Stannous Ion Stabilization in Oral Compositions via Citrate Complexation

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Solution Overview

Problem

Oral compositions containing stannous ions for treating biofilm-related oral health issues face stability problems due to precipitation in neutral pH solutions or with water, leading to a decrease in antibacterial activity over time, especially during long-term storage.

Innovation Solution

An oral composition comprising water, a stannous ion source, casein phosphopeptide-amorphous calcium phosphate (CPP-ACP), and at least citric acid or a citric acid salt, which stabilizes stannous ions and maintains high concentrations of stannous, fluorine, calcium, and inorganic phosphate ions even after long-term storage, enhancing antibacterial and remineralization activities.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If stannous ions are used in an aqueous solution for antibacterial activity, then the composition can treat biofilm-related oral health issues, but the stannous ions precipitate in neutral pH solutions or during storage, leading to loss of antibacterial activity

Engineering Contradiction:
Improveantibacterial activityVSAvoidstannous ion stability
Core Design Contradiction:
ReliabilityVSStability of the object's composition

Solution Approach 1:

The patent introduces citric acid or citric acid salt as an intermediary substance that forms a stable complex with stannous ions. This complex acts as a mediator that prevents direct precipitation of stannous ions while maintaining their antibacterial activity, thus resolving the contradiction between stability and effectiveness

Inventive Principle:
Principle #24Intermediary (Mediator)

Solution Approach 2:

The patent changes the chemical environment parameters by adjusting pH to acidic range (5.0-7.0) and introducing citric acid/citrate buffer system. This parameter change prevents stannous ion precipitation by maintaining conditions where the ions remain soluble and stable throughout storage

Inventive Principle:
Principle #35Parameter changes

2Duration of action of stationary object

If the oral composition is stored for long-term, then it can be used over extended periods, but the concentration of stannous ions gradually decreases due to precipitation and degradation

Engineering Contradiction:
Improvestorage durationVSAvoidstannous ion concentration
Core Design Contradiction:
Duration of action of stationary objectVSQuantity of substance

Solution Approach 1:

The patent applies preliminary action by forming a stable complex between stannous ions and citric acid/citrate before storage. This pre-complexation prevents degradation and precipitation during storage, maintaining ion concentration throughout the shelf life of the product

Inventive Principle:
Principle #10Preliminary action

Solution Approach 2:

The citric acid/citrate complex acts as a protective intermediary that shields stannous ions from degradation pathways during storage, including oxidation and precipitation, thereby preserving the quantity of active stannous ions over extended storage periods

Inventive Principle:
Principle #24Intermediary (Mediator)

3Ease of operation

If the pH is adjusted to neutrality for comfort, then the composition is more comfortable for oral use, but stannous ions precipitate and lose stability

Engineering Contradiction:
Improveoral comfortVSAvoidstannous ion stability
Core Design Contradiction:
Ease of operationVSStability of the object's composition

Solution Approach 1:

The patent optimizes pH parameters to a specific range (5.0-7.0) that balances comfort and stability. Within this range, the citrate buffer system maintains acidic conditions sufficient to prevent stannous ion precipitation while remaining comfortable for oral application

Inventive Principle:
Principle #35Parameter changes

Solution Approach 2:

The citric acid/citrate buffer system serves as a mediating chemical environment that allows the composition to maintain stability at a pH level comfortable for oral use, preventing ion precipitation without requiring extreme acidity that would compromise comfort

Inventive Principle:
Principle #24Intermediary (Mediator)

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 maintains high concentrations of stannous and other ions, ensuring sustained antibacterial and anti-caries activity, with improved stability and effectiveness over time, even after storage at elevated temperatures.

Implementation Method 1

compositions limiting the amount of water or using a chelating effect have been proposed

Methodology Applied
Scientific EffectChelating effect:

Implementation Method 2

casein phosphopeptide-amorphous calcium phosphate (CPP-ACP), and at least citric acid or a citric acid salt

Methodology Applied
Scientific EffectComplexation:

Data Source

PatentEP3988077B1Oral composition
Publication Date: 2023.07.12 GC LAB AMERICA INC

AI summary

An oral composition for treating diseases in the mouth caused by formulation of biofilms on teeth. The oral composition includes water, stannous ion source, casein phosphopeptide-amorphous calcium phosphate, and at least citric acid or a citric acid salt.