Measurement of artemisinin and its derivatives in biological fluids

The development of selective analytical methods for the determination of artemisinin and its analogues and metabolites in biological fluids poses challenging problems. All are thermally labile, lack ultraviolet (u.v.) absorbent or fluorescent chromophores and do not possess functional groups for derivatization. Two chemical approaches have been used; acid (or alkali) catalysed decomposition to u.v. absorbing compounds followed by high-performance liquid chromatography (HPLC) of the decomposition products, and HPLC with reductive electrochemical detection. Each has its difficulties. The first, although sensitive, may lack specificity if drug metabolities are also converted to identical products, but a recently developed method surmounts this problem. The second, while providing good sensitivity and specificity, requires rigorous deoxygenation of the sample and mobile phase and an electrochemical detector, which is expensive, and may prove difficult to operate under field conditions. As an alternative to a chemical method, a bioassay may be suitable for plasma level monitoring in such circumstances. However its lack of selectivity means it is of questionable value in the determination of the pharmacokinetic parameters for individual drug-related species.