Preserved Surfactant Formulations Preventing Phase Separation
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Solution Overview
Problem
Current protein and peptide-based drug products requiring surfactants for stability cannot be preserved for multi-use due to incompatibility between surfactants and preservatives, leading to phase separation and the need for single-use formulations, which increases costs and waste.
Innovation Solution
Incorporating a solvent modifier at sufficient concentrations to prevent phase separation in formulations containing non-ionic surfactants and phenolic preservatives above their concentration threshold, ensuring the solution remains clear and stable for extended periods.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Stability of the object's composition
If surfactants are included in formulations at concentrations necessary for protein stability, then protein stability is improved, but the formulation cannot be preserved for multi-use due to phase separation when preservatives are added
Solution Approach 1:
The patent introduces a third component (preservative) that mediates between the conflicting requirements of surfactant stability and formulation preservation. By adding preservatives like phenol or metacresol at specific concentrations (0.5-5% w/v), the formulation achieves both protein stability through surfactants and preservation capability, resolving the phase separation issue that previously prevented multi-use formulations
Solution Approach 2:
The patent changes the concentration parameters of multiple components simultaneously - maintaining surfactant concentrations (0.01-1% w/v) for protein stability while adding preservatives at optimized concentrations (0.5-5% w/v) to prevent microbial growth. This parameter optimization allows the formulation to achieve both stability and preservation without phase separation
2Reliability
If preservatives are added in sufficient concentrations to meet regulatory requirements for sterility, then antimicrobial effectiveness is improved, but phase separation occurs due to interaction with surfactants
Solution Approach 1:
The patent optimizes the concentration parameters of both preservatives and surfactants to prevent phase separation. By specifying preservative concentrations in the range of 0.5-5% w/v and surfactant concentrations in the range of 0.01-1% w/v, the formulation maintains regulatory antimicrobial effectiveness while preserving formulation homogeneity and preventing visible precipitates
3Device complexity
If single-use formulations are used to avoid preservation issues, then formulation simplicity is improved, but costs and waste increase
Solution Approach 1:
The patent introduces preservatives as a mediating component that enables multi-use formulations by preventing microbial contamination. This allows the formulation to be used multiple times (e.g., in multi-dose pens or vials) without compromising sterility, thereby reducing product waste and costs while maintaining formulation simplicity through the use of well-established preservative agents
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
Enables the creation of stable, multi-use injectable formulations by preventing phase separation, allowing for the use of surfactants and preservatives at concentrations necessary for stability and antimicrobial effectiveness without cloudiness or precipitation, thereby reducing waste and costs.
Implementation Method 1
Incorporating a solvent modifier at sufficient concentrations to prevent phase separation in formulations containing non-ionic surfactants and phenolic preservatives above their concentration threshold, ensuring the solution remains clear and stable for extended periods.
Implementation Method 2
one or more solvent modifiers, such as propylene glycol (PPG), N-methyl-2-pyrrolidone (NMP), polyethylene glycol (PEG) 400 or glycerol
Data Source
AI summary
The present invention relates to preserved, surfactant-containing pharmaceutical compositions that are suitable for parenteral administration.