Amine Fluoride Stock Composition for Higher Aqueous Solubility

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Solution Overview

Problem

Existing oral hygiene compositions containing amine fluorides like olaflur face challenges due to low aqueous solubility, leading to high production and transportation costs and difficulties in achieving stable concentrations.

Innovation Solution

Incorporating an alkali salt, such as sodium chloride, into the amine fluoride solution significantly increases solubility by at least 45%, allowing for higher concentrations and more efficient production and transportation.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Quantity of substance

If amine fluoride is dissolved in water to create a stock solution, then the active agent can be used in oral care compositions, but the solubility is very low requiring high amounts of solution to carry relatively small amounts of the active agent

Engineering Contradiction:
Improveconcentration of amine fluorideVSAvoidhandling costs
Core Design Contradiction:
Quantity of substanceVSEase of manufacture

Solution Approach 1:

The patent applies parameter changes by modifying the chemical composition parameters of the stock solution. Specifically, it adjusts the pH to between 5 and 8 and incorporates specific co-solvents (polyols like propylene glycol, glycerin, or sorbitol at 5-50% v/v, and carboxylic acids like citric acid or lactic acid at 0.1-10% w/v) to dramatically increase the solubility of amine fluoride. This allows concentrations to be increased from very low levels to at least 0.1% and preferably at least 0.5% w/v, thereby reducing the volume of solution needed for transport and handling while maintaining the same amount of active agent.

Inventive Principle:
Principle #35Parameter changes

2Quantity of substance

If the concentration of amine fluoride in the stock solution is increased beyond moderate levels, then more active agent can be transported efficiently, but incomplete dissolution, precipitate formation, or gel-like structure occurs

Engineering Contradiction:
Improveconcentration of amine fluorideVSAvoidsolution stability
Core Design Contradiction:
Quantity of substanceVSReliability

Solution Approach 1:

The patent resolves this contradiction by systematically adjusting multiple parameters simultaneously: pH is controlled between 5 and 8, specific polyols are added at 5-50% v/v concentrations, and carboxylic acids are incorporated at 0.1-10% w/v. These parameter changes create a stable chemical environment that allows high concentrations of amine fluoride (at least 0.1% and preferably at least 0.5% w/v) to remain dissolved without precipitation or gel formation, ensuring solution stability while achieving high active agent loading.

Inventive Principle:
Principle #35Parameter changes

Solution Approach 2:

The patent creates a composite stock solution system combining amine fluoride with multiple co-solvents (polyols and carboxylic acids) working synergistically. The polyols (propylene glycol, glycerin, or sorbitol) and carboxylic acids (citric acid or lactic acid) form a composite solvent system that enhances the solubility capacity beyond what any single component could achieve alone, enabling stable high-concentration formulations.

Inventive Principle:
Principle #40Composite materials

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 increased solubility results in cost savings and streamlined synthesis of amine fluorides, enabling more effective oral care compositions with enhanced solubility and stability.

Implementation Method 1

The solubility of amine fluoride and/or its non hydrofluoride salt counterpart (referred to as 'tertiary amine') in water can be raised by at least 45% when an alkali salt (e.g., sodium chloride) is added to the stock solution.

Methodology Applied
Scientific EffectSolubility enhancement:

Data Source

PatentUS12544325B2Compositions and related methods
Publication Date: 2026.02.10 COLGATE PALMOLIVE CO

AI summary

The present disclosure relates to amine hydrofluorides and mixtures of these amine hydrofluorides, and to a process for the preparation of these amine hydrofluorides and their use in oral hygiene compositions.