Oral Composition Alpha-Gel Adsorption

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Solution Overview

Problem

Medicinal ingredients like glycyrrhetinic acid and tocopherol in oral compositions have low solubility and stability issues, limiting their effectiveness and regulatory compliance due to potential foreign taste and restricted usage, necessitating enhanced adsorption performance on gums and oral mucosa.

Innovation Solution

An oral composition comprising specific amounts of higher alcohols, surfactants, and water, forming an α-gel structure to increase the adsorption of oil-soluble medicinal ingredients such as glycyrrhetinic acid and tocopherol, ensuring effective embedding and prolonged action while adhering to regulatory limits.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If the amount of oil-soluble medicinal ingredients (glycyrrhetinic acid, tocopherol) is increased to enhance medicinal effects, then the pharmacological effectiveness is improved, but foreign taste occurs and regulatory compliance deteriorates

Engineering Contradiction:
Improvepharmacological effectivenessVSAvoidforeign taste
Core Design Contradiction:
ReliabilityVSObject-generated harmful factors

Solution Approach 1:

The patent uses higher alcohols (12-22 carbon atoms) and surfactants as intermediary substances to form an α-gel structure that mediates between the oil-soluble medicinal ingredients and the aqueous environment. This gel structure allows effective delivery of medicinal ingredients without requiring excessive amounts that would cause foreign taste, thus resolving the contradiction between pharmacological effectiveness and sensory acceptability.

Inventive Principle:
Principle #24Intermediary (Mediator)

Solution Approach 2:

The patent changes the physical state and organizational structure of the formulation by forming an α-gel phase with specific molecular arrangement. This parameter change in the system's physical state allows for controlled release and reduced irritation while maintaining effective medicinal ingredient concentrations within regulatory limits.

Inventive Principle:
Principle #35Parameter changes

2Reliability

If the amount of oil-soluble medicinal ingredients is increased to overcome low solubility, then the medicinal effect is enhanced, but storage stability deteriorates

Engineering Contradiction:
Improvemedicinal effectVSAvoidstorage stability
Core Design Contradiction:
ReliabilityVSStability of the object's composition

Solution Approach 1:

The patent creates a composite system consisting of higher alcohols, surfactants, and oil-soluble medicinal ingredients organized in an α-gel structure. This composite material approach allows the incorporation of oil-soluble medicinal ingredients with maintained solubility and improved storage stability, as the gel matrix provides a stable environment that prevents precipitation and degradation.

Inventive Principle:
Principle #40Composite materials

3Stability of the object's composition

If conventional surfactants and oil agents are used to improve solubility of medicinal ingredients, then dispersibility is enhanced, but the medicinal ingredient adsorption to gums and oral mucosa is insufficient

Engineering Contradiction:
ImprovedispersibilityVSAvoidadsorption performance
Core Design Contradiction:
Stability of the object's compositionVSReliability

Solution Approach 1:

The patent applies local quality by creating a specific α-gel structure with particular molecular arrangement and properties in the formulation. This localized structural organization provides both good dispersibility and enhanced adsorption performance to gums and oral mucosa, as the gel structure facilitates close contact and binding at the application site while maintaining overall formulation stability.

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 composition effectively enhances the adsorption of medicinal ingredients to the gums and oral mucosa, improving their pharmacological effects and stability, thus overcoming solubility and regulatory constraints.

Implementation Method 1

when an oral composition comprises specific higher alcohol and surfactant in specific amounts, respectively, in addition to an oil-soluble medicinal ingredient, such as glycyrrhetinic acid, and water such that the content of oil agent other than the oil-soluble medicinal ingredient, higher alcohol, and flavoring agent is restricted with respect to the content of the higher alcohol and that the content of an abrasive powder comprising a polyvalent metal is restricted, the amount of the oil-soluble medicinal ingredient adsorbed to the gums and oral mucosa can be effectively increased

Methodology Applied
Scientific Effectα-gel formation: Gel

Implementation Method 2

the amount of the oil-soluble medicinal ingredient adsorbed to the gums and oral mucosa can be effectively increased

Methodology Applied
Scientific EffectAdsorption: Adsorption

Data Source

PatentEP3375432B1Oral cavity composition
Publication Date: 2020.10.21 KAO CORP
  • EP3375432B1 patent drawingFigure 1

AI summary

The present invention relates to an oral composition showing increased adsorption performance of an oil-soluble medicinal ingredient such as glycyrrhetinic acid and tocopherol to the gums and oral mucosa. The invention relates to an oral composition comprising the following ingredients (A), (B), (C), and (D): (A) 0.01 mass% or more and 2.5 mass% or less of one or more oil-soluble medicinal ingredients selected from the group consisting of glycyrrhetinic acid, tocopherol, and a tocopherol derivative; (B) 4 mass% or more and 30 mass% or less of a higher alcohol having 12 or more and 22 or less carbon atoms comprising (b1) cetanol and (b2) stearyl alcohol; (C) 0.1 mass% or more and 10 mass% or less of a surfactant including one or more selected from the group comprising of (c1) a nonionic surfactant selected from the group consisting of sorbitan fatty acid ester and polyoxyethylene sorbitan fatty acid ester, and (c2) an anionic surfactant being a fatty acid having 12 or more and 22 or less carbon atoms or a salt thereof; and (D) water, wherein a mass ratio of the content of (E) an oil agent other than ingredients (A), (B), and (C) and a flavoring agent to the content of ingredient (B), ((E)/(B)), is less than 1; and the content of (F) an abrasive powder comprising a polyvalent metal is 5 mass% or less.