Ophthalmic Suspension Composition for Easy Redispersion
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Solution Overview
Problem
Current dry eye therapeutic agents require frequent administration due to poor redispersibility, leading to inconvenience for patients.
Innovation Solution
An aqueous suspension agent comprising (E)-2-(7-trifluoromethylchroman-4-ylidene)-N-(7-hydroxy-5,6,7,8-tetrahydronaphthalen-1-yl)acetamide, a heterocyclideneacetamide derivative, combined with a cellulosic polymer and nonionic surfactant, to improve redispersibility and stability.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Reliability
If conventional dry eye therapeutic agents are used, then the treatment effect is achieved, but the administration frequency is high (4-6 times per day) due to poor redispersibility
Solution Approach 1:
The patent changes the physical and chemical parameters of the suspension formulation by incorporating specific surfactants (nonionic surfactants like polysorbate 80) and polymers (carboxymethylcellulose sodium) to improve redispersibility. This allows the suspension to maintain stable particle distribution and re disperse easily after settling, enabling less frequent administration while maintaining treatment efficacy
Solution Approach 2:
The patent uses a composite formulation combining heterocyclideneacetamide derivative active ingredient with carboxymethylcellulose sodium and nonionic surfactants. This composite suspension system provides both therapeutic effect and improved redispersibility, allowing the suspension to settle uniformly and re disperse easily with minimal shaking, thereby reducing administration frequency
2Stability of the object's composition
If the suspension settles during storage, then stability is achieved, but redispersibility is poor requiring many shakes or inversions
Solution Approach 1:
The patent uses carboxnymethylcellulose sodium and nonionic surfactants as intermediary substances that prevent excessive particle aggregation during settling. These intermediaries create a stable suspension structure where particles settle uniformly but remain easily redispersible with minimal shaking or inversion, solving the contradiction between settling stability and redispersibility
Solution Approach 2:
The patent optimizes the concentration parameters of carboxymethylcellulose sodium (0.003-0.03% w/v) and nonionic surfactants (0.001-0.01% w/v) to achieve the desired balance. At these optimized concentrations, the suspension settles stably during storage but redisperses easily with 10 or fewer inversions, resolving the contradiction between stability and redispersibility
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 suspension agent achieves improved redispersibility, allowing for fewer shakes or inversions to reconstitute, and enhanced stability, reducing the frequency of application and improving patient compliance.
Implementation Method 1
a nonionic surfactant
Implementation Method 2
a cellulosic polymer
Data Source
AI summary
The present disclosure provides suspendable ophthalmic solutions with excellent redispersibility. The present disclosure provides an aqueous suspension agent comprising (E)-2-(7-trifluoromethylchroman-4-ylidene)-N-(7-hydroxy-5,6,7,8-tetrahydronaphthalen-1-yl)acetamide or a pharmaceutically acceptable salt or solvate thereof, a cellulosic polymer, and a nonionic surfactant.