title: Physicochemical properties of amorphous roxithromycin prepared by quench cooling of the melt or desolvation of a chloroform solvate.
abstract: Roxithromycin is a poorly soluble antibacterial drug. The aim of this study was to prepare and characterize an amorphous form of roxithromycin. The amorphous form was prepared by desolvation of its chloroform solvate, and by quench cooling a melt of the crystalline monohydrated solid. The X-ray powder diffraction pattern of the desolvated chloroform solvate was indistinguishable from that of the glass prepared by melting, which indicated that it was amorphous. The roxithromycin glass was determined to be a fragile glass, but due to its high Kauzmann temperature (approximately 8°C), it should remain fairly stable upon refrigeration or even at room temperature. It was also determined that this glass remains stable in the presence of moisture with no indication of crystallization.
authors.affiliation: Unit for Drug Research and Development, Faculty of Health Sciences, Private Bag X6001, North-West University, Potchefstroom, 2520, South Africa. Marique.Aucamp@nwu.ac.za
authors.forename: Marique
authors.initials: M
authors.lastname: Aucamp
authors.forename: Wilna
authors.initials: W
authors.lastname: Liebenberg
authors.forename: Schalk J
authors.initials: SJ
authors.lastname: Strydom
authors.forename: Elsa C
authors.initials: EC
authors.lastname: van Tonder
authors.forename: Melgardt M
authors.initials: MM
authors.lastname: de Villiers
mesh_terms: D000900:Anti-Bacterial Agents / Q000737:chemistry*; D002152:Calorimetry, Differential Scanning; D002626:Chemistry, Pharmaceutical; D002725:Chloroform / Q000737:chemistry*; D003460:Crystallization; D018360:Crystallography, X-Ray; D004355:Drug Stability; D004356:Drug Storage; D007700:Kinetics; D008956:Models, Chemical; D033362:Powder Diffraction; D015575:Roxithromycin / Q000737:chemistry*; D012995:Solubility; D012997:Solvents / Q000737:chemistry*; D013499:Surface Properties; D013678:Technology, Pharmaceutical / Q000379:methods*; D044366:Transition Temperature; D014867:Water / Q000737:chemistry
chemical_list: D000900:Anti-Bacterial Agents; D012997:Solvents; D014867:Water; D015575:Roxithromycin; D002725:Chloroform