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Preparation and Solid-State Characterization of Eltrombopag Crystal Phases
Vincenzo Mirco Abbinante1, Massimo Zampieri2, Giuseppe Barreca2
1Dipartimento di Scienza e Alta Tecnologia & To.Sca.Lab., Università dell'Insubria, via Valleggio 11, 22100 Como, Italy.
Molecules (Basel, Switzerland)
|December 30, 2020
Summary
Eltrombopag free acid exhibits over 20 crystal forms, including hydrates and solvates. This study characterizes these polymorphs and their stability using X-ray diffraction and thermal analysis for better drug quality control.
Area of Science:
- Crystallography
- Pharmaceutical Science
- Solid-State Chemistry
Background:
- Eltrombopag is a key drug for treating thrombocytopenia.
- Its free acid form exists in numerous crystalline polymorphs, including hydrates and solvates.
- Characterizing these forms is crucial for pharmaceutical manufacturing and quality control.
Purpose of the Study:
- To comprehensively index and characterize the diverse crystal forms of eltrombopag free acid.
- To elucidate the stability fields and interconversion processes of these polymorphs.
- To identify new crystalline forms and solvates.
Main Methods:
- Preparation and crystallization of 13 monophasic eltrombopag free acid samples.
- X-ray powder diffraction (XRPD) for crystal form identification and indexing.
- Simultaneous thermogravimetric (TGA) and calorimetric (DSC) analyses for thermal stability.
- Variable temperature X-ray diffraction studies to observe phase transitions.
Main Results:
- Complete indexing of 13 monophasic samples, revealing diverse crystal structures.
- Detailed mapping of stability fields for various crystalline forms, hydrates, and solvates.
- Observation of interconversion processes between different solid forms.
- Identification of novel crystalline polymorphs and solvates.
Conclusions:
- The study provides a clear understanding of eltrombopag free acid's polymorphic landscape.
- Accurate crystallographic and thermal data are essential for identifying and quantifying crystal forms in industrial settings.
- The findings contribute to improved control over eltrombopag drug substance manufacturing.
