Stabilizing Ethyl Lauroyl Arginate in Low-Alcohol Oral Rinses

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Solution Overview

Problem

Ethyl lauroyl arginate hydrochloride, a cationic surfactant effective against bacteria and fungi, lacks stability in low-alcohol or alcohol-free oral care compositions, necessitating the development of stable formulations for effective oral hygiene.

Innovation Solution

Combining ethyl lauroyl arginate hydrochloride with a source of gluconate anions and Vitamin E or its ester in an aqueous oral rinse composition, ensuring a concentration of at least 15 mM gluconate anions and less than 1% w/v of C1-C4 monoalcohol, enhances stability and maintains efficacy.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Object-affected harmful factors

If ethyl lauroyl arginate hydrochloride is used in low-alcohol or alcohol-free oral care compositions, then the composition becomes suitable for sensitive users and reduces irritation, but the stability of ethyl lauroyl arginate hydrochloride deteriorates

Engineering Contradiction:
Improveirritation to oral tissuesVSAvoidstability of ethyl lauroyl arginate hydrochloride
Core Design Contradiction:
Object-affected harmful factorsVSStability of the object's composition

Solution Approach 1:

The patent introduces gluconate salts and Vitamin E as intermediary substances that mediate between ethyl lauroyl arginate hydrochloride and the aqueous environment. These intermediaries prevent direct degradation reactions while maintaining the antimicrobial efficacy of the active ingredient in low-alcohol formulations.

Inventive Principle:
Principle #24Intermediary (Mediator)

Solution Approach 2:

The patent modifies the chemical environment by adjusting pH levels and introducing specific ions (gluconate) to create optimal stability conditions for ethyl lauroyl arginate hydrochloride. By changing these parameters, the formulation maintains stability without requiring high alcohol content.

Inventive Principle:
Principle #35Parameter changes

2Object-affected harmful factors

If the alcohol content is reduced to less than 1% w/v, then the composition becomes gentler on oral tissues, but the stability and shelf life of the composition deteriorates

Engineering Contradiction:
Improvegentleness to oral tissuesVSAvoidshelf life
Core Design Contradiction:
Object-affected harmful factorsVSDuration of action of stationary object

Solution Approach 1:

Gluconate salts serve as intermediary protective agents that prevent degradation of ethyl lauroyl arginate hydrochloride in the low-alcohol environment. These intermediaries extend shelf life by preventing oxidation and hydrolysis reactions that would otherwise occur rapidly in aqueous, low-alcohol formulations.

Inventive Principle:
Principle #24Intermediary (Mediator)

Solution Approach 2:

The patent creates a composite stabilization system combining gluconate salts with Vitamin E. This composite approach provides multiple mechanisms of protection (ionic interaction and antioxidant activity) that collectively extend shelf life in low-alcohol formulations.

Inventive Principle:
Principle #40Composite materials

3Stability of the object's composition

If encapsulation is used to improve stability of ethyl lauroyl arginate hydrochloride, then stability increases, but device complexity and formulation complexity increases

Engineering Contradiction:
Improvestability of ethyl lauroyl arginate hydrochlorideVSAvoidformulation complexity
Core Design Contradiction:
Stability of the object's compositionVSDevice complexity

Solution Approach 1:

The patent extracts the stabilization function from complex encapsulation systems and implements it through simple soluble gluconate salts and Vitamin E. This extraction approach achieves stability enhancement without the complexity of encapsulation technologies.

Inventive Principle:
Principle #2Taking out (Extraction)

4Stability of the object's composition

If cationic-compatible inorganic particulates are used, then stability improves, but manufacturing complexity and cost increases

Engineering Contradiction:
Improvestability of ethyl lauroyl arginate hydrochlorideVSAvoidmanufacturing simplicity
Core Design Contradiction:
Stability of the object's compositionVSEase of manufacture

Solution Approach 1:

The patent changes the approach from using particulate materials to using soluble gluconate salts, thereby maintaining stability benefits while dramatically simplifying manufacturing processes and reducing equipment requirements.

Inventive Principle:
Principle #35Parameter changes

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 combination stabilizes ethyl lauroyl arginate hydrochloride, maintaining its effectiveness over time, even at elevated temperatures, in low-alcohol or alcohol-free oral rinses, effectively inhibiting plaque formation and oral infections.

Implementation Method 1

combining a gluconate salt and Vitamin E allows obtaining stable low-alcohol or alcohol-free oral rinses comprising ethyl lauroyl arginate hydrochloride

Methodology Applied
Scientific EffectAntioxidation: Oxidation

Implementation Method 2

combining a gluconate salt and Vitamin E allows obtaining stable low-alcohol or alcohol-free oral rinses comprising ethyl lauroyl arginate hydrochloride

Methodology Applied
Scientific EffectIonic interaction: Ion Repulsion/Attraction

Data Source

PatentEP3348253B1Low-alcohol oral care compositions comprising ethyl lauroyl arginate
Publication Date: 2019.07.17 LACER SA
  • EP3348253B1 patent drawingFigure 1~2
  • EP3348253B1 patent drawingFigure 3
  • EP3348253B1 patent drawing

AI summary

The present invention relates to stable aqueous low-alcohol or alcohol free oral rinse compositions comprising ethyl lauroyl arginate by use of a combination comprising at least 15 mM of gluconate anions, and Vitamin E or an ester thereof.