Rapamycin Liquid Formulation Stabilization
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Solution Overview
Problem
Rapamycin degrades due to temperature effects in liquid formulations, requiring frozen storage, which is impractical for users and poses challenges in transportation.
Innovation Solution
A formulation sealing vessel containing 2% rapamycin, 94% polyethylene glycol, and 4% ethanol, with no antioxidants, is used, allowing for long-term stabilization even at refrigeration temperatures of 2° C. to 8° C.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Ease of operation
If rapamycin is stored in liquid formulation at refrigeration temperature (2°C to 8°C), then ease of operation and transportation is improved, but stability of the substance deteriorates due to degradation
Solution Approach 1:
The patent applies parameter changes by modifying the chemical composition parameters of the liquid formulation. Specifically, it uses a solvent system comprising polyethylene glycol (94% w/w) and ethanol (4% w/w) to dissolve rapamycin (2% w/w), creating a stable liquid formulation that maintains potency without requiring frozen storage conditions. This parameter optimization enables refrigeration-level storage while preserving drug stability.
2Reliability
If rapamycin is stored in frozen state (−20°C), then stability of the substance is improved, but ease of operation and transportation deteriorates
Solution Approach 1:
The patent changes the physical state parameter of the formulation from frozen to liquid by optimizing the solvent composition. The specific parameter set (polyethylene glycol 94%, ethanol 4%, rapamycin 2%) enables the formulation to remain liquid and stable at refrigeration temperatures, eliminating the need for frozen storage and thereby improving ease of operation and transportation while maintaining substance stability.
3Reliability
If antioxidant is added to liquid formulation, then stability of rapamycin is improved, but device complexity and manufacturing complexity increases
Solution Approach 1:
The patent applies the extraction principle by removing the antioxidant component from the formulation. The stable liquid formulation achieves rapamycin stabilization through the optimized solvent system (polyethylene glycol and ethanol) without requiring additional antioxidant additives, thereby simplifying the formulation composition and reducing manufacturing complexity while maintaining drug stability.
Solution Approach 2:
The patent employs a simple, minimalistic formulation approach using only three components (polyethylene glycol, ethanol, and rapamycin), eliminating the need for complex antioxidant systems. This simplified formulation is more economical and easier to manufacture while achieving the desired stability through the carefully selected solvent ratio.
Data Source
AI summary
In order to enable long-term stabilization of rapamycin contained in a liquid formulation, a formulation sealing vessel of the present invention includes: a sealed vessel body in which a liquid formulation containing 2% (w/w) rapamycin or a salt thereof, 94% (w/w) polyethylene glycol, and 4% (w/w) ethanol is sealed, the sealed vessel body having a volume of 0.1 mL to 1.0 mL, the liquid formulation containing no antioxidant, and the liquid formulation having a total volume of 0.02 mL to 1.0 mL.