Multicomponent crystals of an artemisinin derivative and cinchona alkaloids for use as antimalarial drugs

Pharmaceutical multicomponent crystals (MCCs) including salts and co-crystals of active pharmaceutical ingredients (APIs), are an active focus of research to improve various physicochemical properties of drugs. In this work, we demonstrate that the pharmaceutical artesunate (AS), a derivative of art...

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Veröffentlicht in:CrystEngComm 2021-10, Vol.23 (39), p.6843-6847
Hauptverfasser: Jiang, Qi, Hirsh, David A, Tu, Yifan, Luo, Laibin
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Sprache:eng
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Zusammenfassung:Pharmaceutical multicomponent crystals (MCCs) including salts and co-crystals of active pharmaceutical ingredients (APIs), are an active focus of research to improve various physicochemical properties of drugs. In this work, we demonstrate that the pharmaceutical artesunate (AS), a derivative of artemisinin (ART), forms a 1 : 1 salt with two cinchona alkaloids: quinine (QN) and cinchonidine (CND), representing the first report of MCCs combining two major types of antimalarial drugs. Multicomponent crystals of an artemisinin derivative and cinchona alkaloids were produced, combining two major types of antimalaria drugs with unique hydrogen bond interactions. These salts demonstrate a new category of antimalarial pharmaceuticals.
ISSN:1466-8033
1466-8033
DOI:10.1039/d1ce00974e