Ophthalmic Composition Hyaluronate Ectoine Panthenol Dry Eye

Resolve Bottlenecks,
Find Innovative Solutions
Generate Solutions

Solution Overview

Problem

Current treatments for dry eye syndrome, such as hyaluronic acid eye drops, have limited action time and can cause discomfort, while combinations with additional active ingredients may lead to side effects.

Innovation Solution

An ophthalmic composition combining hyaluronate with ectoine and panthenol, which exhibits a synergistic effect in water binding capacity and dynamic viscosity, providing prolonged moisturization without discomfort and side effects.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Duration of action of moving object

If hyaluronic acid eye drops are used to treat dry eye syndrome, then moisture retention and cornea hydration are improved, but the action time is limited requiring frequent repetition

Engineering Contradiction:
Improveaction timeVSAvoidfrequency of instillation
Core Design Contradiction:
Duration of action of moving objectVSQuantity of substance

Solution Approach 1:

The patent combines hyaluronic acid with ectoine and panthenol in a single ophthalmic composition. This merging of multiple active ingredients works synergistically to extend the duration of action while maintaining effective moisture retention, reducing the need for frequent instillation.

Inventive Principle:
Principle #5Merging (Combining)

Solution Approach 2:

The invention uses a composite formulation containing hyaluronic acid (0.01-2%), ectoine (0.5-5%), and panthenol (0.5-5%). This composite material leverages the complementary properties of each component: hyaluronic acid for hydration, ectoine for water binding and protection, and panthenol for moisturization, achieving prolonged action time.

Inventive Principle:
Principle #40Composite materials

2Reliability

If additional active ingredients such as immunosuppressants or anti-inflammatories are added to treat severe dry eye, then treatment effectiveness is improved, but undesired side effects increase particularly with prolonged use

Engineering Contradiction:
Improvetreatment effectivenessVSAvoidside effects
Core Design Contradiction:
ReliabilityVSObject-affected harmful factors

Solution Approach 1:

The patent converts potentially harmful side effects into beneficial effects by using ectoine and pantheseol, which are naturally occurring substances with protective and moisturizing properties. These ingredients provide anti-inflammatory and soothing effects without the harmful side effects of conventional immunosuppressants or anti-inflammatories.

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

Solution Approach 2:

The invention changes the chemical parameters of the treatment by using ectoine (a cyclic amino acid) and panthenol (a provitamin B5) instead of conventional pharmaceutical agents. This parameter change maintains treatment effectiveness while eliminating harmful side effects associated with prolonged use of immunosuppressants and anti-inflammatories.

Inventive Principle:
Principle #35Parameter changes

3Duration of action of stationary object

If the viscosity of eye drops is increased to prolong retention on the eye surface, then remanence is improved, but discomfort and occlusion of lacrimal ducts may occur

Engineering Contradiction:
ImproveremanenceVSAvoiddiscomfort and occlusion
Core Design Contradiction:
Duration of action of stationary objectVSObject-affected harmful factors

Solution Approach 1:

The patent optimizes the viscosity parameter by formulating with hyaluronic acid at 0.01-2%, ectoine at 0.5-5%, and panthenol at 0.5-5%. This combination achieves the right balance: sufficient viscosity to prolong retention time and improve remanence, while remaining low enough to avoid discomfort and lacrimal duct occlusion. The synergistic interaction of these components allows fine-tuning of the viscosity parameter.

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 effectively treats dry eye syndrome and related conditions with increased tear film thickness and reduced surface tension, offering prolonged action without the need for additional active ingredients or preservatives, thus minimizing side effects.

Implementation Method 1

Hyaluronic acid is used in eye drops for the hydration of the cornea. It forms a transparent, lubricating and wetting film on the surface of the eye, protecting the cornea against drying.

Methodology Applied
Scientific EffectHydration: Absorption (physical)

Implementation Method 2

The triple combination of hyaluronate with ectoine and panthenol shows surprisingly high water binding capacity, thus improving moistening of the eye.

Methodology Applied
Scientific EffectWater binding: Absorption (physical)

Implementation Method 3

The composition of the invention also has a surprisingly high dynamic viscosity, which ensures that the composition adheres to the surface of the eye and remains there for a long time.

Methodology Applied
Scientific EffectViscosity:

Implementation Method 4

the presence of dexpanthenol in the composition of the invention unexpectedly results in decreased surface tension. This is very important because the tear film thickness increases exponentially with drop of the surface tension

Methodology Applied
Scientific EffectSurface tension: Surface Tension

Implementation Method 5

The tear film acts inter alia as a slip or lubricating agent between the eyelid and the surface of the eye.

Methodology Applied
Scientific EffectLubrication: Lubrication

Data Source

PatentEP3827818A1Ophthalmic composition
Publication Date: 2021.06.02 ZAKLADY FARMACEUTYCZNE POLPHARMA SA
  • EP3827818A1 patent drawingFigure 1
  • EP3827818A1 patent drawingFigure 2
  • EP3827818A1 patent drawingFigure 3

AI summary

The application refers to an ophthalmic composition comprising: 0.001 to 2 % by weight of hyaluronic acid or an ophthalmologically acceptable salt thereof; 0.5 to 5 % by weight of ectoine or an ophthalmologically acceptable salt or derivative thereof; 0.5 to 5 % by weight of a compound selected from the group consisting of panthenol, pantothenic acid, an ophthalmologically acceptable salt of pantothenic acid, and combinations thereof; and an amount of water up to 100% by weight of the composition. The application also refers to the above composition for use in the prevention and/or treatment of an ophthalmological pathology selected from the group consisting of dry eye syndrome, Sjogren syndrome, inflammation of the conjunctiva, irritation, itchiness, burning and allergic reactions of the eye, and related conditions.