Ionic Liquid Compositions for Pharmaceutical Polymorphism Control
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Solution Overview
Problem
Pharmaceuticals often exhibit polymorphism, leading to variations in physical and chemical properties that affect bioavailability, stability, and solubility, making it difficult to achieve consistent dosage and manufacturing processes, and there is a need for compositions with controllable properties to overcome solubility and delivery issues.
Innovation Solution
Development of ionic liquid compositions that can be used in pharmaceutical, biological, and nutritional applications, where the physico-chemical properties of pharmaceutical salts are modified by adding protic acids or bases to form new ionic liquid species, allowing for control over solubility, bioavailability, and polymorphism, and enabling controlled release of active compounds.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Reliability
If traditional crystallization methods are used to obtain pharmaceutical compounds, then the compound can be obtained in solid form, but the physical and chemical properties (solubility, bioavailability, stability) vary significantly due to polymorphism and pseudo-polymorphism
Solution Approach 1:
The patent applies parameter changes by transitioning from solid crystalline forms to liquid ionic liquid forms, fundamentally changing the physical state parameter. This allows continuous tuning of properties such as solubility, bioavailability, and stability by adjusting the ionic liquid composition ratios, thereby achieving both reliability and adaptability simultaneously
Solution Approach 2:
The patent uses composite materials by combining the pharmaceutical compound with ionic liquids to form eutectic mixtures. These composite systems exhibit synergistic effects where the ionic liquid component modulates the physical and chemical properties of the pharmaceutical, providing consistent and controllable performance across different formulations
2Reliability
If multiple polymorphic forms are investigated to find the optimal crystalline form, then the desired properties (solubility, stability, bioavailability) can be optimized, but the development time and experimental effort increase significantly
Solution Approach 1:
The patent exploits phase transitions by deliberately forming eutectic mixtures that melt at temperatures below the melting points of the individual components. This phase transition from solid to liquid state eliminates polymorphic issues while providing a single, well-defined system with tunable properties, significantly reducing development time and experimental complexity
Solution Approach 2:
The ionic liquid acts as an intermediary substance that mediates between the pharmaceutical compound and the biological system. By adjusting the ionic liquid-to-compound ratio, one can continuously optimize solubility, stability, and bioavailability without needing to screen multiple polymorphic forms, thereby reducing development time while achieving property optimization
3Reliability
If salts of the pharmaceutical compound are formed to control dissolution rate and solubility, then the desired release profile can be achieved, but extensive experimentation with different salts and solvents is required
Solution Approach 1:
The patent applies universality by using ionic liquids that can serve multiple functions simultaneously: they act as solubilizing agents, dissolution rate modifiers, stability enhancers, and bioavailability improvers. This multi-functionality eliminates the need to screen multiple different salts and solvents, as the ionic liquid system can achieve all desired effects through composition ratio adjustments, thereby simplifying manufacturing
Solution Approach 2:
The patent uses parameter changes by continuously varying the ionic liquid to pharmaceutical compound ratio to precisely control dissolution rate and solubility. This continuous parameter adjustment provides fine-tuned control over release profiles without requiring discrete salt formation experiments, significantly reducing manufacturing complexity and experimentation requirements
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 ionic liquid compositions provide a means to tune the physical and chemical properties of pharmaceuticals, enhancing bioavailability, stability, and solubility, and facilitating controlled release, thereby improving manufacturing and delivery processes.
Implementation Method 1
compositions of ionic liquids that are 'solvated,' for example, 'hydrated'
Data Source
AI summary
Disclosed herein are ionic liquid compositions comprising active pharmaceutical, biological, and nutritional compounds, and methods of use. Further disclosed are compositions of matter including liquid ion pairs alone or in solution and their use; compositions of ionic liquids that are ‘solvated,’ for example, ‘hydrated’ and their uses.