Lipid-Based Ophthalmic Emulsion for Dry Eye Hydration

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Solution Overview

Problem

Current artificial tear compositions for dry eye disease require frequent application, are cumbersome, and may cause blurring due to oil globule formation on the eye, while they provide only temporary hydration protection against desiccation.

Innovation Solution

A lipid-based ophthalmic emulsion containing hydroxypropyl guar, anionic lipids, and a mucoadhesive galactomannan polymer, which maintains small oil droplet size and stability, enhancing hydration protection and retention without benzalkonium chloride, and reducing blurring upon instillation.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If artificial tear compositions are used to provide hydration protection, then ocular surface lubrication is improved, but the treatment requires frequent application (10-20 times per day) which is cumbersome and reduces patient compliance

Engineering Contradiction:
Improvehydration protectionVSAvoidapplication frequency
Core Design Contradiction:
ReliabilityVSEase of operation

Solution Approach 1:

The patent changes the physical-chemical parameters of the artificial tear formulation by incorporating specific polymers (hydroxypropyl guar at 0.05-0.5% w/v, galactomannan at 0.1-0.5% w/v) and lipids to create a formulation with extended residence time and sustained hydration properties, reducing the need for frequent reapplication

Inventive Principle:
Principle #35Parameter changes

Solution Approach 2:

The invention uses a composite formulation combining multiple components: hydroxypropyl guar polymer, galactomannan polymer, phospholipids, and other excipients. This composite structure provides synergistic effects that enhance both the lubricating properties and the duration of action, allowing longer-lasting hydration protection

Inventive Principle:
Principle #40Composite materials

2Stability of the object's composition

If oil and anionic lipids are included in the emulsion to improve lipid layer stability, then tear film stability is enhanced, but oil globules form on the eye surface causing blurring upon instillation

Engineering Contradiction:
Improvetear film stabilityVSAvoidblurring
Core Design Contradiction:
Stability of the object's compositionVSObject-generated harmful factors

Solution Approach 1:

The patent optimizes the concentration parameters of lipid components (phospholipids at 0.001-0.1% w/v) and combines them with specific polymer concentrations to control the physical state and distribution of oil droplets, preventing globule formation while maintaining tear film stability

Inventive Principle:
Principle #35Parameter changes

Solution Approach 2:

The patent introduces hydrophilic polymers (hydroxypropyl guar and galactomannan) as intermediary substances that interact with lipid components to stabilize the emulsion structure, prevent oil globule aggregation, and ensure uniform distribution on the ocular surface without causing blurring

Inventive Principle:
Principle #24Intermediary (Mediator)

3Reliability

If polymer concentration is increased to enhance hydration protection and retention, then desiccation protection is improved by at least 10%, but the formulation complexity and manufacturing precision requirements increase

Engineering Contradiction:
Improvedesiccation protectionVSAvoidpolymer concentration control
Core Design Contradiction:
ReliabilityVSManufacturing precision

Solution Approach 1:

The patent establishes specific concentration ranges for polymers (hydroxypropyl guar: 0.05-0.5% w/v, galactomannan: 0.1-0.5% w/v) that optimize desiccation protection while remaining manufacturable. These parameter specifications balance performance requirements with manufacturing feasibility

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 emulsion provides at least 10% higher hydration protection against desiccation and longer ocular surface hydration retention, maintaining stability and reducing blurring, thus addressing the limitations of existing artificial tear compositions.

Implementation Method 1

a mucoadhesive galactomannan polymer

Methodology Applied
Scientific EffectMucoadhesion: Adhesive

Implementation Method 2

A lipid-based ophthalmic emulsion containing the gellable polymer hydroxypropyl guar and anionic lipids

Methodology Applied
Scientific EffectEmulsion: Emulsion

Data Source

PatentUS11730699B2Lipid-based ophthalmic emulsion
Publication Date: 2023.08.22 ALCON INC
  • US11730699B2 patent drawing
  • US11730699B2 patent drawing
  • US11730699B2 patent drawing

AI summary

The present invention is directed to a lipid-based ophthalmic emulsion. The emulsion has an increased amount of a mucoadhesive galactomannan polymer that promotes a long-lasting protection against desiccation and moisture retention.