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New Applications of Electron Microscopy in Pharmaceuticals: Crystallinity Assessment and Polymorph Determination

Published online by Cambridge University Press:  02 July 2020

Z. G. Li ,
L. Liang ,
R. L. Harlow ,
C. M. Foris ,
R. E. Olson ,
T. M. Sielecki ,
J. Liu ,
R. D. Vickery  and
M. B. Maurin
Z. G. Li
Affiliation:
Central Research & Development, DuPont Company, Wilmington, DE19880-0228
L. Liang
Affiliation:
Central Research & Development, DuPont Company, Wilmington, DE19880-0228
R. L. Harlow
Affiliation:
Central Research & Development, DuPont Company, Wilmington, DE19880-0228
C. M. Foris
Affiliation:
Central Research & Development, DuPont Company, Wilmington, DE19880-0228
R. E. Olson
Affiliation:
The DuPont Pharmaceuticals Company, P.O. Box 80500, Wilmington, DE19880-0500
T. M. Sielecki
Affiliation:
The DuPont Pharmaceuticals Company, P.O. Box 80500, Wilmington, DE19880-0500
J. Liu
Affiliation:
The DuPont Pharmaceuticals Company, P.O. Box 80500, Wilmington, DE19880-0500
R. D. Vickery
Affiliation:
The DuPont Pharmaceuticals Company, P.O. Box 80500, Wilmington, DE19880-0500
M. B. Maurin
Affiliation:
The DuPont Pharmaceuticals Company, P.O. Box 80500, Wilmington, DE19880-0500
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Extract

Recently, transmission electron microscopy has been used in crystallinity assessments and unit cell parameter/polymorph determinations in solid drug substances [1,2]. Lumaxis™ (roxifiban) is a glycoprotein nb/ffla (GPHb/HIa) antagonist discovered recently at The DuPont Pharmaceuticals Company [3] currently undergoing clinical evaluation for the treatment of thrombotic disorders. Lumaxis™ is converted in vivo to a zwitterionic active metabolite, XV459. As reported here, we have assessed by electron microscopy and x-ray diffraction the crystallinity of XP280, the benzenesulfonate salt of XV459, and determined the unit cell parameters of SC877, the methanesulfonate salt of the methyl ester of XV459.

Crystallinity assessment. Partial or complete transformation of crystalline phases into amorphous phases can occur during production processes that may ultimately affect the activity associated with various batches of a drug [4, 5]. Whether desired or not, the amorphous content of any drug substance is thus an important issue for the pharmaceutical industry.

Type
Microscopy and Microanalysis in the Pharmaceutical Industry
Information
Microscopy and Microanalysis , Volume 6 , Issue S2: Proceedings: Microscopy & Microanalysis 2000, Microscopy Society of America 58th Annual Meeting, Microbeam Analysis Society 34th Annual Meeting, Microscopical Society of Canada/Societe de Microscopie de Canada 27th Annual Meeting, Philadelphia, Pennsylvania August 13-17, 2000 , August 2000 , pp. 1004 - 1005
Copyright
Copyright © Microscopy Society of America

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References

References:

1.Li, Z. G. et al., J. Pharmaceutical Sciences, 88 (1999)297.CrossRefGoogle Scholar
2.Li, Z. G. et al., J. Pharmaceutical Sciences (submitted).Google Scholar
3.Chu, C. et al., J. Med. Chem., 40 (1997)2064.Google Scholar
4.Byrn, S. R., The Solid State Chemistry of Drugs, New YorkAcademy Press, (1982).Google Scholar
5.Brittain, H. G. (editor), Polymorphous in Pharmaceutical Solids, New YorkMarcel Dekker(1999).Google Scholar