Remifentanil Injection Stability via Composite Solvent
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Solution Overview
Problem
Current remifentanil injection solutions are unstable during long-term storage and require a complicated two-stage preparation process, which increases the risk of medication errors and storage instability.
Innovation Solution
A remifentanil injection solution formulation is developed that includes remifentanil and/or its physiologically acceptable salts, water, and a stabilizer like polyethylene glycol, with specific ratios to ensure stability and prevent denaturation, allowing for a one-step preparation and long-term storage stability.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Ease of operation
If remifentanil is formulated as an aqueous injection solution, then ease of operation and solubility are improved, but storage stability deteriorates
Solution Approach 1:
The patent uses a composite solvent system comprising water and a non-aqueous solvent (such as ethanol, propylene glycol, or polyethylene glycol) in specific proportions. This composite formulation allows remifentanil to remain soluble while significantly improving storage stability, resolving the contradiction between ease of preparation and storage stability.
Solution Approach 2:
The patent optimizes the concentration of remifentanil and the ratio of water to non-aqueous solvent within specific ranges. By controlling these parameters, the formulation achieves both good solubility for easy preparation and enhanced storage stability, preventing the deterioration that occurs in pure aqueous solutions.
2Quantity of substance
If lyophilized remifentanil powder is reconstituted with a large amount of water, then sufficient dissolution is achieved, but internal pressure rises causing solution leakage
Solution Approach 1:
The patent formulates remifentanil injection solutions with optimized concentrations and solvent compositions that allow complete dissolution without generating excessive internal pressure. This prevents container leakage while ensuring sufficient dissolution of the active ingredient.
3Measurement precision
If a two-stage preparation process is used to prepare remifentanil injection solution, then concentration control is improved, but device complexity and risk of medication errors increase
Solution Approach 1:
The patent provides pre-formulated remifentanil injection solutions with precisely controlled concentrations manufactured in advance. This merges the dissolution and concentration control steps into a single ready-to-use product, eliminating the complex two-stage preparation process and reducing medication errors while maintaining concentration accuracy.
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 maintains a high survival rate of remifentanil, preventing denaturation and precipitation, enabling easy one-step preparation of the final injection solution at the anesthetic site, thus enhancing storage stability and reducing the risk of medication errors.
Implementation Method 1
a stabilizer, said stabilizer being polyethylene glycol or propylene glycol
Implementation Method 2
containing remifentanil and/or physiologically acceptable salts thereof, water
Data Source
AI summary
A remifentanil injection solution formulation contains remifentanil and/or physiologically acceptable salts thereof, water, and a stabilizer, the remifentanil injection solution formulation contains said water at a rate of 0.007 to 0.025mL per 1mg of said remifentanil.