Ophthalmic Composition for Glaucoma via Multi-Drug Synergy
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Solution Overview
Problem
Current treatments for ocular hypertension and glaucoma, particularly post-surgical and post-laser trabeculectomy episodes, lack effective ocular hypotensive agents that can manage intraocular pressure effectively and safely.
Innovation Solution
A composition comprising 8-(5-bromoquinoxalin-6-yl)-5-oxo-2,3,5,6,7,8-hexahydroimidazo[1,2-a]pyrimidine-7-carboxylic acid, combined with brimonidine tartrate and timolol, is developed to treat and prevent ocular hypertension and glaucoma, with specific formulations and preparation methods to enhance efficacy and stability.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Reliability
If topical β-adrenoreceptor antagonists are used to treat glaucoma, then intraocular pressure is reduced, but the treatment lacks effectiveness in post-surgical and post-laser trabeculectomy ocular hypertensive episodes
Solution Approach 1:
The patent combines multiple active ingredients (timolol maleate, brimonidine tartrate, and the compound of Formula I) into a single ophthalmic composition that can treat various types of ocular hypertensive conditions including primary open-angle glaucoma, acute angle-closure glaucoma, and post-surgical ocular hypertensive episodes, making the treatment universally applicable across different clinical scenarios
Solution Approach 2:
The invention uses a composite formulation containing three distinct pharmacologically active compounds working synergistically: timolol maleate (β-adrenoreceptor antagonist), brimonidine tartrate (α2-adrenoreceptor agonist), and the compound of Formula I (new chemical entity), creating a multi-component therapeutic system that addresses multiple mechanisms of intraocular pressure regulation
2Productivity
If a single active ingredient is used in ophthalmic composition, then the formulation is simple, but the efficacy in managing intraocular pressure is insufficient
Solution Approach 1:
The patent merges three different pharmacologically active compounds into a single ophthalmic composition: timolol maleate (0.25%-1.0%), brimonidine tartrate (0.05%-0.2%), and the compound of Formula I (0.001%-0.1%). This combination allows synergistic action on multiple pathways of aqueous humor dynamics, achieving superior intraocular pressure reduction compared to any single agent alone
3Reliability
If multiple active ingredients are combined in ophthalmic composition, then the treatment efficacy is improved, but the manufacturing and stability become more difficult
Solution Approach 1:
The patent specifies precise concentration ranges for each active ingredient to optimize stability and efficacy: timolol maleate (0.25%-1.0%), brimonidine tartrate (0.05%-0.2%), and compound of Formula I (0.001%-0.1%). These parameter specifications guide manufacturing processes and ensure consistent product quality while maintaining therapeutic effectiveness
Data Source
AI summary
Novel compounds and their uses are disclosed herein.