.

Inventive Principle:

Principle #35Parameter changes

3Stability of the object's composition

If conventional ascorbic acid derivatives are used, then some stability improvement is achieved, but discoloration and odor problems persist

Engineering Contradiction:

Improvestability improvementVSAvoiddiscoloration and odor

Core Design Contradiction:

Stability of the object's compositionVSObject-generated harmful factors

Solution Approach 1:

The patent applies local quality modification by introducing hydroxyisobutyl groups at specific positions (2-position and/or 3-position) of the ascorbic acid molecule. This localized structural change provides the necessary stability improvement while the specific positioning prevents discoloration and odor generation, resolving the contradiction.

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 derivative exhibits superior stability, maintains effectiveness over long-term storage, and provides enhanced antioxidant, melanin inhibition, collagen production promotion, and hyaluronic acid production, resulting in improved cosmetic formulations with sustained whitening and moisturizing effects.

Implementation Method 1

it has superior antioxidant effect compared to conventional ascorbic acid derivatives

Methodology Applied

Scientific EffectAntioxidant effect: Oxidation

Implementation Method 2

it has superior antioxidant effect compared to conventional ascorbic acid derivatives such as glyceryl ascorbic acid

Methodology Applied

Scientific EffectMelanin production inhibition:

Implementation Method 3

it has superior antioxidant effect compared to conventional ascorbic acid derivatives such as glyceryl ascorbic acid

Methodology Applied

Scientific EffectCollagen production promotion:

Implementation Method 4

it has superior antioxidant effect compared to conventional ascorbic acid derivatives such as glyceryl ascorbic acid

Methodology Applied

Scientific EffectHyaluronic acid production:

Data Source

PatentUS20260001853A1Ascorbic acid derivative or salt thereof, and cosmetic thereof

Publication Date: 2026.01.01 SEIWA KASEI CO JP

AI summary

As a novel ascorbic acid derivative or a salt thereof that has the superior inherent functions of ascorbic acid such as a whitening action, a collagen production promoting action, and a moisture retaining action, while also being stable even when stored for a long period, demonstrating little change in color, change in smell, reduction in activity, and similar, the present invention provides an ascorbic acid derivative or a salt thereof wherein one hydrogen among the hydroxyl groups in the second position and the third position of ascorbic acid has been substituted with R—O—CH2—CH(OH)—CH2—, R—O—CH—CH(CH2OH)—, R—CH(CH2OH)—, R—CH(OH)—CH2— (R being H, an alkyl group, an alkenyl group, or a phenyl group), HO—C(CH3)2—CH2—, or HO—CH2—C(CH3)2—. The present invention also provides a cosmetic including said ascorbic acid derivative or a salt thereof.