Oral Care Compositions Stabilizing Stannous Ions with Dentate Ligands

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Solution Overview

Problem

Stannous fluoride in oral care compositions is challenging to formulate due to reactivity with other components, leading to either under-stabilization or over-stabilization, which reduces the availability of bioactive stannous ions.

Innovation Solution

An oral care composition comprising a mixture of dentate ligands, including a first polydentate ligand such as oxalic acid and a monodentate ligand like lactic acid, with a stannous ions to ligand ratio in the range of 1:3 to 1:4, optimized to stabilize stannous ions while maintaining their reactivity.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Stability of the object's composition

If stannous fluoride is stabilized with chelants in oral care compositions, then stability of stannous ions is improved, but availability of bioactive stannous ions deteriorates

Engineering Contradiction:
Improvestability of stannous ionsVSAvoidavailability of bioactive stannous ions
Core Design Contradiction:
Stability of the object's compositionVSQuantity of substance

Solution Approach 1:

The invention segments the chelating function into two distinct components: a polydentate ligand (providing at least 3 carboxylate groups) and a monodentate ligand (providing 1 carboxylate group). This segmentation allows the polydentate ligand to provide structural stability through multiple binding sites while the monodentate ligand modulates the complex to maintain bioavailability, resolving the contradiction between stability and availability

Inventive Principle:
Principle #1Segmentation

Solution Approach 2:

The invention creates a composite chelating system combining polydentate and monodentate ligands in specific molar ratios (0.5:1 to 2:1 polydentate:monodentate). This composite approach leverages the strong binding capability of polydentate ligands for stability while the monodentate component prevents excessive stabilization, maintaining the balance between stability and bioavailability of stannous ions

Inventive Principle:
Principle #40Composite materials

2Reliability

If stannous fluoride is formulated with carboxylate-containing compounds, then reactivity with other components is reduced, but amount of available stannous ions decreases

Engineering Contradiction:
Improvereactivity control of stannous fluorideVSAvoidamount of available stannous ions
Core Design Contradiction:
ReliabilityVSQuantity of substance

Solution Approach 1:

The invention optimizes the molar ratio parameters of polydentate to monodentate ligands (specifically 0.5:1 to 2:1 ranges) to achieve the desired balance. By adjusting these stoichiometric parameters, the formulation controls the degree of chelation to provide sufficient stability against unwanted reactions while maintaining adequate availability of stannous ions for oral care benefits

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 composition achieves optimal bioavailability and stability of stannous ions, enhancing hydroxyapatite protection against citric acid challenge and improving fluoride uptake, thereby providing effective oral care benefits.

Implementation Method 1

a mixture of dentate ligands comprising: i. a first polydentate ligand, wherein the first polydentate ligand is oxalic acid, a salt thereof, or a combination thereof; and ii. a monodentate ligand, wherein the monodentate ligand is lactic acid or a salt thereof

Methodology Applied
Scientific EffectChelation:

Implementation Method 2

The stannous ion source can deposit on the tooth surfaces creating an acid-resistant coating that helps the teeth resist dissolution from dietary acids

Methodology Applied
Scientific EffectDeposition: Deposition (physical)

Implementation Method 3

They can also include a fluoride source that helps the teeth resist plaque acids for the prevention of cavities. Stannous fluoride provides both stannous and fluoride ions for the protection of teeth from dietary and plaque acids

Methodology Applied
Scientific EffectFluoride uptake:

Data Source

PatentUS20250120893A1Oral care compositions comprising dicarboxylic acid
Publication Date: 2025.04.17 PROCTER & GAMBLE CO
  • US20250120893A1 patent drawing
  • US20250120893A1 patent drawing
  • US20250120893A1 patent drawing

AI summary

Oral care compositions are disclosed comprising a mixture of dentate ligands including mono-, di- and/or tetracarboxylic acid(s) as well as a stannous ion source and a fluoride ions source, such as stannous fluoride. Said oral care compositions show an ability to prevent and/or treat dental erosion and/or carics.