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. 2010 Jul 22:9:212.
doi: 10.1186/1475-2875-9-212.

The pharmaceutical death-ride of dihydroartemisinin

Frans Herwig Jansen  1
Affiliations

The pharmaceutical death-ride of dihydroartemisinin

Frans Herwig Jansen. Malar J. .

Abstract

In the 2010 second edition of WHO's guidelines for the treatment of malaria, the relatively new fixed dose combination dihydroartemisinin-piperaquine is included as one of the recommended artemisinin combination therapies. However, experimental testing demonstrates that, due to its intrinsic chemical instability, dihydroartemisinin is not suitable to be used in pharmaceutical formulations. In addition, data show that the currently available dihydroartemisinin preparations fail to meet the internationally accepted stability requirements. At a time when many efforts aim to ban counterfeit and substandard drugs from the malaria market, the obvious question rises how WHO and public-private partnerships, such as Medicine for Malaria venture (MMV), can support the production and marketing of anti-malarial drugs that do not even meet the International Pharmacopoeia requirements?

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Figures

Figure 1
Figure 1
Structure of artemisinin (A), dihydroartemisinin (B), artesunate (C) and artemether (D). The insert shows the lacton (for artemisinin) and trioxane functional groups (marked in red).
Figure 2
Figure 2
Interconversion of α/β epimers of dihydroartemisinin with ring opening.
See this image and copyright information in PMC

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