Lyophilized Antibacterial Injection Formulation for Solubility and Stability
Find Innovative SolutionsGenerate Solutions
Solution Overview
Problem
The compound of Formula (I) requires improved solubility in pharmaceutically acceptable vehicles for parenteral administration and stability during long-term storage to effectively treat bacterial infections, particularly those with multiple drug resistance.
Innovation Solution
A formulation comprising a compound of Formula (I) or its salt, a solubilizing agent, a hydrotropic agent, and a pH modifier, along with a lyophilized and reconstituted formulation process, to enhance solubility and stability.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Quantity of substance
If the compound of Formula (I) is formulated for parenteral administration, then the solubility in pharmaceutically acceptable vehicles is improved, but the stability during long-term storage deteriorates
Solution Approach 1:
The patent applies parameter changes by modifying the physical state of the formulation through lyophilization (freeze-drying). This transforms the liquid formulation into a solid lyophilized cake, which dramatically improves storage stability while maintaining the solubility benefits. The process changes temperature, pressure, and moisture content parameters to achieve the desired stability-solubility balance.
Solution Approach 2:
The patent utilizes phase transitions inherent in the lyophilization process. The formulation undergoes freezing (liquid to solid), primary drying (ice sublimation to vapor), and secondary drying (desorption of bound water). These phase transitions remove bulk water while maintaining the drug in a stable solid state, resolving the contradiction between solubility and stability.
2Quantity of substance
If the compound of Formula (I) is formulated with solubilizing agents and hydrotropic agents, then the solubility is improved, but the formulation complexity increases
Solution Approach 1:
The patent merges multiple formulation components (solubilizing agents, hydrotropic agents, pH modifiers) into a single integrated lyophilized formulation. By combining these elements and removing water through lyophilization, the patent reduces formulation complexity while maintaining improved solubility characteristics. The final product is a single dry cake that incorporates all necessary solubility-enhancing components.
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 achieves improved solubility and stability, enabling effective treatment of various bacterial infections, including those with multiple drug resistance, and maintains stability for extended periods.
Implementation Method 1
lyophilized injectable pharmaceutical formulations
Implementation Method 2
lyophilized formulation
Implementation Method 3
a solubilising agent
Implementation Method 4
a hydrotropic agent
Data Source
AI summary
The present disclosure provides a formulation comprising a compound of Formula (I) or its salt thereof with a solubilising agent, a hydrotropic agent, and a pH modifier. The present disclosure also provides a lyophilized formulation and a reconstituted formulation. The present disclosure further provides a process of preparing the formulations and methods thereof. Formula (I)