Rutin Solubilization via Polyhydroxyalkyl Alcohols

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Solution Overview

Problem

Rutin, an anti-oxidant and anti-inflammatory agent, is poorly soluble in water, limiting its effective delivery and efficacy in oral care formulations for conditions like gingivitis and periodontitis.

Innovation Solution

The use of polyhydroxyalkyl alcohols, specifically propylene glycol and sorbitol, enhances rutin's solubility in oral care compositions, allowing for higher concentrations and improved delivery to the oral cavity, particularly through the formation of a pre-mix that dissolves rutin before combining with other ingredients.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If rutin is used in oral care formulations, then anti-oxidant and anti-inflammatory effects are achieved, but water solubility is poor limiting delivery effectiveness

Engineering Contradiction:
Improveanti-oxidant and anti-inflammatory efficacyVSAvoidwater solubility
Core Design Contradiction:
ReliabilityVSQuantity of substance

Solution Approach 1:

The patent uses polyhydroxyalkyl alcohols (propylene glycol, sorbitol, glycerol) as intermediary solubilizing agents that mediate between the hydrophobic rutin and the aqueous oral care formulation environment. These intermediaries form mixed solvent systems that increase rutin's solubility without compromising its bioactive properties, thereby resolving the contradiction between maintaining efficacy and improving solubility.

Inventive Principle:
Principle #24Intermediary (Mediator)

Solution Approach 2:

The patent changes the physical-chemical parameters of the formulation system by introducing polyhydroxyalkyl alcohols that alter the solvent properties. By adjusting the type and concentration of polyhydroxyalkyl alcohol (e.g., 5-20% propylene glycol, 5-15% sorbitol), the solubility parameter of rutin is modified, enabling higher concentrations of rutin to be delivered effectively in the oral care composition.

Inventive Principle:
Principle #35Parameter changes

2Quantity of substance

If polyhydroxyalkyl alcohols are added to enhance rutin solubility, then water solubility increases, but formulation complexity increases

Engineering Contradiction:
Improvewater solubilityVSAvoidformulation complexity
Core Design Contradiction:
Quantity of substanceVSDevice complexity

Solution Approach 1:

The patent optimizes the concentration parameters of polyhydroxyalkyl alcohols to achieve effective solubility enhancement without excessive formulation complexity. By establishing specific concentration ranges (e.g., propylene glycol 5-20%, sorbitol 5-15%, glycerol 5-20%), the formulation achieves rutin solubility improvement while maintaining manageable complexity through defined compositional parameters.

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

This approach significantly increases rutin's solubility and effectiveness in oral care products, enabling more efficient reduction of inflammation and oxidative damage in the mouth, and promoting healing of oral tissues.

Implementation Method 1

dissolving rutin in a solvent to form a pre-mix; wherein the solvent of the step (a) comprises a first and second polyhydroxyalkyl alcohol

Methodology Applied
Scientific EffectSolvation: Solvation

Data Source

PatentEP3082728B1Method for solubilizing rutin with polyhydroxyalkyl alcohols
Publication Date: 2020.02.19 COLGATE PALMOLIVE CO
  • EP3082728B1 patent drawing

AI summary

The present invention generally relates to oral care compositions which enhance the solubility of rutin comprising rutin and at least one polyhydroxyalkyl alcohol. The present invention also relates to methods for use and manufacturing said oral care compositions.