青蒿琥酯在奶牛体内的药代动力学与代谢

青蒿琥酯(artesunate,AS)是抗疟新药青蒿素的一个活性衍生物。近年来我国兽医工作者将其用于治疗牛羊泰勒氏焦虫病及双芽、巴贝斯焦虫病、鸡球虫病和耕牛血吸虫病,也收到了满意的效果。AS在大白鼠、兔、狗及人体内的药代动力学研究已见报道。本

PHARMACOKINETICS AND METABOLISM OF ARTESUNATE IN COWS

The pharmacokinetics of artesunate (AS) was studied in 3 cows, single dose of AS (5 mg/kg) were administered intravenously and the drug concentrations were determined by means of a TLC method developed in our laboratory. The plasma drug concentration-time course of AS, after the treatment with a pharmacokinetic microcomputer program MCPKP edited by Wen-Jiang Xia, was found to be best fitted to a two compartment open model and its pharmacokinetic parameters were as follows, T1/2 alpha = 2.43 min, T1/2 beta = 31.45 min, V1 = 0.124 L/kg, VB = 0.937 L/kg, ClB = 0.0215 L/kg. min, AUC = 236 mg/L.min. Dihydroartemisinine (DHA), the main active metabolite of AS in the bodies, was detected simultaneously. Peak plasma concentration of 3.5 micrograms/ml of DHA was reached at about 3 minutes after dosing and the AUC was 82 mg/L.min.