Stannous Ion Stabilization in Aqueous Oral Care via Polyphosphate Complexation

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Solution Overview

Problem

Stannous ion sources in oral care compositions are unstable in aqueous solutions due to hydrolysis, limiting their therapeutic benefits, and existing solutions either restrict water content or use costly dual-phase systems, which are difficult to formulate and package effectively.

Innovation Solution

Combining stannous pyrophosphate, nitric acid or soluble nitrate salts with polyphosphate sources having three or more phosphate moieties, such as hexametaphosphate or phytic acid, in high-water compositions to stabilize stannous ions, allowing for effective caries prevention, dental erosion protection, and relief from hypersensitivity and malodor.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If stannous ion sources are used in aqueous oral care compositions, then therapeutic benefits (caries prevention, gingivitis reduction) are improved, but stability of the composition deteriorates due to hydrolysis and precipitation

Engineering Contradiction:
Improvetherapeutic benefitsVSAvoidstability of stannous ions
Core Design Contradiction:
ReliabilityVSStability of the object's composition

Solution Approach 1:

The patent introduces nitrate ions and polyphosphate ions as intermediary substances that mediate between stannous ions and water. These intermediaries form soluble complexes with stannous ions, preventing direct hydrolysis and precipitation. The nitrate and polyphosphate act as protective mediators that maintain stannous ion stability in aqueous environments without compromising therapeutic efficacy.

Inventive Principle:
Principle #24Intermediary (Mediator)

Solution Approach 2:

The invention creates a composite ionic system where stannous ions are combined with nitrate ions and polyphosphate ions in specific ratios. This composite approach forms a stable multi-ionic complex that maintains the therapeutic properties of stannous ions while gaining the stability benefits of the nitrate-polyphosphate system. The composite material strategy allows simultaneous achievement of both stability and therapeutic benefit.

Inventive Principle:
Principle #40Composite materials

2Stability of the object's composition

If water content is limited to maintain stannous ion stability, then stability is improved, but ease of manufacture and rheological properties deteriorate

Engineering Contradiction:
Improvestability of stannous ionsVSAvoidrheological properties
Core Design Contradiction:
Stability of the object's compositionVSEase of manufacture

Solution Approach 1:

The patent fundamentally changes the chemical parameters of the system by introducing nitrate and polyphosphate ions. This parameter change allows the composition to maintain stannous ion stability at high water contents (above 10% w/w), eliminating the need to restrict water content. The parameter change transforms the stability-waterness trade-off into a win-win situation where both stability and ease of manufacture are improved.

Inventive Principle:
Principle #35Parameter changes

3Stability of the object's composition

If dual-phase systems are used to stabilize stannous ions, then stability is improved, but device complexity and manufacturing cost increase

Engineering Contradiction:
Improvestability of stannous ionsVSAvoidsystem complexity
Core Design Contradiction:
Stability of the object's compositionVSDevice complexity

Solution Approach 1:

The invention merges multiple stabilizing functions into a single-phase aqueous system. Instead of using separate phases as in traditional dual-phase systems, the patent combines stannous ions, nitrate ions, and polyphosphate ions into one homogeneous phase. This merging eliminates the complexity of phase separation, packaging, and manufacturing while maintaining stannous ion stability through the synergistic interaction of the ionic components.

Inventive Principle:
Principle #5Merging (Combining)

4Stability of the object's composition

If polyphosphate sources with three or more phosphate moieties are combined with stannous ions, then solubility and stability are improved, but formulation complexity increases

Engineering Contradiction:
Improvesolubility and stabilityVSAvoidformulation complexity
Core Design Contradiction:
Stability of the object's compositionVSDevice complexity

Solution Approach 1:

The patent specifies optimal concentration ranges for polyphosphate sources (0.1-5% w/w) and defines the structural parameter of having three or more phosphate moieties. By establishing these clear parameter guidelines, the invention reduces formulation complexity while achieving the desired solubility and stability improvements. The parameter specifications provide a straightforward framework for formulation development.

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 achieves stable and soluble stannous ions in high-water oral care compositions, maintaining therapeutic efficacy while providing clear and translucent toothpaste aesthetics, and is more cost-effective and easier to formulate than dual-phase systems.

Implementation Method 1

a combination of stannous pyrophosphate, nitric acid or a soluble nitrate salt, and one or more polyphosphate sources, wherein the polyphosphate source comprises three or more phosphate moieties or units... results in stability of stannous, fluoride and nitrate in solution

Methodology Applied
Scientific EffectComplexation:

Implementation Method 2

stannous salts readily hydrolyze at a pH above 4, resulting in precipitation from solution... the combination... results in stability of stannous, fluoride and nitrate in solution

Methodology Applied
Scientific EffectInhibition of hydrolysis:

Data Source

PatentUS20240050332A1Oral Care Compositions and Methods
Publication Date: 2024.02.15 COLGATE PALMOLIVE CO

AI summary

This application relates to novel aqueous oral care compositions useful for combining and delivering incompatible stannous fluoride, and/or stannous chloride, and/or stannous pyrophosphate and potassium salts, with a polyphosphate source, wherein the polyphosphate source comprises three or more phosphate moieties or units, in a high-water composition, for example, to provide effective caries prevention, protection against dental erosion, relief from dental hypersensitivity, and to treat or reduce malodor.