Crystalline versus amorphous content of lumaxistrade mark analog XP280 using X-ray and electron diffraction methods.
In the course of the development of Lumaxistrade mark (roxifiban), the physical state of XP280 (the besylate salt of the active metabolites of roxifiban) and SC887 (the mesylate salt of the free base of roxifiban) were characterized. 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) studies on XP280 and SC887 are reported. The combination of these two techniques allowed an unambiguous assessment of the crystallinity, as well as determination of four of the unit cell parameters of XP280 and complete determination of the unit cell parameters for SC887.
Li
Z G
ZG
Central Research & Development, Science & Engineering Laboratory, Experimental Station, DuPont Company, Wilmington, Delaware 19880-0228, USA. zhigang-rick.li@usa.dupont.com
Liang
L
L
Harlow
R L
RL
Foris
C M
CM
Olson
R E
RE
Sielecki
T M
TM
Liu
J
J
Vickery
R D
RD
Maurin
M B
MB
D000578:Amidines / Q000737:chemistry* / Q000378:metabolism; D002317:Cardiovascular Agents / Q000737:chemistry* / Q000378:metabolism; D003460:Crystallization; D007555:Isoxazoles / Q000737:chemistry* / Q000378:metabolism; D008698:Mesylates / Q000737:chemistry*; D008854:Microscopy, Electron / Q000379:methods; D014961:X-Ray Diffraction / Q000379:methods
D000578:Amidines; D002317:Cardiovascular Agents; D007555:Isoxazoles; D008698:Mesylates; C118235:roxifiban