Benakis A, Schopfer C, Paris M, Plessas C T, Karayannakos P E, Dondas I, Kotsarelis D, Plessas S T, Skalkeas G
Department of Pharmacology, University of Geneva, Switzerland.
Eur J Drug Metab Pharmacokinet. 1991 Oct-Dec;16(4):325-8. doi: 10.1007/BF03189978.
A pharmacokinetic study has been conducted in six beagle dogs after i.m. administration of 25 mg/kg of arteether, a qinghaosu (artemisinin) derivative of high anti-malarial activity. Arteether plasma concentrations were measured during a 24 h period using HPLC with an electrochemical detector in the reductive mode. The pharmacokinetic parameters were established using an open two-compartment model. Results showed a relatively rapid absorption phase: T1/2ka was 0.300 +/- 0.096 h and a mean elimination half-life of 27.95 +/- 11.93 h. Cmax was 110 +/- 16 ng/ml, Cltot/F was 1.69 +/- 0.34 ml/min and AUC was 2797 +/- 476 ng/ml/h.
对6只比格犬进行了一项药代动力学研究，这些犬经肌肉注射给予25mg/kg蒿甲醚（一种具有高抗疟活性的青蒿素（青蒿琥酯）衍生物）。在24小时内，使用具有电化学检测器的高效液相色谱法在还原模式下测量蒿甲醚的血浆浓度。药代动力学参数采用开放二室模型确定。结果显示吸收期相对较快：吸收半衰期（T1/2ka）为0.300±0.096小时，平均消除半衰期为27.95±11.93小时。峰浓度（Cmax）为110±16ng/ml，总清除率（Cltot/F）为1.69±0.34ml/分钟，曲线下面积（AUC）为2797±476ng/ml/h。
