药学学报, 1984, 19(2): 81-84
引用本文:
曾衍霖;张银娣;许帼英;王长根;姜纪荣. 蒿甲醚在兔体内的药代动力学[J]. 药学学报, 1984, 19(2): 81-84.
ZENG Yan-lin; ZHANG Yin-di; XU Guo-ying; WANG Chang-gen and JIANG Ji-rong. THE PHARMACOKINETICS AND BIOAVAILABILITY OF OMETHYLDIHYDROARTEMESININE IN THE RABBIT[J]. Acta Pharmaceutica Sinica, 1984, 19(2): 81-84.

蒿甲醚在兔体内的药代动力学
曾衍霖;张银娣;许帼英;王长根;姜纪荣
中国科学院上海药物研究所;*南京医学院药理教研室
摘要:
本文报道蒿甲醚在兔体内的药代动力学。静脉输注蒿甲醚脂肪乳剂(蒿甲醚80mg/kg)后,血药时间数据用NONLIN程序拟合曲线,符合线性二室开模型。药代动力学参数的平均(SD)为:t1/2(αβ)分别为0.144(0.077)h和0.896(0.371)h;k21,k10和k12分别为1.235(0.705),4.143(1.370)和1.140(0.951)h-1;Vc,Vd(area)和Vd(ss)分别为0.609(0.119),2.985(0.787)和1.054(0.202)L/kg;清除率为2.401(0.339)L·kg-1·h。肌内注射油剂250mg/kg或125mg/kg,血药时间数据按矩量法计算,得吸收速率常数(Ka)为0.0377(0.0119)h-1;吸收程度为36.14(18.39)%。
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THE PHARMACOKINETICS AND BIOAVAILABILITY OF OMETHYLDIHYDROARTEMESININE IN THE RABBIT
ZENG Yan-lin; ZHANG Yin-di; XU Guo-ying; WANG Chang-gen and JIANG Ji-rong
Abstract:
The pharmacokinetics of o-methyldihydroartemisinine(MDHA, artemether) in rabbits was studied. MDHA fat emulsion was given to rabbits by intravenous infusion. Plasma C × t data were fitted to curves employing NONLIN program. The results indicated that the data fitted a two-compartment open model adequately. The pharmacokinetic parameters(mean±SD) are: t 1/2α, 0.144±0.077 h; t1/2β, 0.896±0.371 h; k21, 1.235±0.705 h-1; k10, 4.143±1.370 h-1; k12, 1.140±0.951 h-1; V1, 0.609±0.119 L/kg; Vd(area), 2.985±0.787 L/kg; Vdd(ss), 1.054±0.202 L/kg; Clearance, 2.401±0.339 L.kg-1. h. MDHA oil solution was given to rabbits intramuscularly. AUC was calculated by the trapezoidal rule. Bioavailability was estimated by statistical moments. The extent of absorption was found to be 36.14±18.39%, and the absorption rate constant was 0.0377±0.0119 h-1.
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