Vitamin E Glycoside Aqueous Composition Using 1,2-Hexanediol
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Solution Overview
Problem
Glycosides of vitamin E have low solubility in water, making it difficult to formulate them into an aqueous composition for skin applications.
Innovation Solution
An aqueous composition containing glycosides of vitamin E, 1,2-hexanediol, and water, with specific mass percentages of each component, which enhances solubility and stability of the glycosides, particularly tocopheryl glucoside, and includes additional components like pharmacologically acceptable carriers for skin preparations.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Reliability
If glycoside of vitamin E is used as an active ingredient, then anti-allergic and anti-inflammatory effects are improved, but water solubility deteriorates
Solution Approach 1:
The patent introduces 1,2-hexanediol as an intermediary substance that acts as a solubilizing agent between the hydrophobic glycoside of vitamin E and water. This mediator enables the formation of stable aqueous compositions by bridging the solubility gap, allowing the active ingredient to be effectively delivered in water-based formulations without compromising its biological activity.
Solution Approach 2:
The patent modifies the chemical environment parameters of the formulation by adjusting the concentration ratios of 1,2-hexanediol to water and glycoside of vitamin E. By optimizing these parameters (1,2-hexanediol at 0.1-10%, glycoside at 0.01-2%), the formulation achieves stable solubility while maintaining the therapeutic effects of the active ingredient.
2Reliability
If concentration of glycoside of vitamin E is increased to improve efficacy, then therapeutic effect is improved, but solubility in water deteriorates
Solution Approach 1:
1,2-hexanediol serves as a solubilizing intermediary that enables higher concentrations of glycoside of vitamin E to be dissolved in aqueous formulations. The intermediary substance expands the solubility ceiling, allowing therapeutic concentrations (0.01-2% glycoside) to be achieved while maintaining complete solubility and formulation stability.
Solution Approach 2:
The patent creates a composite aqueous system combining water, 1,2-hexanediol, and glycoside of vitamin E in specific proportions. This composite formulation leverages the complementary properties of each component: water provides the aqueous base, 1,2-hexanediol provides solubilizing capability, and the glycoside provides therapeutic activity, achieving both high concentration and full solubility simultaneously.
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 promotes the expression of TRPV4, CLDN1, and OCL genes, improving skin barrier function and moisturizing properties, reducing transepidermal water loss, and enhancing skin smoothness.
Implementation Method 1
Since a glycoside of vitamin E (tocopherol or tocotrienol) has significantly low solubility in water, it is difficult to prepare the glycoside of vitamin E as an aqueous composition. The present invention includes an aqueous composition containing a glycoside of vitamin E, 1,2-hexanediol, and water.
Data Source
AI summary
An aqueous composition contains a glycoside of vitamin E, represented by General Formula (1), 1,2-hexanediol, and water. In Formula (1), R1, R2, and R3 each independently represents a hydrogen atom or a methyl group, Rx represents a monosaccharide, and Ry represents a group represented by Formula (Ry-1) or (Ry-2). * represents a bonding site to a carbon atom to which Ry in General Formula (1) is bonded. An external preparation for skin, containing the aqueous composition, is also provided.