Ball milling – a new concept for predicting degradation profiles in active pharmaceutical ingredients

Reinhard P. Kaiser; Everaldo F. Krake; Laura Backer; Jonas Urlaub; Wolfgang Baumann; Norbert Handler; Helmut Buschmann; Torsten Beweries; Ulrike Holzgrabe; Carsten Bolm

doi:10.1039/D1CC04716G

Ball milling – a new concept for predicting degradation profiles in active pharmaceutical ingredients†

Reinhard P. Kaiser,^a Everaldo F. Krake,

^b Laura Backer,^c Jonas Urlaub,^c Wolfgang Baumann,

^b Norbert Handler,^d Helmut Buschmann,^d Torsten Beweries,

*^b Ulrike Holzgrabe

*^c and Carsten Bolm

*^a

Author affiliations

* Corresponding authors

^a RWTH Aachen University, Institute of Organic Chemistry, Landoltweg 1, 52074 Aachen, Germany
E-mail: carsten.Bolm@oc.rwth-aachen.de

^b Leibniz-Institut für Katalyse e.V., Albert-Einstein-Str. 29a, 18059 Rostock, Germany
E-mail: torsten.beweries@catalysis.de

^c Institut für Pharmazie und Lebensmittelchemie, Am Hubland, 97074 Würzburg, Germany
E-mail: ulrike.holzgrabe@uni-wuerzburg.de

^d RD&C Research, Development & Consulting GmbH, Neuwaldegger Strasse 35/2/3, 1170 Vienna, Austria

Abstract

A method for forced oxidative mechanochemical degradation of active pharmaceutical ingredients (APIs) using clopidogrel hydrogensulfate as a model compound is presented. Considerable and selective formation of degradants occurs already after very short reaction times of less than 15 minutes and the nature of the products is strongly dependent on the used oxidant.

Chemical Communications

Ball milling – a new concept for predicting degradation profiles in active pharmaceutical ingredients†

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Ball milling – a new concept for predicting degradation profiles in active pharmaceutical ingredients

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