Artemisinin is rapidly absorbed from the gut after oral administration, 0.5 to 1 hour after the peak plasma concentration, decreased by half after four hours, 72 hours only a trace of blood. Its concentration in red blood cells is lower than plasma concentrations. After absorption and distribution in the tissue to the intestine, liver and kidney are more content. The product is fat-soluble substance, it can enter the brain through the blood-brain barrier. Quickly metabolized in the body, structure and properties of metabolites unclear. Mainly from the kidney and intestinal tract, can discharge 84% 24 hours, 72 hours only a small amount of residual. Since the metabolism and excretion are fast, effective blood concentration of short duration, is not conducive to completely kill the malaria parasite, so the higher recurrence rate. Artemisinin derivative artesunate, T1 / 2 was 0.5 hours, it should be repeated doses.
IndicationsMainly used for vivax malaria, falciparum malaria symptom control, and treatment of chloroquine-resistant insect strains, it can also be used to treat dangerous type of malignant malaria, such as cerebral, jaundice, and so on. Also for the treatment of systemic lupus erythematosus and discoid lupus erythematosus.
Chemical structureArtemisinin formula C15H22O5, molecular weight 282.33, component content: C 63.81%, H 7.85%, 28.33% O.
Physical and chemical propertiesColorless needle-like crystals, bitter taste. In acetone, ethyl acetate, chloroform, benzene and acetic acid soluble, soluble in ethanol and methanol, ether and petroleum ether, almost insoluble in water. Melting point: 156-157 ℃