Ocular Corticosteroid Composition With Oxygen Scavengers for pH Stability
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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, necessitating a method to stabilize the pH and prevent drug oxidation.
Innovation Solution
The addition of an additive, such as antioxidants or oxygen scavengers, to the aqueous composition comprising a corticosteroid, particularly at concentrations between 0.15% and 0.6% (w/v), stabilizes the pH by preventing oxidation of the corticosteroid.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Duration of action of stationary object
If cyclodextrin-based eye drops are stored in LDPE vials for several months, then the pH of the composition decreases over time, but this pH instability compromises the drug efficacy and safety
Solution Approach 1:
The patent introduces an oxygen scavenger (such as sodium bisulfite, sodium metabisulfite, or ascorbic acid) as an intermediary substance that reacts with dissolved oxygen in the aqueous composition, thereby preventing oxidation of the corticosteroid drug and stabilizing the pH during storage. This mediator eliminates the harmful oxidation process without requiring changes to the storage container or conditions.
2Reliability
If the corticosteroid is exposed to oxygen during storage, then oxidation occurs leading to drug degradation, but preventing oxidation requires adding stabilizing additives to the composition
Solution Approach 1:
The patent employs small amounts of inexpensive, short-acting oxygen scavengers (such as sodium bisulfite or ascorbic acid at concentrations of 0.01-0.5% w/v) that are consumed during storage to prevent oxidation. These disposable stabilizing agents effectively protect the corticosteroid without requiring complex formulation systems or expensive 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 method effectively maintains pH stability for over six months, ensuring the corticosteroid's efficacy in ocular treatments by preventing degradation and maintaining drug solubility.
Implementation Method 1
the addition of an additive to prevent oxidation of the corticosteroid
Data Source
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.