Pyrrolidone Carboxylic Acid Ocular Hydration Formulation

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Solution Overview

Problem

Current treatments for dry eye disease and related ocular disorders, such as hyperosmolarity and inflammation, are inadequate, with existing tear substitutes providing short-term relief and requiring frequent application, and surgical solutions can be uncomfortable and ineffective.

Innovation Solution

Pyrrolidone carboxylic acid (PCA) and its pharmaceutically acceptable salts or derivatives, combined with additional active ingredients like copper sulfate and hyaluronic acid, are used in pharmaceutical formulations to improve ocular hydration and combat infections, offering prolonged hydration and enhanced antibacterial/antiviral effects.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Duration of action of moving object

If tear substitutes are used to treat dry eye disease, then ocular hydration is improved, but application frequency must be very high (every 1-2 hours) which reduces patient compliance

Engineering Contradiction:

Improveduration of ocular hydrationVSAvoidpatient compliance

Core Design Contradiction:

Duration of action of moving objectVSEase of operation

Solution Approach 1:

The patent changes the chemical parameter of the tear substitute by incorporating pyrrolidone carboxylic acid (PCA) at concentrations of 0.01-5% w/v. This chemical modification extends the duration of ocular hydration from 1-2 hours with conventional tears to potentially longer duration, reducing application frequency and improving patient compliance while maintaining therapeutic efficacy

Inventive Principle:

Principle #35Parameter changes

2Reliability

If conventional tear substitutes are used, then short-term relief is provided, but treatment effectiveness is insufficient for long-term management

Engineering Contradiction:

Improvetreatment effectivenessVSAvoidduration of therapeutic effect

Core Design Contradiction:

ReliabilityVSDuration of action of stationary object

Solution Approach 1:

The patent creates a composite tear substitute formulation by combining pyrrolidone carboxylic acid (PCA) with conventional tear substitute components. This composite material provides both the immediate symptomatic relief of conventional tears and the extended therapeutic effect of PCA, achieving reliable long-term treatment effectiveness while maintaining short-term comfort

Inventive Principle:

Principle #40Composite materials

3Reliability

If surgical solutions are used to treat dry eye disease, then ocular surface protection is improved, but patient comfort deteriorates due to discomfort

Engineering Contradiction:

Improveocular surface protectionVSAvoidpatient comfort

Core Design Contradiction:

ReliabilityVSEase of operation

Solution Approach 1:

The patent replaces the mechanical surgical intervention (punctal occlusion or grafting) with a chemical/pharmacological approach using pyrrolidone carboxylic acid. This substitution provides comparable ocular surface protection through enhanced tear film stability and anti-inflammatory effects, while avoiding the discomfort and invasiveness of surgical procedures

Inventive Principle:

Principle #28Mechanics substitution (Replace mechanical system)

Data Source

PatentUS10456374B2Pyrrolidone carboxylic acid (PCA) for ophthalmic use

Publication Date: 2019.10.29 LAB BALDACCI

AI summary

The present invention relates to pyrrolidone carboxylic acid (PCA) and/or pharmaceutically acceptable salts or derivatives thereof for use in the treatment of ocular diseases and/or disorders.A further object of the present invention are compositions comprising pyrrolidone carboxylic acid (PCA) and/or pharmaceutically acceptable salts or derivatives thereof, at least one physiologically acceptable excipient, and optionally at least one additional active ingredient for use in the treatment of ocular diseases and/or disorders.