Ionic Liquid Compositions for Pharmaceutical Polymorphism Control
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Solution Overview
Problem
The challenge of polymorphism and pseudo-polymorphism in pharmaceuticals and other compounds leads to variations in physical and chemical properties, making it difficult to achieve consistent quality, bioavailability, and regulatory compliance, as well as posing challenges in solubility and delivery.
Innovation Solution
The development of ionic liquid compositions that are amorphous and non-crystalline, allowing for controlled and tunable chemical, biological, and physical properties, and enabling controlled release and improved solubility by using specific ion combinations that avoid the issues associated with crystalline forms.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Stability of the object's composition
If crystalline forms of pharmaceutical compounds are used, then structural stability is improved, but polymorphism and pseudo-polymorphism cause variations in physical and chemical properties leading to inconsistent quality and bioavailability
Solution Approach 1:
The patent transforms the crystalline solid state into a liquid state by changing the physical parameters (temperature, molecular arrangement), thereby eliminating polymorphism while maintaining stability through the liquid ionic liquid composition
Solution Approach 2:
The patent uses composite ionic liquid compositions containing multiple ions (e.g., cholinium, carboxylate, alkyl chains) that work together to provide both stability and consistent properties without crystalline structure
2Ease of manufacture
If solvent molecules are incorporated into crystal lattice during crystallization, then crystal formation is facilitated, but entrapped solvent molecules affect the three-dimensional crystal lattice and create pseudo-polymorphs with varying properties
Solution Approach 1:
The patent extracts the compound from the crystalline state and dissolves it in ionic liquid, removing the crystal lattice structure and any entrapped solvent molecules, thereby eliminating pseudo-polymorphism
Solution Approach 2:
The ionic liquid acts as an intermediary solvent that dissolves the pharmaceutical compound without forming crystal lattices, preventing solvent entrapment and lattice distortion
3Ease of manufacture
If traditional crystalline pharmaceutical forms are used, then manufacturing processes are established, but solubility and delivery problems persist
Solution Approach 1:
The patent changes the physical state from solid crystal to liquid, and modifies the molecular environment using ionic liquids with tunable properties, thereby improving solubility and delivery while maintaining manufacturability
Solution Approach 2:
The ionic liquid composition serves multiple functions: it acts as a solvent, a delivery vehicle, and a stability enhancer, replacing multiple separate components used in traditional crystalline formulations
Data Source
AI summary
Disclosed are ionic liquids and methods of preparing ionic liquid compositions of active pharmaceutical, biological, nutritional, and energetic ingredients. Also disclosed are methods of using the compositions described herein to overcome polymorphism, overcome solubility and delivery problems, to control release rates, add functionality, enhance efficacy (synergy), and improve ease of use and manufacture.