Antioxidant Ophthalmic Composition to Limit N-Oxopyridine Formation
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Solution Overview
Problem
Current eye drop formulations for posterior segment eye diseases are limited, and existing treatments like intraocular injections face patient compliance issues, side effects, and stability challenges, particularly with the conversion of the active ingredient 3-phenyl-4-propyl-1-(pyridin-2-yl)-1H-pyrazol-5-ol into the ineffective N-oxopyridine compound during long-term storage.
Innovation Solution
An eye drop composition containing 3-phenyl-4-propyl-1-(pyridin-2-yl)-1H-pyrazol-5-ol with pharmaceutically acceptable salts and an antioxidant substance, such as cysteine, N-acetyl cysteine, or monothioglycerol, minimizes the formation of N-oxopyridine compound to less than 3% even after six months, ensuring stability and safety.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Stability of the object's composition
If the active ingredient 3-phenyl-4-propyl-1-(pyridin-2-yl)-1H-pyrazol-5-ol is stored in liquid form for long-term, then it converts into N-oxopyridine compound, but this conversion reduces therapeutic efficacy and increases impurity levels
Solution Approach 1:
The patent introduces antioxidants (such as ascorbic acid, tocopherol, or cysteine) as intermediary substances that mediate between the active ingredient and oxygen in the aqueous environment. These antioxidants preferentially react with oxygen or free radicals, preventing the oxidation of the pyridine nitrogen in the active ingredient, thus blocking the formation pathway of N-oxopyridine compound while maintaining the stability of the liquid formulation.
Solution Approach 2:
The patent modifies the chemical environment parameters of the formulation by adjusting pH levels and introducing chelating agents that alter the reactivity of the active ingredient. By controlling the oxidation-reduction potential and pH of the solution, the patent suppresses the spontaneous oxidation reaction that leads to N-oxopyridine formation, thereby improving long-term storage stability without compromising therapeutic efficacy.
2Reliability
If intraocular injection is used to treat posterior segment eye diseases, then therapeutic effect is achieved, but patient compliance deteriorates due to repeated injections and side effects
Solution Approach 1:
The patent replaces the mechanical injection system with a chemical delivery system in the form of eye drops. Instead of physically injecting the drug into the eye using needles and syringes, the active ingredient is delivered topically through the ocular surface in a stable liquid formulation. This substitution eliminates the mechanical trauma associated with injections while maintaining therapeutic effectiveness through optimized drug delivery to the posterior segment.
Solution Approach 2:
The patent introduces ophthalmic formulation components (such as viscosity-enhancing agents, penetration enhancers, and preservatives) as intermediaries that facilitate the delivery of the active ingredient from the ocular surface to the posterior segment. These intermediary substances help the drug traverse the ocular barriers (cornea, aqueous humor, vitreous) without requiring direct injection, thereby improving patient compliance while achieving reliable therapeutic effects.
3Ease of operation
If eye drop formulation is used for posterior segment diseases, then patient compliance improves, but delivery of active ingredient to posterior segment is limited by complex eye tissue barriers
Solution Approach 1:
The patent optimizes physical-chemical parameters of the eye drop formulation, including viscosity, osmolarity, pH, and surfactant concentration, to enhance drug penetration through ocular barriers. By adjusting these parameters, the formulation achieves prolonged residence time on the ocular surface and improved transcorneal and transvitreous transport, enabling reliable delivery to the posterior segment while maintaining ease of administration.
Solution Approach 2:
The patent employs composite formulation systems combining multiple functional components: the active ingredient, antioxidants, viscosity agents, penetration enhancers, and preservatives work synergistically. This composite approach creates a formulation that simultaneously protects the drug from degradation, enhances penetration through complex tissue barriers, and maintains patient compliance through convenient drop administration.
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 maintains therapeutic efficacy for posterior segment diseases like macular degeneration through instillation, comparable to intraocular injections, with improved patient compliance and reduced side effects.
Implementation Method 1
there is a difference from the eye drop composition of the present invention, which proposes a method for solving the above problem
Data Source
AI summary
The present invention relates to an eye drop preparation which contains an active ingredient selected from 3-phenyl-4-propyl-1-(pyridin-2-yl)-1H-pyrazol-5-ol compound or pharmaceutically acceptable salts thereof, an antioxidant substance and thus N-oxopyridine compound in an amount of less than about 3%. The eye drop according to the present invention is excellent in stability and safety and shows an excellent effect on prevention or treatment of eye diseases including posterior segment eye diseases simply through instillation rather than a direct injection into an eyeball.