Stannous-Ascorbyl Phosphate Complexes for Oral Care Stability

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Solution Overview

Problem

Stannous ions in oral care compositions are unstable in aqueous solutions above a pH of 4, leading to precipitation and loss of therapeutic properties, limiting their use due to formulation and cost constraints in dual-phase systems and low-water compositions.

Innovation Solution

Formation of complexes between stannous or stannic ions and ascorbyl phosphate, which provides stability and solubility, allowing for effective antibacterial activity and protection against erosion, by forming stannous-ascorbyl phosphate (SAP2) or stannic-ascorbyl phosphate (SAP4) complexes, optionally with additional fluoride, zinc, and amino acid sources in oral care formulations.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If stannous ion sources are used in oral care compositions, then antibacterial efficacy and protection against gingivitis are improved, but stability in aqueous solutions deteriorates

Engineering Contradiction:
Improveantibacterial efficacyVSAvoidstability in aqueous solution
Core Design Contradiction:
ReliabilityVSStability of the object's composition

Solution Approach 1:

The patent introduces ascorbyl phosphate as an intermediary substance that forms a stable complex with stannous ions. This complex acts as a mediator that delivers stannous ions to the oral cavity while preventing their premature oxidation and precipitation in the aqueous formulation, thus maintaining both stability and efficacy

Inventive Principle:
Principle #24Intermediary (Mediator)

Solution Approach 2:

The invention creates a composite material system where stannous ions are combined with ascorbyl phosphate to form a stable complex. This composite approach allows the formulation to maintain stannous ions in a stable, soluble state while preserving their antibacterial activity, overcoming the limitations of using stannous ions alone

Inventive Principle:
Principle #40Composite materials

2Stability of the object's composition

If water content is reduced to improve stannous ion stability, then stability is improved, but ease of formulation and rheological properties deteriorate

Engineering Contradiction:
Improvestannous ion stabilityVSAvoidformulation ease and rheology
Core Design Contradiction:
Stability of the object's compositionVSEase of manufacture

Solution Approach 1:

The invention changes the chemical parameters of the system by introducing ascorbyl phosphate, which fundamentally alters the behavior of stannous ions in aqueous solution. This parameter change allows the formulation to maintain high water content for good rheology while achieving stannous ion stability through complex formation rather than water reduction

Inventive Principle:
Principle #35Parameter changes

3Stability of the object's composition

If dual phase systems are used to improve stannous ion stability, then stability is improved, but manufacturing cost and complexity increase

Engineering Contradiction:
Improvestannous ion stabilityVSAvoidformulation complexity
Core Design Contradiction:
Stability of the object's compositionVSDevice complexity

Solution Approach 1:

The patent achieves stannous ion stability in a homogeneous single-phase aqueous formulation by using ascorbyl phosphate complex formation. This eliminates the need for complex dual-phase systems, reducing manufacturing complexity while maintaining stability and allowing for easier production and packaging

Inventive Principle:
Principle #33Homogeneity

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 complexes offer enhanced stability and delivery of stannous or stannic ions, providing improved antibacterial activity, protection against erosion, and reduced bacterial colonization, while maintaining stability and solubility in aqueous media, thus overcoming the limitations of traditional stannous ion sources.

Implementation Method 1

stannous and stannic ions can form a complex with ascorbyl phosphate

Methodology Applied
Scientific EffectComplex formation: Chemical Bonding

Implementation Method 2

the stannous is not only bonded with the phosphate group like other phosphate complex but is also bonded to the hydroxyl group on the ascorbyl portion

Methodology Applied
Scientific EffectChelation: Chemical Bonding

Implementation Method 3

the formation of the complex allows the stannous or stannic to avoid being oxidized too quickly

Methodology Applied
Scientific EffectOxidation prevention: Oxidation

Data Source

PatentEP3724201B1Novel compounds
Publication Date: 2022.02.02 COLGATE PALMOLIVE CO
  • EP3724201B1 patent drawingFigure 1
  • EP3724201B1 patent drawingFigure 2
  • EP3724201B1 patent drawingFigure 3

AI summary

Disclosed herein are stannous-ascorbyl phosphate and stannic-asorbyl phosphate complexes, oral care compositions stannous-ascorbyl phosphate and stannic-asorbyl phosphate complexes, and methods of making and using the same.