Study on the Polymorphism and Transformation of Fluconazole

OBJECTIVE To investigate the polymorphism and transformation of fluconazole. METHODS The polymorphism of fluconazole was analyzed by IR, NIR, Raman, XRD and TGA. The influences of temperature, humidity, solvent and grind on crystal transformation were explored. RESULTS Crystal form of 18 batch of samples from 10 manufacturers were defined as form Ⅱ, form Ⅲ and monohydrate by XRD. Form Ⅱ and monohydrate were interconvertible in different temperatures, humidities and solvents. Form I of fluconazole was obtained by recrystallizing in chloroform and melting in high temperature. CONCLUSION Crystal forms of fluconazole can be controlled since their characteristics are significantly different. Form I, form Ⅱ and monohydrate are interconvertible and the transformation condition is established.