Vancomycin Aqueous Composition for Room-Temperature Stability
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Solution Overview
Problem
Existing vancomycin compositions for intravenous use are inconvenient due to the need for freezing storage and thawing before administration, and some contain excipients that pose risks during pregnancy.
Innovation Solution
Aqueous solution compositions of vancomycin stabilized by D-lactic acid and polyols like propylene glycol, sucrose, or glycerol, with osmolarity controlled between 400-1250 mOsm/L, allowing for stable, ready-to-administer formulations without the need for dilution.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Stability of the object's composition
If vancomycin is formulated as a frozen premixed solution, then storage stability is improved, but ease of operation deteriorates due to required thawing before use
Solution Approach 1:
The patent changes the formulation parameters by replacing freezing conditions with room temperature stability through the use of specific excipients (mannitol, sodium acetate, acetic acid) that stabilize vancomycin in liquid form without requiring frozen storage, thereby eliminating the thawing step while maintaining stability
Solution Approach 2:
The patent creates a composite formulation by combining vancomycin with specific stabilizing excipients (mannitol as a bulking agent, sodium acetate and acetic acid as pH buffers) that work together to provide room temperature stability, transforming the storage requirements from frozen to ambient conditions
2Stability of the object's composition
If vancomycin is formulated with certain excipients for stability, then storage stability is improved, but object-affected harmful factors worsen due to fetal malformation risks
Solution Approach 1:
The patent removes the harmful excipients (N-acetyl-D-alanine and PEG400) from the formulation and replaces them with safe alternatives (mannitol, sodium acetate, acetic acid) that provide equivalent or superior stability without the fetal malformation risk, thereby extracting the harmful components while maintaining the beneficial stability property
Solution Approach 2:
The patent replaces the problematic excipients with safer, well-established pharmaceutical excipients (mannitol, sodium acetate, acetic acid) that have known safety profiles and are commonly used in parenteral formulations, providing a safer alternative that achieves the same formulation goals without harmful effects
Data Source
AI summary
There is provided inter alia a storage stable aqueous solution composition comprising vancomycin or a pharmaceutically acceptable salt thereof, at a concentration of 1-10 mg/mL; D-lactic acid or a pharmaceutically acceptable salt thereof; and a polyol selected from the group consisting of propylene glycol, sucrose, glycerol, trehalose, lactose, glucose, sorbitol and mannitol, or a mixture thereof; wherein the osmolarity of the composition is 400-1250 mOsm/L.