Crystalline versus amorphous content of Lumaxis (TM) analog XP280 using X-ray and electron diffraction methods

In the course of the development of Lumaxis(TM) (roxifiban), the physical s tate of XP280 (the besylate salt of the active metabolites of roxifiban) an d SC887 (the mesylate salt of the free base of roxifiban) were characterize d. Powder X-ray diffraction patterns of XP280 were ambiguous in that a high degree of background signal was present and potentially indicative of the existence of an amorphous phase. Herein the results of combined synchrotron X-ray diffraction and electron microscopy (diffraction and imaging) studie s on XP280 and SC887 are reported. The combination of these two techniques allowed an unambiguous assessment of the crystallinity, as well as determin ation of four of the unit cell parameters of XP280 and complete determinati on of the unit cell parameters for SC887. (C) 2000 Wiley-Liss, Inc. and the American Pharmaceutical Association.