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2-氟-双脱氧胞苷(2FddC)是一种天然核苷的类似物,它在哺乳动物细胞中可代谢为2FddC三磷酸酯,后者能较强地抑制HIV-1病毒反转录酶,而对哺乳动物的γ聚合酶的抑制较弱。本工作研究了2FddC在艾滋病患者体内的药动学,由此提出2FddC口服剂量的合理范围,使其血药峰浓度接近IC_(50)值(150ng/ml)。 HIV-1抗体反应呈阳性的病人(18～45岁)21名,分为两组进行平行交叉实验。第一组依次接受iv 0.01,0.1 mg/kg和po 0.1mg/kg剂量的2FddC。第二组病人依此接受
2-Fluoro-dideoxycytidine (2FddC) is an analogue of natural nucleosides that is metabolized in mammalian cells to 2FddC triphosphate, which strongly inhibits HIV-1 viral reverse transcriptase , While the inhibition of mammalian gamma polymerase is weak. This work studied the pharmacokinetics of 2FddC in patients with AIDS, and proposed a reasonable range of oral doses of 2FddC, so that the peak plasma concentration near the IC 50 value (150ng / ml). Twenty-one patients (18-45 years old) with positive HIV-1 antibody response were divided into two groups and subjected to parallel crossover experiments. The first group received 2FddC in doses of iv 0.01, 0.1 mg / kg and po 0.1 mg / kg in turn. The second group of patients accepted it accordingly