Kinetic Stability and Glass-Forming Ability of Thermally Labile Quinolone Antibiotics

The application of drugs in the amorphous state is one way to improve their bioavailability. As such, the determination of the optimal conditions for production and the assessment of the stability of the amorphous system are actively researched topics of present-day pharmaceutical science. In the present work, we have studied the kinetic stability and glass-forming ability of the thermally labile quinolone antibiotics using fast scanning calorimetry. The critical cooling rates for avoiding crystallization of the melts of oxolinic and pipemidic acids and sparfloxacin were determined to be 10 000, 40, and 80 K·s –1, respectively. The studied antibiotics were found to be “strong” glass formers. Based on a combination of nonisothermal and isothermal kinetic approaches, the Nakamura model was suitable for describing the crystallization process of the amorphous forms of the quinolone antibiotics.