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Antisolvent Recrystallization Strategy to Screen Appropriate Carriers to Stabilize Filgotinib Amorphous Solid
Fuzheng Ren1, Hanjing Sun2, Lin Cui2
1Laboratory of Pharmaceutical Crystal Engineering & Technology, School of Pharmacy, East China University of Science and Technology, Shanghai 200237, China; Shanghai Key Laboratory of New Drug Design, School of Pharmacy, East China University of Science and Technology, Shanghai 200237, China.
Journal of Pharmaceutical Sciences
|February 19, 2018
Summary
A new microscopic method rapidly screens polymers for amorphous solid dispersions (ASDs). This technique effectively stabilizes filgotinib (FTN) ASDs, enhancing drug dissolution and formulation efficacy.
Area of Science:
- Pharmaceutical Sciences
- Materials Science
- Drug Delivery
Background:
- Amorphous solid dispersions (ASDs) enhance drug solubility and bioavailability.
- Stabilizing amorphous drugs within polymeric carriers is crucial for preventing recrystallization.
- Filgotinib (FTN) is a drug candidate requiring advanced formulation strategies.
Purpose of the Study:
- To develop a rapid screening method for selecting appropriate polymers for filgotinib (FTN) ASDs.
- To validate the screening method using accelerated experimentation.
- To investigate the stabilization mechanisms and dissolution enhancement of FTN ASDs.
Main Methods:
- Microscopic observation after antisolvent recrystallization for polymer screening.
- Solvent evaporation technique for preparing FTN ASDs.
- Fourier-transform infrared spectroscopy, Raman scattering, and nuclear magnetic resonance for characterizing drug-polymer interactions.
- Flory-Huggins interaction parameter and water sorption isotherms for evaluating interaction strength.
Main Results:
- The developed microscopic method effectively screened polymers for FTN ASD formulation.
- Hydrogen bonding between FTN and polymers was identified as critical for ASD stabilization.
- ASDs significantly improved the dissolution rate of FTN, with polymers exhibiting solubilization effects.
- Accelerated experimentation validated the screening method's efficacy.
Conclusions:
- Microscopic observation after antisolvent recrystallization is a valuable preliminary tool for polymer selection in ASD design.
- Understanding drug-polymer interactions, particularly hydrogen bonding, is key to stabilizing ASDs.
- FTN ASDs demonstrate improved dissolution profiles, highlighting the potential of this formulation approach.
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