A new derivative detected in accelerated ageing of artesunate-amodiaquine fixed dose combination tablets

作者:Charrier Cedric; Bertho Gildas; Petigny Olivier; Moneton Philippe; Azerad Robert*
来源:Journal of Pharmaceutical and Biomedical Analysis, 2013, 81-82: 20-26.
DOI:10.1016/j.jpba.2013.03.009

摘要

An unknown impurity detected in small amounts during the heat treatment of artesunate-amodiaquine bilayer tablets was purified by semipreparative HPLC and identified by MS and NMR as the tetrahydrofuranyl acetate-rearranged derivative of anhydrodihydroartemisinin. When anhydrodihydroartemisinin was treated with a Fe-II salt in acetonitrile water solution, the same product was generated, together with an isomeric 2-deoxy-4 alpha-hydroxy-anhydrodihydroartemisinin derivative, as expected from the usual homolytic radical opening of the endoperoxide bond previously described for other artemisinin derivatives.

  • 出版日期2013-8