Xylitol-Based Intra-Articular Formulation for Joint Inflammation

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Solution Overview

Problem

Current treatments for joint irritation and inflammation, particularly in the context of arthritis, are inadequate in providing effective intra-articular solutions that address the unique challenges of joint tissue absorption and hyaline cartilage, leading to suboptimal alleviation of joint irritation and inflammation.

Innovation Solution

An injectable pharmaceutical formulation comprising Xylitol as the active ingredient, combined with an anionic polymer such as sodium hyaluronate, which exhibits non-Newtonian shear thinning viscosity, is developed for intra-articular injection to reduce joint irritation and inflammation, potentially including additional anti-inflammatory agents, vitamins, or antioxidants.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If conventional intra-articular formulations are used, then joint irritation and inflammation are treated, but the formulations exhibit high viscosity and stickiness, making them difficult to inject and less effective

Engineering Contradiction:
Improveeffectiveness in reducing joint irritation and inflammationVSAvoidinjectability and viscosity characteristics
Core Design Contradiction:
ReliabilityVSEase of operation

Solution Approach 1:

The patent changes the chemical composition parameters of the formulation by using Xylitol instead of traditional osmotic agents and combining it with anionic polymers. This parameter change results in a formulation with reduced viscosity and improved injectability while maintaining therapeutic effectiveness for joint irritation and inflammation

Inventive Principle:
Principle #35Parameter changes

Solution Approach 2:

The patent creates a composite formulation by combining Xylitol with anionic polymers (such as sodium hyaluronate). This composite approach produces a formulation that exhibits non-Newtonian shear thinning behavior, allowing it to be easily injected while providing sustained therapeutic effect in the joint space

Inventive Principle:
Principle #40Composite materials

2Strength

If formulations with high molecular weight polymers are used to provide lubrication, then cartilage protection is improved, but the viscosity increases and stickiness between cartilage surfaces increases

Engineering Contradiction:
Improvelubrication and cartilage protectionVSAvoidstickiness between cartilage surfaces
Core Design Contradiction:
StrengthVSObject-affected harmful factors

Solution Approach 1:

The patent modifies the physical-chemical parameters of the polymer formulation by using anionic polymers with specific molecular weights and combining them with Xylitol. This results in a formulation that provides adequate lubrication while reducing excessive stickiness between cartilage surfaces through optimized rheological properties

Inventive Principle:
Principle #35Parameter changes

Solution Approach 2:

The Xylitol acts as an intermediary substance that modifies the interaction between the anionic polymer and cartilage surfaces. It mediates the balance between lubrication and stickiness, allowing the polymer to provide protective lubrication without causing excessive adhesion between opposing cartilage surfaces

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 formulation effectively reduces joint irritation and inflammation by providing a non-sticky, easily injectable solution with lubricant properties, as demonstrated by reduced dynamic viscosity and improved cartilage interaction, offering a surprising effectiveness for Xylitol in intra-articular applications.

Implementation Method 1

said pharmaceutical formulation further comprises an anionic polymer with molecular weight higher than 500,000 dalton in order to provide the formulation with non-newtonian shear thinning viscosity

Methodology Applied
Scientific EffectNon-Newtonian shear thinning viscosity: Non-Newtonian Fluids

Implementation Method 2

the non-Newtonian (salt free) formulation was less sticky than the usual formulations. In 24 measurements (Load: 10N, speed of movement 1 mm/sec., temperature 36-37° C.) the dynamic viscosity coefficient of the non-Newtonian (isotonicity by polyol) formulation was 0.03759±0.01481

Methodology Applied
Scientific EffectShear thinning: Shear Thinning

Implementation Method 3

said Xylitol is in isotonic concentration

Methodology Applied
Scientific EffectIsotonicity: Osmotic Pressure

Data Source

PatentUS9913808B2Injectable pharmaceutical compositions for the treatment of joints
Publication Date: 2018.03.13 SEGAL

AI summary

The present invention relates to an injectable pharmaceutical formulation for the alleviation or reduction of joint irritation or for the reduction of worsening of existing joint inflammation, formulated for intra-articular injection comprising an active polyol ingredient, which polyol active ingredient is xylitol. Use of the intra-articular injectable formulations for the treatment of joint diseases or conditions including arthritis is described.