摘要
本文报道用放射免疫测定法研究口服青蒿琥酯片剂的生物利用度,结果为静脉注射青蒿琥酯后的血药时程为二房室模型,T1/2β为33.96±4.73分钟;口服青蒿琥酯片剂后的血药时程为一房室模型,其达峰时间为53.07±20.58分钟,峰浓度为1.94±1.05mg/L(1.94±1.05μg/ml),T1/2k为41.35±17.89分钟,绝对生物利用度为40.39±14.99％。结果提示口服青蒿琥酯片剂后,在人体内的吸收速度较快,而吸收程度较差。
The pharmacokinetics and the bioavailability of Artesunate were investigated in the present study by using radioimmunoassay to measure serum concentration periodically for 9 hrs (i.v.) and 15 hrs (p.o.) in the healthy subjects. The concentration time data were analysed with the MCPKP-automatic pharmacokinetic program on an IBM microcom- puter. The result showed that the concentration time course after i.v. administration (120mg) were fitted to a linear two-compartment open model and the pharmacokinetics after p.o. Artesunate tablet (120mg) was described by one compartment open model. The maximum serum concentration (Cmax) and the time to maximum serum con- centration (Tmax) of oral administration are 1.94±1.05(μg/ml) and 53±20 (rain) respec- tively; T(1/2)k is 41.35±17.89 (min) and the absolute bioavailability is 40.39±14.99%. The result suggested that the Artesunate tablet is absorbed rapidly but the bioavailability is low.
关键词
青蒿素
药代动力学
抗疟药
ARTEMISININ/pharmacokinetics
ARTEMISININ/analogs and derivatives
ARTEMISININ/administration and dosage
