Aqueous Composition Synergistic Antiseptic Formulation
Solution Overview
Problem
Aqueous compositions used in eye drops and other applications are susceptible to microbial contamination due to contact with non-sterile air, and existing antiseptics like parabens and benzalkonium chloride can cause cytotoxicity, necessitating a formulation with enhanced antiseptic effects while minimizing the use of these agents.
Innovation Solution
An aqueous composition combining ripasudil, a halogenated isoquinoline derivative, with benzalkonium chloride at concentrations of 0.0001 to 0.01 w/v%, providing a synergistic antiseptic effect while reducing the amount of benzalkonium chloride required.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Reliability
If antiseptics like parabens or benzalkonium chloride are incorporated to prevent microbial contamination, then the antiseptic effect is improved, but cytotoxicity increases causing corneal injury
Solution Approach 1:
The patent combines ripasudil (a halogenated isoquinoline derivative with Rho kinase inhibitory action) with benzalkonium chloride to create a synergistic antiseptic formulation. This combination allows the aqueous composition to achieve enhanced antiseptic effects while using minimal amounts of benzalkonium chloride (0.0001 to 0.01 w/v%), thereby reducing cytotoxicity and corneal injury risk compared to using conventional antiseptics alone at higher concentrations
2Reliability
If conventional antiseptics are used at sufficient concentrations to ensure antiseptic effect, then microbial contamination is prevented, but the amount of antiseptic required increases leading to higher cytotoxicity
Solution Approach 1:
By combining ripasudil with benzalkonium chloride, the patent achieves synergistic antiseptic effects that allow the use of benzalkonium chloride at concentrations 10-100 times lower than conventional formulations (0.0001 to 0.01 w/v% vs. typical 0.1-0.5 w/v%). This dramatically reduces the quantity of antiseptic substance required while maintaining or enhancing the antiseptic effect
Solution Approach 2:
The patent creates a composite antiseptic system where ripasudil (providing Rho kinase inhibitory action and some antiseptic effect) works synergistically with benzalkonium chloride. This composite formulation achieves superior antiseptic performance at lower overall antiseptic concentrations compared to conventional single-agent formulations
Data Source
AI summary
An aqueous composition having an excellent antiseptic effect is provided. An aqueous composition comprising a compound represented by Formula (1), wherein X represents a halogen atom, or a salt thereof, or a solvate of the compound or the salt thereof, and a quaternary ammonium surfactant.