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Publication Details
AFRICAN RESEARCH NEXUS
SHINING A SPOTLIGHT ON AFRICAN RESEARCH
Stability-indicating HPLC-DAD/UV-ESI/MS impurity profiling of the anti-malarial drug lumefantrine
Malaria Journal, Volume 10, Article 51, Year 2011
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Description
Background: Lumefantrine (benflumetol) is a fluorene derivative belonging to the aryl amino alcohol class of anti-malarial drugs and is commercially available in fixed combination products with -artemether. Impurity characterization of such drugs, which are widely consumed in tropical countries for malaria control programmes, is of paramount importance. However, until now, no exhaustive impurity profile of lumefantrine has been established, encompassing process-related and degradation impurities in active pharmaceutical ingredients (APIs) and finished pharmaceutical products (FPPs). Methods. Using HPLC-DAD/UV-ESI/ion trap/MS, a comprehensive impurity profile was established based upon analysis of market samples as well as stress, accelerated and long-term stability results. In-silico toxicological predictions for these lumefantrine related impurities were made using Toxtree* and Derek*. Results: Several new impurities are identified, of which the desbenzylketo derivative (DBK) is proposed as a new specified degradant. DBK and the remaining unspecified lumefantrine related impurities are predicted, using Toxtree* and Derek*, to have a toxicity risk comparable to the toxicity risk of the API lumefantrine itself. Conclusions: From unstressed, stressed and accelerated stability samples of lumefantrine API and FPPs, nine compounds were detected and characterized to be lumefantrine related impurities. One new lumefantrine related compound, DBK, was identified and characterized as a specified degradation impurity of lumefantrine in real market samples (FPPs). The in-silico toxicological investigation (Toxtree* and Derek*) indicated overall a toxicity risk for lumefantrine related impurities comparable to that of the API lumefantrine itself. © 2011 Verbeken et al; licensee BioMed Central Ltd.
Authors & Co-Authors
Verbeken, Mathieu
Belgium, Ghent
Universiteit Gent
Suleman, Sultan
Belgium, Ghent
Universiteit Gent
Ethiopia, Jimma
Jimma University
Baert, Bram
Belgium, Ghent
Universiteit Gent
Vangheluwe, Elien
Belgium, Ghent
Universiteit Gent
Van Dorpe, Sylvia
Belgium, Ghent
Universiteit Gent
Burvenich, Christian
Belgium, Ghent
Universiteit Gent
Duchateau, Luc
Belgium, Ghent
Universiteit Gent
Jansen, Frans Herwig
Belgium, Brussels
Fondation Act-ion Afrique
De Spiegeleer, Bart M.J.
Belgium, Ghent
Universiteit Gent
Statistics
Citations: 26
Authors: 9
Affiliations: 3
Identifiers
Doi:
10.1186/1475-2875-10-51
e-ISSN:
14752875
Research Areas
Infectious Diseases
Substance Abuse