Aripiprazole Injectable Suspension for Stable Redispersion
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Solution Overview
Problem
Aripiprazole injectable suspensions suffer from particle aggregation and settling during long-term storage, making them difficult to redisperse, which is a challenge in maintaining stability and patient compliance.
Innovation Solution
The formulation includes a cellulose-based suspending agent and polyoxyethylene (20) sorbitan monooleate in a specific ratio, along with optional mannitol and buffer salts, to create a stable injectable suspension that maintains long-acting and sustained-release properties.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Duration of action of moving object
If aripiprazole is formulated as an injectable suspension, then long-acting sustained-release properties are achieved, but particles aggregate and settle during long-term storage making them difficult to redisperse
Solution Approach 1:
The patent introduces a specific suspending agent system comprising cellulose-based suspending agent in combination with polyoxyethylene (20) sorbitan monooleate as an intermediary substance. This mediator prevents particle aggregation and settling while maintaining sustained-release properties, resolving the contradiction between long-acting duration and storage stability.
Solution Approach 2:
The invention uses a composite suspending agent system combining cellulose-based suspending agent with polyoxyethylene (20) sorbitan monooleate. This composite material provides both the sustained-release capability needed for long-acting formulation and the stability required to prevent particle aggregation during storage.
2Stability of the object's composition
If freeze-dried technology is used to prepare lyophilized powder, then particle aggregation and settling problems are avoided, but production complexity and cost increase
Solution Approach 1:
The patent replaces the complex freeze-drying process with a simpler suspending agent-based formulation approach. This eliminates the need for expensive and complex lyophilization equipment while achieving comparable or superior stability through the cellulose-based suspending agent system.
Solution Approach 2:
The invention changes the formulation parameters by introducing specific suspending agents and their ratios instead of relying on freeze-drying conditions. This parameter change transforms the approach from process-intensive (freeze-drying) to formulation-intensive (suspending agent selection), reducing production complexity.
3Ease of manufacture
If particles are allowed to settle during storage, then formulation simplicity is maintained, but redispersion becomes difficult and patient compliance decreases
Solution Approach 1:
The suspending agent system acts as an intermediary that maintains particle suspension without requiring complex formulation techniques. The cellulose-based suspending agent combined with polyoxyethylene (20) sorbitan monooleate prevents settling while keeping the formulation simple to manufacture, and ensures easy redispersion if settling occurs.
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 formulation achieves prolonged shelf life with particles remaining stable and easily redispersible, ensuring sustained drug release for up to 6 weeks and maintaining therapeutic efficacy.
Implementation Method 1
it comprises a cellulose-based suspending agent and polyoxyethylene (20) sorbitan monooleate
Implementation Method 2
the combination of cellulose-based suspending agent and polyoxyethylene (20) sorbitan monooleate is especially suitable for preparing aripiprazole suspension injectable formulation, so as to overcome the drawback that particles would aggregate and settle
Implementation Method 3
the injectable formulation sustainedly releases a therapeutic effective amount of aripiprazole during a period of at least 1 week, preferably 2 weeks, 3 weeks or 4 weeks, and up to 6 weeks or longer
Implementation Method 4
After injection, the injectable formulation sustainedly releases a therapeutic effective amount of aripiprazole
Data Source
AI summary
The present invention belongs to the field of pharmaceutical formulation, and particularly relates to an aripiprazole injectable suspension formulation having prolonged shelf life, and methods of using the formulation in treating schizophrenia and related diseases. In another aspect, the present invention also relates to a method of prolonging shelf life of an aripiprazole injectable suspension formulation.