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目的:研究硫喷妥钠在离体兔心肌的摄取动力学过程。方法:以三种浓度硫喷妥钠(500μmol、1500μmol、500μmol)持续灌注兔心肌共15分钟,应用高效液相色谱法测定心肌灌出液内硫喷妥钠浓度,用左室压力最大上升速率(LV+dp/dt_(max))作为效应指标。结果:硫喷妥钠在心肌内摄取分布符合二室开放模型,它能较快分布于心肌组织(T_(1/2α)=0.5±0.1分钟),但从心肌清除较慢(T_(1/2β)=25.3±10.1分钟)。药物自中央室向周边室的转运速率快于自周边室向中央室的转运。对LV-bdp/dt_(max)的最大理论抑制效应(Emax)为19.0+11.2kPa·s~(-1)。结论:离体免心肌对硫喷妥钠的摄取过程符合二室开放模型,其特点为快速分布而清除较慢。
Objective: To study the uptake kinetics of thiopental in isolated rabbit myocardium. Methods: Myocardium was perfused continuously with three concentrations of thiopental sodium (500μmol, 1500μmol, 500μmol) for 15 minutes. The concentration of thiopental in myocardial perfusate was measured by high performance liquid chromatography (HPLC) (LV + dp / dt_ (max)) as an effect index. Results: The distribution of thiopental in myocardium was in accordance with the two - compartment open model, which could be quickly distributed in myocardial tissue (T 1 / 2α = 0.5 ± 0.1 minutes) 2β) = 25.3 ± 10.1 minutes). The rate of drug delivery from the central chamber to the peripheral chamber was faster than the transport from the peripheral chamber to the central chamber. The maximum theoretical inhibitory effect (Emax) on LV-bdp / dt max was 19.0 + 11.2 kPa · s -1. CONCLUSION: In vitro release of thiopental from isolated myocardium conforms to a two-compartment open model characterized by rapid distribution and slower clearance.