Sodium Deoxycholate Carrier for Tunicamycin Solubility
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Solution Overview
Problem
The clinical adoption of modified tunicamycins has been limited by their poor water solubility and the toxicity of existing solubilizing agents, hindering their intravenous administration in large animals and pharmacological studies.
Innovation Solution
The development of aqueous formulations comprising sodium deoxycholate (DOC) with antibiotics like tunicamycin, which form stable complexes that enhance solubility and reduce toxicity, allowing for effective intravenous administration.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Reliability
If modified tunicamycins are used as antibiotics, then antibacterial activity is improved, but water solubility deteriorates
Solution Approach 1:
Sodium deoxycholate acts as an intermediary substance that forms soluble complexes with hydrophobic modified tunicamycins, enabling their dissolution in aqueous formulations while maintaining their antibacterial activity. The bile salt mediates between the hydrophobic antibiotic molecules and the hydrophilic aqueous environment.
2Quantity of substance
If existing solubilizing agents like DMSO are used, then water solubility is improved, but toxicity increases
Solution Approach 1:
The invention replaces expensive and toxic solubilizing agents like DMSO with a biocompatible, naturally occurring bile salt (sodium deoxycholate) that is safe for intravenous administration. This substitution eliminates the need for toxic solvents while achieving the same solubilization function.
3Reliability
If modified tunicamycins are administered intravenously, then clinical effectiveness is improved, but safety deteriorates due to toxicity of solubilizing agents
Solution Approach 1:
The invention changes the chemical composition parameters of the formulation by substituting toxic organic solvents with physiologically compatible bile salts. This parameter change maintains the solubility function while dramatically improving the safety profile for intravenous administration in large animals.
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 use of sodium deoxycholate-based formulations improves the stability, solubility, and bioactivity of tunicamycins, enabling their safe and effective use in veterinary medicine without the need for toxic solvents like DMSO.
Implementation Method 1
aqueous formulation comprising an antibiotic and sodium deoxycholate (DOC)... form stable complexes that enhance solubility
Data Source
AI summary
The disclosure provides stable aqueous formulations comprising an antibiotic and sodium deoxycholate (DOC), and optionally further comprising at least one carrier and/or excipient. The disclosure also provides methods for preparing such aqueous formulations, and methods for using such aqueous formulations to treat, attenuate, or prevent bacterial infection in a subject.