关键词: 硫酸氢氯吡格雷, 多晶体, 离心力辅助析晶, 热稳定性

Abstract:

Of all reported polymorphs of clopidogrel hydrogen sulfate, Form I is difficult to produce and store owing to its poor thermostability. It is reported that Form I can spontaneously transform into Form II at high temperature and humidity. In this study, high purity Form I of clopidogrel hydrogen sulfate with good thermodynamic stability was prepared by a centrifugation-assisted recrystallization technology. The resultant product was characterized by powder X-ray diffraction (PXRD), differential scanning calorimetry (DSC) and scanning electron microscope (SEM). The results showed that the crystallinity and crystallite size of the Form I prepared by the centrifugation-assisted recrystallization method were larger than those obtained by conventional anti-solvent recrystallization methods. Long-term thermostability testing demonstrated that the improved product can keep stable crystal structure even at high temperature and humidity.

Key words: Clopidogrel hydrogen sulfate, Polymorph, Centrifugation-assisted recrystallization, Thermostability