Characterization and interconversion of polymorphs of premafloxacin, a new quinolone antibiotic

Journal of Pharmaceutical Sciences
W C SchinzerL M Madden

Abstract

The quinolone antibiotic premafloxacin crystallizes in at least five solid modifications, including three anhydrous phases (Forms I-III), a hydrate, and a methanolate. The anhydrous phases were studied by optical microscopy, X-ray powder diffraction, HPLC, hot-stage microscopy, dynamic moisture sorption gravimetry, differential scanning calorimetry, thermal gravimetry, and solution and isothermal calorimetry. Dry samples of Form I converted to Form II and ultimately to Form III through a sequence of melts and recrystallizations. Form III was stable to its melting temperature near 200 degrees C. Humidified samples of Form I converted directly to Form III via a moisture-mediated solid-state phase transformation at temperatures as low as 40 degrees C. The calorimetric and solubility data confirmed that Form III was lower in free energy and enthalpy than Form I at room temperature. Our investigation revealed that Form I was not crystallized directly from solution. Rather, Form I was the product of facile solid-state desolvation of the methanol solvate.

References

Feb 1, 1963·Journal of Pharmaceutical Sciences·W I HIGUCHIJ W SHELL

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Citations

Jul 5, 2003·Chemical & Pharmaceutical Bulletin·Katsuhiro KobayashiYuji Ohashi
Mar 17, 2005·Journal of Pharmaceutical Sciences·Madhu Pudipeddi, Abu T M Serajuddin
Jun 26, 2007·International Journal of Pharmaceutics·Lei Du-CunyManfred Kansy
Oct 20, 2006·International Journal of Pharmaceutics·Ann F FiorittoJames A Wesley
Jun 4, 2008·Journal of Psycholinguistic Research·James W MontgomeryMichelle H O'Malley
Oct 22, 2009·International Journal of Audiology·Jean L DesjardinLaurie S Eisenberg

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