Rocuronium Stabilization with Polyhydroxy Acids
Find Innovative SolutionsGenerate Solutions
Solution Overview
Problem
Current neuromuscular blocking agents are unstable in aqueous solutions, particularly at elevated temperatures, requiring cool chain shipment and storage, which is inconvenient and costly, and they have insufficient long-term stability for room temperature storage and shipment.
Innovation Solution
An aqueous composition comprising a quaternary ammonium neuromuscular blocking agent, such as Rocuronium, stabilized with a polyhydroxy acid like D-gluconic acid or its lactone, which inhibits hydrolytic degradation, allowing for thermal sterilization and storage at room temperature without cooling.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Ease of operation
If neuromuscular blocking agents are formulated as ready-to-use aqueous solutions, then convenience of use is improved, but stability is worsened requiring cool chain storage
Solution Approach 1:
A zwitterionic stabilizer acts as an intermediary substance between the neuromuscular blocking agent and the aqueous environment, protecting the active ingredient from hydrolytic degradation and enabling stable ready-to-use formulations without cool chain requirements
Solution Approach 2:
The formulation changes the chemical environment by introducing zwitterionic substances that alter the aqueous solution properties, creating a stable matrix that prevents degradation of the neuromuscular blocking agent at room temperature
2Device complexity
If neuromuscular blocking agents are stored at room temperature, then logistics complexity is reduced, but degradation increases reducing shelf life
Solution Approach 1:
The zwitterionic stabilizer serves as a protective intermediary that enables room temperature storage by preventing direct interaction between the neuromuscular blocking agent and degrading aqueous environments, eliminating cool chain logistics while maintaining shelf life
3Stability of the object's composition
If cool chain storage is implemented, then stability is improved, but cost and environmental impact increase
Solution Approach 1:
The formulation converts the potentially harmful aqueous environment into a stabilizing matrix by adding zwitterionic substances, transforming what would cause degradation into a protective system that eliminates the need for energy-intensive cool chain storage
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 stabilization of neuromuscular blocking agents with polyhydroxy acids extends their shelf life, eliminates the need for cool chain storage, and enables thermal sterilization without affecting stability, enhancing environmental sustainability and reducing costs.
Implementation Method 1
an aqueous composition comprising a quaternary ammonium neuromuscular blocking agent and a stabilizer selected from a polyhydroxy acid
Implementation Method 2
enables thermal sterilization without affecting stability
Data Source
AI summary
The present invention relates to an aqueous composition comprising:(i) a steroidal neuromuscular blocking agent that is a Rocuronium salt, further wherein the steroidal neuromuscular blocking agent is present at a concentration ranging from 5 mg/mL to 20 mg/mL based on the total volume of the aqueous composition; and(ii) an excipient that includes D-gluconic acid, D-glucono-delta-lactone, or a combination thereof, where the steroidal neuromuscular blocking agent and the excipient are dissolved in a solution consisting of water.Furthermore the present invention relates to a liquid pharmaceutical composition comprising or consisting of said aqueous composition and a method for producing said aqueous composition.