Pharmacokinetic and pharmacodynamic aspects of artelinic acid in rodents.

The efficacy of artelinic acid and artemisinin, orally administered at 10 and 50 mg kg-1 day-1, was compared in Plasmodium berghei infected mice. Subsequently, the pharmacokinetics of artelinic acid after intravenous, intramuscular, oral and rectal administration of a 20 mg kg-1 aqueous solution to rabbits were studied in a four-way randomized cross-over experiment. After intravenous administration, artelinic acid concentrations in blood plasma were high (C0: 76 +/- 15 mg L-1), and the drug was rapidly eliminated from the central compartment, showing linear elimination kinetics with an elimination half-life of 15 +/- 3 min.

Assay of artelinic acid in serum by high-performance liquid chromatography.

A simple and rapid high-performance liquid chromatographic method with UV detection for the determination in serum of the antimalarial artelinic acid is described. Artelinic acid is a water-soluble semi-synthetic derivative of artemisinin (or Qinghaosu), which is the parent compound of a completely new class of antimalarials with great potential value. Calibration curves of artelinic acid in serum from 0.

The pharmacokinetics of artemisinin after oral, intramuscular and rectal administration to volunteers.

The pharmacokinetics after oral, intramuscular and rectal administration of artemisinin, a new potent antimalarial drug, to healthy volunteers has been examined. The study was set-up as a four-way cross-over design with a wash-out period of one week between the test days. In ten volunteers artemisinin concentrations in serum were monitored using a reversed phase HPLC assay with UV detection after derivatization.

The parenteral controlled release of liposome encapsulated chloroquine in mice.

Free (0.6 mg), and liposome encapsulated chloroquine (0.6, 3 mg), were injected intraperitoneally, intramuscularly and subcutaneously in mice.