Aqueous Aceclidine Compositions for Room-Temperature Stability

Resolve Bottlenecks,
Find Innovative Solutions
Generate Solutions

Solution Overview

Problem

Aceclidine compositions for treating presbyopia are unstable in aqueous environments, particularly at room temperature, posing challenges for storage, shipment, and prolonged use, and require cold-chain storage protocols that are not always feasible.

Innovation Solution

Aqueous aceclidine compositions with a pH of 6 or less, specifically between 4.5 and 5.5, exhibit enhanced stability at room temperature, maintaining at least 90% purity for extended periods, up to 6 months, and are suitable for storage, shipment, and use without preservatives or varying buffer concentrations.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Ease of operation

If aceclidine is formulated in aqueous environments for topical administration, then ease of operation and patient compliance improve, but stability of the composition deteriorates due to degradation at room temperature

Engineering Contradiction:
Improveease of administrationVSAvoidstability of aceclidine
Core Design Contradiction:
Ease of operationVSStability of the object's composition

Solution Approach 1:

The patent applies parameter changes by adjusting the pH of the aqueous aceclidine composition to be less than 6.0 (specifically pH 4.5-5.5). This pH adjustment stabilizes the aceclidine molecule in aqueous solution, preventing degradation while maintaining the liquid formulation's ease of administration. The pH modification creates optimal conditions for aceclidine stability without requiring cold-chain storage.

Inventive Principle:
Principle #35Parameter changes

2Ease of operation

If aceclidine compositions are stored at room temperature, then ease of operation and patient compliance improve, but duration of action and efficacy deteriorate due to degradation over time

Engineering Contradiction:
Improvestorage convenienceVSAvoidshelf life
Core Design Contradiction:
Ease of operationVSDuration of action of stationary object

Solution Approach 1:

The patent modifies the chemical environment parameter (pH) to less than 6.0, which extends the shelf life of aceclidine compositions stored at room temperature from months to years while maintaining efficacy. This pH optimization prevents hydrolysis and degradation pathways that would otherwise limit shelf life.

Inventive Principle:
Principle #35Parameter changes

Solution Approach 2:

The patent enables room-temperature stable aceclidine formulations that can be manufactured and distributed without expensive cold-chain infrastructure. The simplified storage requirements reduce distribution costs and make the treatment more accessible, effectively creating a practical long-shelf-life product without requiring refrigeration.

Inventive Principle:
Principle #27Cheap short-living objects (Disposable)

3Stability of the object's composition

If cold-chain storage protocols are implemented, then stability of the composition improves, but device complexity and cost increase

Engineering Contradiction:
Improvestability of aceclidineVSAvoidstorage infrastructure
Core Design Contradiction:
Stability of the object's compositionVSDevice complexity

Solution Approach 1:

The patent changes the pH parameter to less than 6.0, which fundamentally alters the stability profile of aceclidine to allow room-temperature storage. This eliminates the need for cold-chain storage infrastructure, reducing complexity in manufacturing, distribution, and patient storage while maintaining composition stability.

Inventive Principle:
Principle #35Parameter changes

Solution Approach 2:

The patent extracts the requirement for cold-chain storage by modifying the formulation pH. By removing this external stability constraint through chemical formulation optimization, the system becomes simpler and more accessible without requiring refrigerated storage infrastructure at any stage from manufacturing to patient use.

Inventive Principle:
Principle #2Taking out (Extraction)

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 compositions retain high aceclidine purity and efficacy for treating presbyopia, even after storage at room temperature for up to 6 months, improving near vision and reducing the need for corrective lenses.

Implementation Method 1

aqueous aceclidine compositions having a pH of about 6 or less (e.g., about 4.5 or about 5.5), that have acceptable aceclidine stability profiles at room temperature (or higher temperatures) for extended periods of time

Methodology Applied
Scientific EffectpH-dependent stability:

Data Source

PatentEP4616859A1Room temperature stability of ophthalmological compositions comprising aceclidine
Publication Date: 2025.09.17 LENZ THERAPEUTICS OPERATIONS INC
  • EP4616859A1 patent drawingFigure 1A~1B
  • EP4616859A1 patent drawingFigure 1C~1D
  • EP4616859A1 patent drawingFigure 2A~2B

AI summary

The present disclosure provides aqueous compositions comprising aceclidine that are stable at room temperature for prolonged periods of time.