Hypertonic Ophthalmic Ointment With Emulsified Salt Diffusion

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Solution Overview

Problem

Existing hypertonic ophthalmic ointments face issues with incomplete diffusion of hydrophilic components like sodium chloride due to their lipophilic nature, leading to prolonged residence time and undesirable eyelid sticking, along with stinging and low transparency, which limits their effectiveness and patient comfort.

Innovation Solution

A hypertonic ophthalmic ointment formulation with a hydrophilic phase containing sodium chloride and hyaluronic acid, dispersed in a lipophilic phase using an emulsifier, allowing for complete diffusion and reducing eyelid sticking, while maintaining prolonged residence time.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Duration of action of moving object

If a lipophilic ointment base is used to provide prolonged residence time in the eye, then the residence time is extended, but the hydrophilic components like sodium chloride do not diffuse completely due to immiscibility with the lipophilic matrix

Engineering Contradiction:
Improveresidence timeVSAvoiddiffusion completeness
Core Design Contradiction:
Duration of action of moving objectVSReliability

Solution Approach 1:

The ointment is divided into two distinct phases: a lipophilic phase providing prolonged residence time and a hydrophilic phase containing sodium chloride and hyaluronic acid for complete diffusion. The emulsifier stabilizes this segmented structure, allowing each phase to fulfill its specific function without compromising the other.

Inventive Principle:
Principle #1Segmentation

Solution Approach 2:

An emulsifier is introduced as an intermediary substance between the lipophilic and hydrophilic phases. This emulsifier enables stable dispersion of the hydrophilic phase within the lipophilic matrix, facilitating complete diffusion of hydrophilic components while maintaining prolonged residence time through the lipophilic base.

Inventive Principle:
Principle #24Intermediary (Mediator)

2Reliability

If a hypertonic ointment with high osmotic component is used to treat corneal oedema, then therapeutic effect is improved, but stinging and discomfort increase

Engineering Contradiction:
Improvetherapeutic effectVSAvoidstinging
Core Design Contradiction:
ReliabilityVSObject-affected harmful factors

Solution Approach 1:

Hyaluronic acid serves as a mediator between the hypertonic sodium chloride and the corneal tissue. It facilitates the osmotic action of sodium chloride while simultaneously reducing stinging and discomfort, allowing the therapeutic effect to be achieved with minimal harm to the patient.

Inventive Principle:
Principle #24Intermediary (Mediator)

Solution Approach 2:

The addition of hyaluronic acid changes the physical and chemical parameters of the ointment formulation. It modifies the interaction between the hypertonic solution and the corneal epithelium, enabling effective osmotic treatment while reducing harmful stinging effects through altered surface properties and enhanced compatibility.

Inventive Principle:
Principle #35Parameter changes

3Loss of time

If a lipophilic ointment base is used to reduce frequency of administration, then administration frequency is reduced, but eyelid sticking occurs due to prolonged residence time

Engineering Contradiction:
Improveadministration frequencyVSAvoideyelid opening
Core Design Contradiction:
Loss of timeVSEase of operation

Solution Approach 1:

The ointment separates the functions of prolonged residence and ease of eyelid opening into different phases. The lipophilic phase provides extended residence time reducing administration frequency, while the hydrophilic phase with hyaluronic acid ensures easy eyelid opening by preventing sticking, thus resolving the contradiction between these two requirements.

Inventive Principle:
Principle #1Segmentation

4Illumination intensity

If aqueous eyedrops are used for daytime use, then transparency and comfort are improved, but residence time is short due to leaching action of lacrimal fluid

Engineering Contradiction:
ImprovetransparencyVSAvoidresidence time
Core Design Contradiction:
Illumination intensityVSDuration of action of moving object

Solution Approach 1:

The invention merges the advantages of both aqueous and lipophilic formulations into a single emulsified ointment system. It combines the transparency and comfort of aqueous-based formulations with the prolonged residence time of lipophilic ointments, creating a hybrid product that achieves both goals simultaneously.

Inventive Principle:
Principle #5Merging (Combining)

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 ointment achieves improved diffusion of sodium chloride, reduces eyelid sticking, and enhances patient comfort by facilitating easier eyelid opening, thus providing effective treatment for corneal oedema without compromising residence time.

Implementation Method 1

an ointment comprising an hydrophilic phase dispersed in a lipophilic phase by means of an emulsifier

Methodology Applied
Scientific EffectEmulsion: Emulsion

Implementation Method 2

allowing for complete diffusion and reducing eyelid sticking

Methodology Applied
Scientific EffectDiffusion: Diffusion

Implementation Method 3

Hypertonic ointments for ophthalmic use, i.e. those having a high content of osmotic component, are relevant to the present invention. Said high content has the therapeutic properties of extracting from the tissues excess of water that causes swelling of membranes in forms of oedema.

Methodology Applied
Scientific EffectOsmosis: Osmosis

Implementation Method 4

The hydrophilic phase contains a saturated solution of sodium chloride and hyaluronic acid or salt

Methodology Applied
Scientific EffectHydrophilic interaction: Hydrophile

Data Source

PatentEP3890699B1Hypertonic ophthalmic ointment
Publication Date: 2026.01.14 ORFEO VINCENZO

AI summary

The invention relates to a composition in the form of an ophthalmic ointment containing a lipophilic phase and hyaluronic acid or a salt thereof dissolved in an aqueous hydrophilic phase saturated with the osmotic agent sodium chloride. The invention also relates to the use of the ointmiP+ui1S4entin the treatment of corneal oedema.