N,N-dialkylalkenyl ester compounds for stable aqueous glaucoma formulations
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Solution Overview
Problem
Current treatments for glaucoma and ocular hypertension often rely on topical β-adrenoreceptor antagonists, which may not be stable in aqueous solutions, limiting their effectiveness and convenience in ocular formulations.
Innovation Solution
Development of well-defined N,N-dialkylalkenyl ester compounds that are stable in aqueous solutions, allowing for their incorporation into stable aqueous formulations for treating glaucoma and ocular hypertension, including pharmaceutical compositions and methods for administering therapeutically effective amounts to reduce intraocular pressure.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Reliability
If topical β-adrenoreceptor antagonists are used to treat glaucoma, then intraocular pressure can be reduced, but the formulations are unstable in aqueous solutions
Solution Approach 1:
The patent changes the chemical parameters of the active ingredient by using N,N-dialkylalkenyl ester compounds instead of traditional β-adrenoreceptor antagonists. These ester compounds have modified chemical structures that provide stability in aqueous solutions while maintaining the ability to reduce intraocular pressure, thus resolving the contradiction between formulation stability and treatment efficacy.
2Ease of operation
If traditional glaucoma treatments are used, then intraocular pressure can be reduced, but the formulations require non-aqueous bases which limit their convenience
Solution Approach 1:
The invention changes the physical parameter of the formulation base from non-aqueous to aqueous by using N,N-dialkylalkenyl ester compounds that are stable in water. This allows the development of aqueous eye drop formulations that are more convenient for patients while maintaining formulation stability, thereby resolving the contradiction between ease of operation and reliability.
Data Source
AI summary
The invention provides well defined N,N-dialkylalkenyl ester compounds for treating glaucoma or ocular hypertension. The esters of the invention are particularly advantageous due to their stability in aqueous solutions.