Borate-Polyol Ophthalmic Composition for Low-Toxicity Preservation
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Solution Overview
Problem
Existing ophthalmic compositions face challenges in achieving effective antimicrobial preservation while minimizing toxicological effects on the cornea, particularly when using lower concentrations of preservatives, and maintaining desired buffering properties without causing eye discomfort.
Innovation Solution
A multi-dose ophthalmic composition comprising a combination of two different polyols, such as mannitol and propylene glycol, with borate and a polymeric quaternary ammonium compound, which balances antimicrobial activity, buffering, and reduces tear pH normalization resistance.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Reliability
If conventional antimicrobial preservatives are used at effective concentrations to prevent microbial contamination, then preservation efficacy is improved, but toxicological effects on the cornea increase
Solution Approach 1:
The patent changes the chemical parameters by introducing borate-polyol complexes that modify the antimicrobial mechanism. This allows achieving preservation efficacy through a different chemical pathway that does not rely on high concentrations of conventional preservatives, thereby reducing corneal toxicity while maintaining reliability
Solution Approach 2:
The patent uses composite formulation containing borate, polyols (such as mannitol and sorbitol), and conventional preservatives. This composite approach creates synergistic effects where the borate-polyol complex enhances preservative activity, allowing lower concentrations of toxic preservatives to achieve the same preservation efficacy
2Object-affected harmful factors
If lower concentrations of antimicrobial agents are used to reduce toxicological effects, then safety is improved, but antimicrobial preservation efficacy becomes insufficient
Solution Approach 1:
The borate-polyol complex acts as an intermediary that enhances the antimicrobial activity of preservatives. This mediator allows lower concentrations of preservatives to achieve adequate preservation by amplifying their effect through complex formation, thus reducing toxicity while maintaining efficacy
Solution Approach 2:
The patent modifies the chemical environment by adding borate and polyols, which change the physical-chemical parameters of the formulation. This creates a more favorable environment for antimicrobial action, allowing effective preservation at lower preservative concentrations
3Reliability
If borate-polyol complexes are used to enhance antimicrobial activity, then preservation efficacy is improved, but buffering effects increase causing tear pH normalization issues
Solution Approach 1:
The patent applies local quality by using specific polyols with particular buffering characteristics that are milder than traditional borate systems. This allows the formulation to provide localized antimicrobial enhancement without excessive buffering that would interfere with tear pH normalization
Solution Approach 2:
The patent adjusts the borate-to-polyol ratio and selects specific polyol types to modify the buffering capacity. By changing these parameters, the formulation achieves adequate antimicrobial activity while limiting the buffering effect to acceptable levels that allow proper tear pH normalization
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 composition achieves superior antimicrobial efficacy, meets stringent preservative efficacy standards, and maintains pH stability, reducing the risk of microbial contamination and eye irritation.
Implementation Method 1
aqueous pharmaceutical compositions containing borate-polyol complexes
Data Source
AI summary
The present invention is directed to the provision of multi-dose, ophthalmic compositions. The compositions possess sufficient antimicrobial activity to satisfy USP preservative efficacy requirements, as well as similar preservative standards (e.g., EP and JP). The compositions include at two different polyols in conjunction with borate, a preservative or both.