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Composition Dependency of the Flory-Huggins Interaction Parameter in Drug-Polymer Phase Behavior
Jana Klueppelberg1, Ulrich A Handge2, Markus Thommes1
1Laboratory of Solids Process Engineering, Department of Biochemical and Chemical Engineering, TU Dortmund University, Emil-Figge-Street 68, 44227 Dortmund, Germany.
Pharmaceutics
|December 23, 2023
Summary
This study enhances amorphous solid dispersion (ASD) modeling by extending Flory-Huggins theory. The improved model accurately predicts drug-polymer solubility temperatures, crucial for developing new oral medications.
Area of Science:
- Materials Science
- Pharmaceutical Sciences
- Physical Chemistry
Background:
- Amorphous solid dispersions (ASDs) are key for oral delivery of poorly soluble drugs, requiring understanding of drug-polymer interactions.
- Current models like Flory-Huggins theory lack accuracy for strong drug-polymer interactions, hindering effective ASD product design.
Purpose of the Study:
- To develop an improved modeling strategy for predicting drug-polymer phase behavior in ASDs.
- To enhance the accuracy of solubility temperature predictions by extending the Flory-Huggins interaction parameter.
Main Methods:
- Experimental evaluation of the composition dependency of the Flory-Huggins interaction parameter for diverse drug-polymer systems.
- Development and validation of an extended Flory-Huggins model incorporating drug fraction correlation.
Main Results:
- The extended model demonstrated high accuracy in predicting solubility temperatures for nine exemplary ASD formulations.
- The model showed particular strength at low drug fractions, effectively capturing composition-dependent drug-polymer interactions.
Conclusions:
- The proposed modeling strategy significantly improves the prediction of drug-polymer solubility temperatures in ASDs.
- This enhanced predictive capability is vital for accelerating the development of novel and effective amorphous solid dispersion products.
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