全麻下儿童丙泊酚的药代动力学特征

Pharmacokinetics of propofol in children under gentral anesthesia

目的研究全麻下儿童丙泊酚的药代动力学特征。方法选择拟在全麻下行择期手术的患儿19例,ASAⅠ或Ⅱ级。丙泊酚3mg/kg在上肢静脉约30s左右注射完毕,注药后1、2、4、6、10、15、30、60、90、150、210、300、420min从右颈内静脉抽取1.5ml全血。血浆药物浓度的测定方法采用反相高效液相色谱技术,应用3p87软件包拟合总的药代动力学参数。结果最终药代动力学参数:清除速率常数(k10)0.1616/min,1室向2室转运速率常数(k12)0.0640/min,2室向1室转运速率常数(k21)0.0062/min,分布半衰期(T1/2α)4.1176min,清除半衰期(T1/2β)123.9559min,清除率(CL)0.0745L.min-1·kg-1,中央室分布容积(Vc)0.9505L/kg,表观分布容积(Vd)27.4100L/kg。未发现体重等变量和各个药代动力学参数间有线性方程可建立。结论丙泊酚在儿童的药代学模型呈二室模型,符合线性药代动力学特点。儿童丙泊酚的药代动力学特征明显不同于成人。

Objective To reveal the pharmacokinetics of propofol in children. Methods Ninteen ASA physical status Ⅰ or Ⅱ children of undergoing general anesthesia were given intravenously. Propofol 3 mg/kg as a bolus over approximately 30 seconds via the upper limb vein. Venous samples （1.5 ml） were abtained at 1,2,4,6,10,15,30,60,90,150,210,300,420 min after injection of propofol. RP-HPLC with fluorescence detector was used and the propofol concentration data were analyzed with 3p87 software. Results The pharmacokinetic parameters for the final model were k10 0. 1616/ min,k12 0. 0640/min, k21 0. 0062/min, T1/2α 4. 1176 min, T1/2β 123. 9559 min, CL 0. 0745 ml/min, Vc 0. 9505 L/kg,Vd 27. 4100 L/kg. The study did not find any linear regression relationship between parameters and body covariates（age, weight, height, body square area）. Conclusion It reveals that the propofol has linear pharmokinetics in children. The pharmokinetics of propofol can be well described by a two-compartment model in children, which is different from adults.