Stable Triamcinolone Acetonide Suspensions for Suprachoroidal Injection
Find Innovative SolutionsGenerate Solutions
Solution Overview
Problem
Existing triamcinolone acetonide suspensions for ocular injection face challenges with stability, resuspendability, and particulate issues, requiring vigorous shaking and immediate use to prevent settling, which complicates administration and may lead to clogging.
Innovation Solution
Development of triamcinolone acetonide suspensions that are essentially particulate- and aggregate-free, prepared through a process involving specific agents and sonication, ensuring uniformity and stability for easy administration via suprachoroidal injection.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Stability of the object's composition
If triamcinolone acetonide suspension is prepared with conventional methods, then the suspension can be formulated, but it requires vigorous shaking and immediate use to prevent settling, indicating poor stability and resuspendability
Solution Approach 1:
The patent modifies physical parameters of the suspension by controlling particle size (D70 < 5 μm) and using specific excipients with optimized concentrations to achieve stable suspension without requiring vigorous shaking
Solution Approach 2:
The patent introduces specific excipients as intermediaries: wetting agents (polysorbate 80, tyloxapol) to improve particle dispersion, viscosity agents (carboxymethylcellulose sodium) to maintain suspension stability, and tonicity agents to ensure physiological compatibility, thereby eliminating the need for vigorous shaking and immediate use
2Ease of operation
If the suspension is made to be stable and readily resuspendable, then administration ease improves, but the formulation complexity increases due to multiple agents required
Solution Approach 1:
The patent employs multi-functional excipients that simultaneously perform multiple functions: carboxymethylcellulose sodium provides both viscosity control and suspension stability; polysorbate 80 and tyloxapol serve as wetting agents to prevent aggregation; the combination achieves stable, readily resuspendable suspension without requiring multiple separate additive systems
3Reliability
If the suspension contains particulate matter, then the formulation is simpler, but it causes clogging in fine-gauge needles and compromises safety
Solution Approach 1:
The patent removes harmful particulate matter from the suspension formulation by implementing strict particle size control (D70 < 5 μm) and using filtration/centrifugation steps during manufacturing, thereby eliminating clogging risks while maintaining formulation effectiveness
Solution Approach 2:
The patent changes the particle size parameter to D70 < 5 μm and controls the distribution of particle sizes to ensure no aggregates form, thereby preventing clogging in fine-gauge needles while maintaining suspension stability and effectiveness
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 suspensions are stable, readily resuspendable, and free of visible particulates, allowing for consistent delivery through fine-gauge needles without clogging, enhancing administration efficiency and safety.
Implementation Method 1
providing an essentially particulate-free second solution comprising one or more wetting agents in an aqueous solvent
Implementation Method 2
sonicating the suspension of Step (d), wherein the suspension comprises about 40 mg/mL of triamcinolone acetonide
Data Source
AI summary
The present disclosure relates to pharmaceutical suspensions of triamcinolone acetonide, methods of producing such suspensions and methods of using of such suspensions. The pharmaceutical suspensions of the present disclosure are stable and suitable for administration by suprachoroidal injection through a 30-gauge microneedle.