Cyclodextrin Stabilization of Chondroitin Sulfate and Glucosamine Solutions

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Solution Overview

Problem

Existing oral solutions of chondroitin sulfate and glucosamine tend to yellow and are not stable, leading to organoleptic issues and reduced effectiveness due to oxidation and bacterial growth, despite the use of preservatives like sodium benzoate and antioxidants.

Innovation Solution

Incorporating cyclodextrin into the solution with chondroitin sulfate, glucosamine, antioxidants, and preservatives to prevent yellowing and maintain stability, with specific concentrations of chondroitin sulfate, N-acetylated glucosamine, antioxidants, and preservatives, along with optional sweetening and flavoring agents, to create a stable and effective oral formulation.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Ease of operation

If aqueous solution of chondroitinsulfate and glucosamine is prepared for oral administration, then immediate availability and ease of administration is improved, but the solution turns yellow over time due to oxidation and bacterial growth, leading to organoleptic deterioration

Engineering Contradiction:
Improveease of administrationVSAvoidstability of solution
Core Design Contradiction:
Ease of operationVSStability of the object's composition

Solution Approach 1:

Cyclodextrin acts as a mediator substance that forms inclusion complexes with chondroitinsulfate and glucosamine, protecting them from oxidation and bacterial degradation. The cyclodextrin molecules create a protective cavity structure that shields the active ingredients from harmful environmental factors while maintaining solution stability and organoleptic properties throughout the shelf life.

Inventive Principle:
Principle #24Intermediary (Mediator)

2Stability of the object's composition

If preservatives and antioxidants are added to prevent yellowing and bacterial growth, then stability is improved, but the formulation complexity and potential adverse effects increase

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

Solution Approach 1:

Cyclodextrin serves as a gentle intermediary protective agent that prevents degradation through physical encapsulation rather than chemical intervention. This approach avoids the need for multiple preservatives and antioxidants, simplifying the formulation while reducing the risk of adverse effects associated with conventional stabilizing agents.

Inventive Principle:
Principle #24Intermediary (Mediator)

Solution Approach 2:

The formulation converts the potential harm of water (which causes oxidation and bacterial growth) into a benefit by using cyclodextrin to create a protected aqueous environment. The water-based solution remains stable because cyclodextrin transforms the harmful interactions between water and active ingredients into a protective mechanism.

Inventive Principle:
Principle #22Blessing in disguise (Convert harm into benefit)

3Reliability

If high concentrations of chondroitinsulfate and glucosamine are used to maximize therapeutic effect, then effectiveness is improved, but oxidation and yellowing occur more rapidly

Engineering Contradiction:
ImproveeffectivenessVSAvoidstability of solution
Core Design Contradiction:
ReliabilityVSStability of the object's composition

Solution Approach 1:

Cyclodextrin provides a protective environment that allows high concentrations of chondroitinsulfate and glucosamine to be formulated without accelerated degradation. The inclusion complexes formed by cyclodextrin prevent oxidative reactions even at elevated active ingredient levels, maintaining both effectiveness and stability simultaneously.

Inventive Principle:
Principle #24Intermediary (Mediator)

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 addition of cyclodextrin stabilizes the solution, preventing yellowing and maintaining the integrity of the active ingredients, ensuring longer shelf life and improved organoleptic properties while maintaining the effectiveness of chondroitin sulfate and glucosamine.

Implementation Method 1

Incorporating cyclodextrin into the solution with chondroitin sulfate, glucosamine, antioxidants, and preservatives to prevent yellowing and maintain stability

Methodology Applied
Scientific EffectInclusion complex formation: Solvation

Implementation Method 2

Existing oral solutions of chondroitin sulfate and glucosamine tend to yellow and are not stable, leading to organoleptic issues and reduced effectiveness due to oxidation and bacterial growth

Methodology Applied
Scientific EffectOxidation prevention: Oxidation

Implementation Method 3

despite the use of preservatives like sodium benzoate and antioxidants

Methodology Applied
Scientific EffectPreservation: Preservative

Data Source

PatentEP2155161B1Stable liquid composition of chondroitinsulfate and glucosamine
Publication Date: 2016.12.28 APHARM SRL

AI summary

The invention concerns a stable liquid composition comprising a glycosaminoglycan and/or optionally N-acetylated glucosamine and a cyclodextrin for oral administration.