头低位（—20℃）限制活动7d对兔庆大霉素药代动力学的影响

目的 探讨模拟失重条件下以血流量改变为经代动力学变化。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７ｄ前后，分别静脉滴注了３ｍｇ／ｋｇ的庆大霉素，用ＴＤｘＦＬｘ测定了给药后４ｈ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（

Effects of 7 d head-down tilt (-20 degrees) immobilization on pharmacokinetics of gentamicin in rabbits]

Objective: To observe pharmacokinetic changes under simulated weightlessness in relevant to body flood flow changes. Method: Gentamicin was selected as probe drug in the present study, and rabbits exposed to Head-Down Tilt (HDT, -20 degrees) immobilization were selected as simulated weightlessness animal model. Seven rabbits were treated inf. with 3 mg/kg of gentamicin sulfate pre-HDT and 7 d after HDT. Gentamicin blood samples within 4 h after administration were analyzed by TDxFLx. Result: The distribution of gentamicin postponed significantly: a significant decrease in alpha from (0.1838 +/- 0.1076) min-1 before HDT to (0.0591 +/- 0.0334) min-1 after HDT; a significant increase in t1/2 alpha from (5.30 +/- 3.55) min to (15.04 +/- 7.49) min; a significant decrease in k12 from (0.1025 +/- 0.0721) min-1 to (0.0181 +/- 0.0161) min-1, a increase trend in V(C) and V(D). After HDT, CL(S) of gentamicin increased from (2.2 +/- 0.5) ml min-1 kg-1 to (2.7 +/- 0.3) ml min-1 kg-1. Conclusion: Simulated weightlessness might induce pharmacokinetic changes.