The investigation of polymorph transition of erlotinib salts
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Abstract
Erlotinib is a reversible tyrosine kinase inhibitor, which acts on the epidermal growth factor receptor (EGFR) and is used to treat non-small cell lung cancer (NSCLC), pancreatic cancer and several other types of cancer [1]. It is known that erlotinib forms different salts which can exist in multiple crystalline solid forms. This important property known as a polymorphism may have an impact on physical and chemical stability of the drug substance (API), processability during manufacturing in the final drug product and bioavailability of the drug to the patient. Changes in the crystal structure of API can lead to the undesired changes in properties. Hence, the control of the polymorphic form is essential during the drug substance manufacture and requires a thorough understanding of solid-state changes that may occur in pharmaceutical materials. To achieve a comprehensive understanding of solid-state transformations different analytical techniques are applied. In our studies the variable–temperature powder X-ray diffraction (VT–PXRD), differential scanning calorimetry (DSC), thermogravimetry (TGA), Fourier transformed infrared (FTIR), attenuated total reflectance (ATR) and Raman spectroscopy were used to investigate the correlation between the thermal behavior and structural transformations of polymorphic forms of erlotinib salts. VT-PXRD method has detected the temperature range of the existence of polymorphic transitions, spectroscopy methods have characterized intramolecular vibrations and thermal methods have provided information on the transition and melting temperature and relationships between polymorphic forms.
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2016. The investigation of polymorph transition of erlotinib salts. PeerJ Preprints 4:e1835v1 https://doi.org/10.7287/peerj.preprints.1835v1Author comment
This is an abstract submitted to the X MKNOL Conference.
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Competing Interests
The authors declare that they have no competing interests.
Author Contributions
Wioleta Maruszak conceived and designed the experiments, performed the experiments, analyzed the data, contributed reagents/materials/analysis tools, wrote the paper, prepared figures and/or tables, reviewed drafts of the paper.
Marta Łaszcz conceived and designed the experiments, performed the experiments, analyzed the data, contributed reagents/materials/analysis tools.
Kinga Trzcińska conceived and designed the experiments, performed the experiments, analyzed the data, contributed reagents/materials/analysis tools.
Wojciech Łuniewski conceived and designed the experiments, performed the experiments, contributed reagents/materials/analysis tools.
Krzysztof Bańkowski conceived and designed the experiments, performed the experiments, contributed reagents/materials/analysis tools.
Kamil Jatczak performed the experiments, contributed reagents/materials/analysis tools.
Data Deposition
The following information was supplied regarding data availability:
The research in this article did not generate any raw data.
Funding
This research project has been supported by the European Union within European Regional Development Fund through grant program INNOMED/I/15/NCBR/2014 “Modern API technology and pharmaceutical composition of kinase inhibitor generic drug for cancer therapy” X-ray measurements were accomplished at the Structural Research Lab. of the Chemistry Department, Warsaw University, Poland, established with the financial support from the European Regional Development Found in the Sectoral Operational Programme “Improvement of the Competitiveness of Enterprises, years 2004–2006” project no: WKP_1/1.4.3./1/2004/72/72/165/2005/U. The funders had no role in study design, data collection and analysis, decision to publish, or preparation of the manuscript.
