Chelator-Free Ophthalmic Composition for Corneal Defect Treatment

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Solution Overview

Problem

Existing ophthalmic compositions for treating corneal and conjunctival defects often cause an astringent effect due to the presence of chelating agents like EDTA, leading to discomfort and ion imbalance in the eye.

Innovation Solution

An ophthalmic composition devoid of chelating agents, comprising a mixture of hyaluronic acid, an ethylene oxide/propylene oxide block copolymer, boric acid, and tris(hydroxymethyl)aminomethane to adjust pH and osmolality, ensuring physiological compatibility and improved mucoadhesive properties.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If chelating agents like EDTA are used in ophthalmic compositions, then the composition can effectively treat corneal and conjunctival defects, but the chelating agents cause an astringent effect and discomfort by sequestering ions from the cornea

Engineering Contradiction:
Improvetreatment effectivenessVSAvoidastringent effect and discomfort
Core Design Contradiction:
ReliabilityVSObject-affected harmful factors

Solution Approach 1:

The patent removes chelating agents (EDTA, citrate salts) from the ophthalmic composition to eliminate the harmful astringent effect caused by ion sequestration, while maintaining treatment effectiveness through alternative formulations with appropriate pH and osmolality adjustments

Inventive Principle:
Principle #2Taking out (Extraction)

Solution Approach 2:

The patent adjusts critical parameters including pH (using boric acid and tromethamine buffer system), osmolality, and ionic composition to achieve physiological compatibility and reduce discomfort while preserving therapeutic efficacy for corneal and conjunctival defects

Inventive Principle:
Principle #35Parameter changes

2Stability of the object's composition

If chelating agents are present in the ophthalmic composition, then the composition can maintain stability, but the chelating agents alter the tonicity of the eye causing burning sensation

Engineering Contradiction:
Improvecomposition stabilityVSAvoidtonicity alteration and burning sensation
Core Design Contradiction:
Stability of the object's compositionVSObject-affected harmful factors

Solution Approach 1:

The patent eliminates chelating agents that cause harmful tonicity alterations and burning sensations, replacing them with a buffer system based on boric acid and tromethamine that maintains composition stability without adverse effects on ocular tonicity

Inventive Principle:
Principle #2Taking out (Extraction)

Solution Approach 2:

The patent optimizes pH and osmolality parameters through the boric acid-tromethamine buffer system to ensure physiological compatibility and prevent burning sensation while maintaining formulation stability

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 composition is more tolerable and effective in treating corneal and conjunctival defects, reducing discomfort and maintaining a stable, long-lasting presence on the eye surface due to its improved mucoadhesive properties.

Implementation Method 1

the mixture comprises, or alternatively, consists of: (a) at least two viscosity adjusting agents; a first viscosity adjusting agent (a.1) selected from among the group comprising or, alternatively, consisting of hyaluronic acid, a salt thereof and mixtures thereof; a second viscosity adjusting agent (a.2) comprising or, alternatively, consisting of an ethylene oxide/propylene oxide block copolymer

Methodology Applied
Scientific EffectMucoadhesion: Adhesive

Implementation Method 2

a buffer agent which is a mixture of boric acid and tris(hydroxymethyl)aminomethane for adjusting the pH to a pH value comprised from 6,5 to 8 ± 0,1

Methodology Applied
Scientific EffectBuffering:

Data Source

PatentEP3972564B1Ophthalmic composition devoid of chelators for use in a method for the treatment of an ocular disorder
Publication Date: 2025.04.02 NTC SRL

AI summary

The present invention regards an ophthalmic composition comprising a mixture for use in a method for the treatment of a disorder or a disease associated with a corneal epithelial defect and/or a conjunctival defect in a subject.