Capturing two new salts of the anticancer drug gefitinib

Abstract

In this text, the new crystal forms of geffitinib were explored through evaporation solution crystallization experiment. The formation of salts was confirmed by the single crystal X-ray diffraction, powder X-ray diffraction, thermo gravimetric analysis and differential scanning calorimetry, Raman spectroscopy, hot-stage microscopy and Hirshfeld surface analysis. Furthermore, Hirshfeld surface analysis confirmed that the driving force and supporting force for the formation of crystals were C-C, C-H, N-H, H-H, O-H and Cl-H interactions. The dissolution rate of the new salts of gefitinib in phosphate buffer of pH 6.8 was evaluated, and the results showed a significant increase in solubility.

Keywords:

• Crystal structure
• Hirshfeld surface
• salt
• thermal analysis
• X-ray diffraction

Disclosure statement

No potential conflict of interest was reported by the authors.

Additional information

Funding

The authors thank the Open Project of Shandong Collaborative Innovation Center for Antibody Drugs, No. CIC-AD1805.