Characterization of melt-quenched and milled amorphous solids of gatifloxacin. (1st November 2016)

• Record Type: Journal Article
• Authors: Hattori, Yusuke; Suzuki, Ayumi; Otsuka, Makoto
• Is Part Of: Drug development and industrial pharmacy. Volume 42:Number 11(2016:Nov.)
• Page Start: 1851
• Page End: 1856
• Publication Date: 2016-11-01
• Subjects: Amorphous solid -- gatifloxacin -- non-isothermal DSC -- time-resolved near-infrared spectroscopy -- X-ray diffraction; Pharmaceutical chemistry -- Periodicals; Pharmaceutical industry -- Periodicals; Drug Industry -- Periodicals; Technology, Pharmaceutical -- Periodicals; 615.05
• DOI: 10.1080/03639045.2016.1179752
• Languages: English
• ISSNs: 0363-9045

Abstract

Abstract: The objectives of this study were to characterize and investigate the differences in amorphous states of gatifloxacin. We prepared two types of gatifloxacin amorphous solids coded as M and MQ using milling and melt-quenching methods, respectively. The amorphous solids were characterized via X-ray diffraction (XRD), nonisothermal differential scanning calorimetry (DSC) and time-resolved near-infrared (NIR) spectroscopy. Both the solids displayed halo XRD patterns, the characteristic of amorphous solids; however, in the non-isothermal DSC profiles, these amorphous solids were distinguished by their crystallization and melting temperatures. The Kissinger–Akahira–Sunose plots of non-isothermal crystallization temperatures at various heating rates indicated a lower activation energy of crystallization for the amorphous solid M than that of MQ. These results support the differentiation between two amorphous states with different physical and chemical properties.