Corticosteroid Ophthalmic Compositions With Antioxidant pH Stabilization

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Solution Overview

Problem

Current ocular treatments face challenges in delivering effective drug doses due to passive diffusion limitations, and cyclodextrin-based eye drops experience pH instability during storage, leading to drug oxidation and degradation.

Innovation Solution

The addition of an additive, such as antioxidants or oxygen scavengers, to the aqueous composition stabilizes the pH by preventing drug oxidation, particularly in cyclodextrin-based eye drops.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Duration of action of stationary object

If cyclodextrin-based eye drops are stored in LDPE vials for extended periods, then the storage duration is improved, but the pH stability deteriorates and drug oxidation occurs

Engineering Contradiction:
Improvestorage durationVSAvoidpH stability
Core Design Contradiction:
Duration of action of stationary objectVSStability of the object's composition

Solution Approach 1:

An antioxidant is added to the eye drop formulation before storage to prevent oxidation of the corticosteroid drug. This preliminary protective action maintains pH stability throughout the storage period, allowing extended storage in LDPE vials without compromising composition stability.

Inventive Principle:
Principle #10Preliminary action

2Duration of action of stationary object

If cyclodextrin-based eye drops are stored in LDPE vials for extended periods, then the storage duration is improved, but the drug oxidation increases

Engineering Contradiction:
Improvestorage durationVSAvoiddrug oxidation
Core Design Contradiction:
Duration of action of stationary objectVSObject-generated harmful factors

Solution Approach 1:

The antioxidant converts the harmful oxidative environment that naturally develops during extended storage into a protective atmosphere. By introducing this counteracting substance, the storage conditions that would normally cause drug degradation are transformed into safe storage conditions that maintain drug integrity over extended periods.

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

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 method maintains pH stability for extended storage periods, ensuring effective drug delivery and reducing degradation products.

Implementation Method 1

the addition of an additive to prevent oxidation of the corticosteroid

Methodology Applied
Scientific EffectOxidation: Oxidation

Data Source

PatentUS12403148B2PH stabilized ophthalmic compositions
Publication Date: 2025.09.02 OCULIS OPERATIONS SARL

AI summary

The present disclosure relates to a method for stabilizing the pH of an aqueous composition comprising a drug which is prone to oxidation, said method comprising the addition of an additive to prevent oxidation of the drug which is prone to oxidation. In particular, the present disclosure relates to a method for stabilizing the pH of an aqueous composition comprising a corticosteroid, said method comprising the addition of an additive to prevent oxidation of the corticosteroid. The present disclosure also relates to a composition comprising a corticosteroid and an additive to prevent oxidation of the corticosteroid.