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Polymorphism of Chlorpropamide on Liquid-Assisted Mechanical Treatment: Choice of Liquid and Type of Mechanical Treatment Matter Full article

Journal CrystEngComm
ISSN: 1466-8033
Output data Year: 2018, Volume: 20, Number: 13, Pages: 1797-1803 Pages count : 7 DOI: 10.1039/c7ce02221b
Tags WATER-SOLUBLE DRUGS; HIGH-PRESSURE POLYMORPHISM; PHARMACEUTICAL COCRYSTALS; CONFORMATIONAL POLYMORPHISM; MECHANOCHEMICAL SYNTHESIS; SOLID-STATE; FORM; CRYSTALS; NANOSUSPENSIONS; FORMULATION
Authors Bouvart Nadia 1,2 , Palix Roland-Marie 1,2 , Arkhipov Sergey G. 1,3 , Tumanov Ivan A. 1,3 , Michalchuk Adam A.L. 1,4,5 , Boldyreva Elena V. 1,3
Affiliations
1 Novosibirsk State University, Novosibirsk, Russian Federation
2 ESCOM, 1 allée du réseau J.-M. Buckmaster, 60200 Compiègne, France
3 Institute of Solid State Chemistry and Mechanochemistry, SB RAS, Novosibirsk, Russian Federation
4 EaStChem School of Chemistry, University of Edinburgh, Edinburgh, UK
5 EPSRC Centre for Continuous Manufacturing and Crystallisation (CMAC), UK

Funding (5)

1 Russian Foundation for Basic Research 16-33-60086 (АААА-А15-115121840103-1)
2 The Ministry of Education and Science of the Russian Federation
3 The University of Edinburgh
4 Engineering and Physical Sciences Research Council CMAC 1/1033459/1
5 Federal Agency for Scientific Organizations 0301-2018-0007

Abstract: Different types of mechanical treatment (tableting, grinding, milling, etc.) are important technological operations in the pharmaceutical industry. Solid materials are not merely comminuted during such treatment, but can undergo polymorphic transitions and amorphisation. A liquid is often added to the solid sample on purpose, e.g. in order to facilitate comminution. In many cases, liquid is present inadvertently, either as a result of trace solvent following up-stream operations, or sorbed from the atmosphere. This work explores the liquid-assisted mechanical treatment of two metastable forms of a model pharmaceutical compound chlorpropamide (CPA), namely the β- and ϵ-forms. We investigate the stability of these polymorphs to mechanical treatment in the presence of a series of fluids that have affinity for different fragments of the CPA molecule. In addition to variation in fluids, the effect of different mechanical treatment is explored, employing model shear and restricted impact devices, alongside grinding in a mortar. CPA offers a clear example of the drastically different results of shear and impact on mechanochemical polymorphism, on the importance of the careful selection of solvent for liquid-assisted treatment, and on the possible role of even trace quantities of solvent. Further, this work demonstrates the importance of the starting polymorph in determining the outcome of a mechanochemical process. All of these factors can have notable consequence on the outcome of technological operations that include mechanical treatment.
Cite: Bouvart N. , Palix R-M. , Arkhipov S.G. , Tumanov I.A. , Michalchuk A.A.L. , Boldyreva E.V.
Polymorphism of Chlorpropamide on Liquid-Assisted Mechanical Treatment: Choice of Liquid and Type of Mechanical Treatment Matter
CrystEngComm. 2018. V.20. N13. P.1797-1803. DOI: 10.1039/c7ce02221b WOS Scopus РИНЦ AN OpenAlex
Files: Full text from publisher
Dates:
Submitted: Dec 24, 2017
Accepted: Feb 10, 2018
Published online: Feb 12, 2018
Published print: Apr 7, 2018
Identifiers:
Web of science: WOS:000428985300006
Scopus: 2-s2.0-85044525259
Elibrary: 35516797
Chemical Abstracts: 2018:256917
OpenAlex: W2786078771
Citing:
DB Citing
Web of science 26
Scopus 27
OpenAlex 27
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