Pepstatin Alginic Acid Ophthalmic Composition Pepsin Inhibition

Resolve Bottlenecks,
Find Innovative SolutionsGenerate Solutions

Solution Overview

Problem

Current treatments for extraesophageal disorders such as lacrimal dysfunction syndrome and conjunctivitis in the periocular region, caused by the presence of pepsin in the lacrimal fluid due to gastric reflux, are ineffective as they do not specifically address the underlying cause and often have side effects.

Innovation Solution

A composition comprising pepstatin and alginic acid, optionally with hyaluronic acid, which effectively inhibits pepsin in the lacrimal fluid by pepstatin's inhibitory action and alginate's sequestrant and lubricating properties, providing a stable, easy-to-administer, and side-effect-free treatment.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If current treatments are used for extraesophageal disorders caused by pepsin in lacrimal fluid, then treatment is provided, but the treatments are ineffective and have side effects because they do not specifically address the underlying cause

Engineering Contradiction:

Improvetreatment effectivenessVSAvoidside effects

Core Design Contradiction:

ReliabilityVSObject-generated harmful factors

Solution Approach 1:

The treatment is divided into two distinct functional components: pepstatin specifically targets and inhibits pepsin activity, while alginic acid handles sequestration and lubrication. This segmentation allows each component to perform its specialized function without the side effects of broad-spectrum steroids.

Inventive Principle:

Principle #1Segmentation

Solution Approach 2:

Alginic acid acts as an intermediary substance that sequesters pepsin molecules, preventing them from damaging ocular tissues. This intermediary approach removes the harmful pepsin from the system without requiring direct confrontation that might cause side effects.

Inventive Principle:

Principle #24Intermediary (Mediator)

2Reliability

If pepstatin and alginic acid are combined to inhibit pepsin, then pepsin is effectively eliminated from lacrimal fluid, but the composition complexity increases

Engineering Contradiction:

Improvepepsin inhibition effectivenessVSAvoidcomposition structure

Core Design Contradiction:

ReliabilityVSDevice complexity

Solution Approach 1:

Two effective substances (pepstatin and alginic acid) are merged into a single ophthalmic composition. This combining allows synergistic action where pepstatin provides specific inhibition and alginic acid provides sequestration and lubrication, achieving comprehensive pepsin neutralization in one formulation.

Inventive Principle:

Principle #5Merging (Combining)

Solution Approach 2:

The alginic acid component performs multiple functions simultaneously: it sequesters pepsin, provides lubrication to the ocular surface, and acts as a stabilizing agent. This multi-functionality reduces the need for additional separate components, managing composition complexity.

Inventive Principle:

Principle #6Universality (Multi-functionality)

3Object-affected harmful factors

If hyaluronic acid is added to enhance viscoelastic activity and lubrication, then ocular surface protection is improved, but the manufacturing complexity increases

Engineering Contradiction:

Improveocular surface protectionVSAvoidcomposition preparation

Core Design Contradiction:

Object-affected harmful factorsVSEase of manufacture

Solution Approach 1:

Hyaluronic acid serves multiple protective functions: it provides viscoelastic support to the tear film, enhances lubrication of the ocular surface, and contributes to tear film stability. This multi-functionality justifies the additional manufacturing step by providing comprehensive ocular surface protection.

Inventive Principle:

Principle #6Universality (Multi-functionality)

Solution Approach 2:

The ophthalmic composition uses a composite material system combining pepstatin, alginic acid, and hyaluronic acid. Each component contributes specific properties that complement the others, creating a synergistic formulation that provides comprehensive protection against pepsin-induced damage while maintaining tear film stability.

Inventive Principle:

Principle #40Composite materials

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 combination of pepstatin and alginic acid synergistically reduces and eliminates pepsin from the lacrimal fluid, effectively treating inflammatory ocular and periocular disorders related to gastric reflux, with the addition of hyaluronic acid enhancing viscoelastic activity and lubrication without using steroidal substances.

Implementation Method 1

pepstatin's inhibitory action

Methodology Applied

Scientific EffectEnzyme inhibition: Enzyme

Implementation Method 2

alginate's sequestrant properties

Methodology Applied

Scientific EffectSequestration: Adsorption

Implementation Method 3

alginate's lubricating properties

Methodology Applied

Scientific EffectLubrication: Lubrication

Implementation Method 4

hyaluronic acid enhancing viscoelastic activity

Methodology Applied

Scientific EffectViscoelasticity: Viscoelasticity

Data Source

PatentUS20230181703A1Composition comprising pepstatin and alginic acid or a salt thereof, and use thereof

Publication Date: 2023.06.15 DRUGS MINERALS & GENERICS ITAL S R L IN FORMA ABBREVIATA D M G ITAL SRL

AI summary

The present invention relates to an aqueous composition for ophthalmic use comprising pepstatin and alginic acid or a salt thereof, and to the use of said composition in a method for the treatment of a disease or symptom of the eyeball and/or periocular region related with or deriving from the presence of pepsin in the lacrimal fluid.