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目的 探讨模拟失重条件下以血流量改变为生理基础的药代动力学变化。方法 选择庆大霉素作为模型药物，采用头低位（ － ２０°） 兔限制活动为模拟失重动物模型，观察模拟失重对兔庆大霉素药代动力学参数的影响。７ 只家兔在头低位７ ｄ 前后，分别静脉滴注了３ ｍｇ／ｋｇ 的庆大霉素，用 Ｔ Ｄｘ Ｆ Ｌｘ 测定了给药后４ ｈ 内的血药浓度。结果 庆大霉素的分布变慢，这表现在α值由头低位前的（０ ．１８３８ ±０ ．１０７６）ｍｉｎ － １ 降至头低位后的（０ ．０５９１ ±０ ．０３３４） ｍｉｎ － １ ，ｔ１／２α由（５ ．３０ ±３ ．５５） ｍｉｎ 延长为（１５ ．０４ ±７ ．４９）ｍｉｎ ， Ｋ１２ 由（０ ．１０２５ ±０ ．０７２１） ｍｉｎ － １ 降至（０ ．０１８１ ±０ ．０１６１） ｍｉｎ１ ，都有显著性差异； Ｖ（ Ｃ） 、 Ｖ（ Ｄ） 也有升高的趋势。庆大霉素清除率在模拟失重后也有所增加， Ｃ Ｌ（ Ｓ） 从（２ ．２ ±０ ．５）ｍｌ·ｍｉｎ１·ｋｇ１ 升至（２ ．７ ±０ ．３）ｍｌ·ｍｉｎ１·ｋｇ１ 。结论 模拟失重可改变药代动力学过程。
Objective To investigate the pharmacokinetic changes of blood flow to physiological basis under simulated weightlessness. Methods Gentamicin was selected as a model drug and the rabbit head restraint (-20 °) activity was used as a model animal model of simulated weightlessness. The effects of simulated weightlessness on gentamicin pharmacokinetic parameters were observed. Seven rabbits were given intravenous drip of gentamicin 3 mg / kg before and after the head low 7 days, respectively, and the blood concentration of the rabbits was determined within 4 h after administration by T Dx F Lx. Results The distribution of gentamicin was slowed down, which showed that the value of α decreased from (0.1838 ± 0.1076) min - 1 before the head low to (0.0591 ± 0.0334) min - 1, t1 / 2α was prolonged from (5.30 ± 3.55) min to (15.04 ± 7.49) min, and K12 was decreased from (0.1025 ± 0.0721) min -1 to (0.0181 ± 0.11) 0161) min 1, there are significant differences; V (C), V (D) also increased. Gentamycin clearance also increased after simulated weightlessness. C L (S) increased from (2.2 ± 0.5) ml · min1 · kg1 to (2.70 ± 0.3) ml · Min 1 · kg 1. Conclusion Simulated weightlessness can change the pharmacokinetic process.