Analysis of Artesunate and Dihydroartemisinin Using a Syncronis C18 HPLC Column

Importance of Topic

Artesunate and dihydroartemisinin are frontline antimalarial agents recommended by the World Health Organization for treatment of severe and drug-resistant malaria. Accurate, reproducible quantification is essential for pharmaceutical quality control and pharmacokinetic studies, especially given the poor UV chromophore of artesunate and the need for mass spectrometric detection at low concentrations.

Objectives and Article Overview

This application note presents a rapid, MS-compatible HPLC method using the Thermo Scientific Syncronis C18 column to separate and quantify artesunate and its active α- and β-dihydroartemisinin metabolites. The approach overcomes limitations of UV-based protocols described in the WHO monograph.

Methodology and Instrumentation

A Thermo Scientific Accela 600 HPLC system equipped with a Syncronis C18 100×2.1 mm, 5 µm column was employed. The mobile phase consisted of water with 0.1 % formic acid and acetonitrile with 0.1 % formic acid (40:60 v/v). Key parameters:

• Flow rate: 0.2 mL/min
• Column temperature: 30 °C
• Injection volume: 1 µL
• Detection wavelength: 210 nm (compatible with MS coupling)

Main Results and Discussion

All analytes eluted in under 5 minutes with well-defined, symmetric peaks. Six replicate injections yielded %RSD values for retention times below 0.11 %, demonstrating excellent precision and column reproducibility. The low UV signal intensity underlines the necessity of MS detection for reliable quantification.

Benefits and Practical Applications

• Significantly reduced analysis time increases laboratory throughput
• MS-compatible mobile phase enables sensitive detection of low-level compounds
• Robust method supports consistent quality control in pharmaceutical production

Future Trends and Potential Uses

The described method can be extended to other artemisinin derivatives and combination therapies. Coupling with LC-MS/MS platforms may further enhance sensitivity and selectivity. Ongoing advancements in column technologies could lead to higher efficiency separations and lower solvent consumption.

Conclusion

The Thermo Scientific Syncronis C18 column facilitates a fast, reproducible, and MS-compatible HPLC analysis of artesunate and dihydroartemisinin, meeting stringent sensitivity and precision requirements for antimalarial drug development and quality control.

Reference

• World Health Organization. Artesunate: Final text for revision of The International Pharmacopoeia. QAS/09.340/Final December 2009.
• American Journal of Tropical Medicine and Hygiene. Analysis of artemisinin derivatives in plasma, 58(3):365–368 (1998).