A stable form of artemisinin wherein an artelinic acid or artesunic acid
is complexed with cyclodextrin analogs, preferably, .beta.-cyclodextrin.
The complexed cyclodextrin artemisinin formulation shields the peroxide
portion of the artemisinin backbone from hydrolytic decomposition
rendering it stable in solution. Artelinic acid and cyclodextrin are
placed into contact with one another to yield a 2:1 molecular species.
Artesunic acid and cyclodextrin yield a 1:1 molecular species. The
complexed cyclodextrin artemisinin formulation is effective for the
treatment of malaria and is stable in solution for long periods of time.