Amorphous Calcium Phosphate Oral Care Stabilization

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Solution Overview

Problem

Current dental whitening products face challenges in delivering high concentrations of amorphous calcium phosphate (ACP) effectively due to rapid crystallization and precipitation, which limits the remineralization process and occlusion of dentine tubules, and existing gel-based systems are prone to untimely precipitation in ethanol-based varnish formulations.

Innovation Solution

A two-component oral healthcare system comprising a calcium salt and a source of phosphoric ions, with one or more amino acids as anti-crystallization agents, is used to prevent rapid crystallization of ACP, allowing for higher concentrations of ACP precursors to be delivered effectively in both gel and varnish forms, using a polar solvent carrier like water or ethanol, and incorporating basic amino acids like arginine and lysine to stabilize ACP in the oral cavity.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Quantity of substance

If high concentrations of calcium salt and phosphoric ions are used to deliver ACP, then the remineralization effect is improved, but rapid crystallization and precipitation occur reducing effectiveness

Engineering Contradiction:

Improveconcentration of ACP precursorsVSAvoidstability of ACP amorphous form

Core Design Contradiction:

Quantity of substanceVSStability of the object's composition

Solution Approach 1:

Amino acids serve as intermediary substances that mediate between calcium salts and phosphoric ions during ACP formation. They temporarily bind with calcium ions to form stable complexes, preventing premature crystallization and allowing high concentrations of ACP precursors to remain stable until application to the tooth surface.

Inventive Principle:

Principle #24Intermediary (Mediator)

Solution Approach 2:

The invention changes the chemical parameters of the formulation by introducing amino acids that alter the ionic interactions between calcium and phosphate. This modifies the supersaturation state and delays nucleation, allowing high concentrations of precursors to be delivered without untimely precipitation while maintaining the amorphous phase.

Inventive Principle:

Principle #35Parameter changes

2Stability of the object's composition

If amino acids are added as anti-crystallization agents, then ACP stability is improved, but formulation complexity increases

Engineering Contradiction:

Improvestability of ACP amorphous formVSAvoidformulation complexity

Core Design Contradiction:

Stability of the object's compositionVSDevice complexity

Solution Approach 1:

The invention modifies the chemical composition parameters by incorporating amino acids at specific concentrations (0.1-10% w/v). This parameter change provides a straightforward method to control ACP stability without requiring complex formulation systems or multiple additives, maintaining relative simplicity while achieving the desired effect.

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 system enables rapid and effective occlusion of dentine tubules and deposition of remineralizing agents on dental enamel, providing a prolonged desensitizing effect and enhanced tooth sensitivity relief, with the amino acids maintaining the amorphous character of ACP, thus overcoming the limitations of existing systems by achieving faster and more complete tubule occlusion.

Implementation Method 1

with one or more amino acids as anti-crystallization agents, is used to prevent rapid crystallization of ACP

Methodology Applied

Scientific EffectAnti-crystallization:

Implementation Method 2

Amino acids are known to the skilled person as being capable of binding to calcium ions to form stable complexes

Methodology Applied

Scientific EffectComplexation:

Implementation Method 3

ACP rapidly obliterates the dentinal tubules by rapid precipitation of calcium phosphate crystals on the surface and also inside the dentinal tubules

Methodology Applied

Scientific EffectPrecipitation: Precipitation

Implementation Method 4

The release of ions (e.g., calcium, and preferably calcium and phosphate ions) into the oral environment is known to enhance the natural remineralising capability of dental structures

Methodology Applied

Scientific EffectDiffusion: Diffusion

Data Source

PatentEP3166692B1Oral care formulation system providing amorphous calcium phosphate

Publication Date: 2019.11.06 KONINKLIJKE PHILIPS NV

AI summary

Disclosed is a system for providing an oral care active formulation that delivers amorphous calcium phosphate (ACP) to the teeth of a subject. The system comprises a component that provides calcium ions and a component that provides phosphate ions. The invention allows to obtain increased ACP concentrations as a result of the inclusion, in either or both of the components, of one or more basic amino acids. The invention also allows providing ACP via the administration of a two-component solvent-based varnish.