异丙酚在容量控制性失血性休克猪体内的药动学研究

Pharmacokinetics of Propofol in Pigs with Hemorrhagic Shock Under Volume Controlled

目的探讨异丙酚在容量控制性失血性休克猪体内药动学的特点。方法健康巴马小型猪12头,应用随机数字表法将其随机分为对照组和休克组。采用HPLC-荧光法测定猪静脉泵入异丙酚后不同时间点的血药浓度。根据测定的血药浓度计算异丙酚的消除半衰期(t1/2),血浆-效应室平衡速率常数(Ke0),药时曲线面积(AUC)以及平均驻留时间(MRT)等药动学参数。结果休克组异丙酚的血药浓度高于对照组,差异有显著性(P<0.05)。休克组最大药物浓度(Cmax)高于对照组,差异有显著性(P<0.05)。休克组t1/2较对照组延长,差异有显著性(P<0.05)。休克组MRT较对照组延长,差异有显著性(P<0.05)。休克组的Ke0、AUC较对照组增大,差异无统计学意义。结论容量控制性失血性休克猪异丙酚的药动学特点是代谢减慢:药物的消除半衰期延长,血浆-效应室平衡速率常数增大,体内的平均驻留时间延长。

OBJECTIVE To investigate the characteristics of pharmacokinetics of propofol in pigs with hemorrhagic shock under volume controlled. METHODS Twelve bama mini pigs were randomly divided into control group, hemorrhagic shock group. The plasma concentration of propofol in pigs was analyzed by HPLC- fluorescence at different time points after the start of the infusion propofol. According to the plasma concentration of propofol to calculate the elimination half-life（t1/2） of propofol, the plasma-effect site equilibration rate content（Ke0）, the drug＇s area under the curve（AUC）, the mean residence time（MRT） and the other pharmacokinetic parameters. RESULTS Plasma concentration of propofol in hemorrhagic shock group was higher than control group significantly（P〈0.05）. Maximum drug concentration（Cmax） in hemorrhagic shock group was higher than control group significantly（P〈0.05）. The t1/2 in hemorrhagic shock group was longer than control group significantly（P〈0.05）. The MRT in hemorrhagic shock group was longer than control group significantly（P〈0.05）. The Ke0 and AUC of hemorrhagic shock group was higher than that of control group, there was not significant difference between groups. CONCLUSION The characteristic of pharmacokinetics of propofol in pigs with hemorrhagic shock under volume controlled was that metabolism delayed, elimination half-life was longer, so dose the mean residence time, the plasma-effect site equilibration rate content was diminished.