de Ruiter G, Popescu D T, de Boer A G, Smeekens J B, Breimer D D
Arch Int Pharmacodyn Ther. 1981 Feb;249(2):180-8.
Eight adult surgical patients received a single i.v. injection of etomidate-base (mean 0.22 mg.kg(-1)). Venous blood samples were drawn at frequent intervals for up to 10 hr following drug administration. Plasma concentrations of etomidate were measured with a newly developed capillary gas chromatographic method. Plasma concentrations fitted best to an open three compartment pharmacokinetic model by a non-linear regression computer programme. The following mean parameters were computed: distribution half-life 2.8 + or - 2.3 min, half-life of the alpha-phase: 22.3 +or - 10.4 min and half-life of the beta-phase 208.8 + or - 64.9 min, distribution volume 3.68 + or - 0.66 l.kg(-1) (Vd area) and 2.16 l.kg(-1) (Vdss) and plasma clearance 879 + or - 135 ml.min(-1). High tissue uptake is indicated by the rapidity and the large volume of distribution. Etomidate is rapidly redistributed from the central to peripheral compartments and rapidly eliminated by metabolism.
八名成年外科手术患者接受了单次静脉注射依托咪酯碱(平均剂量为0.22毫克/千克)。给药后长达10小时内,频繁采集静脉血样。采用新开发的毛细管气相色谱法测定血浆中依托咪酯的浓度。通过非线性回归计算机程序,血浆浓度最适合开放式三室药代动力学模型。计算出以下平均参数:分布半衰期2.8±2.3分钟,α相半衰期:22.3±10.4分钟,β相半衰期208.8±64.9分钟,分布容积3.68±0.66升/千克(Vd面积)和2.16升/千克(Vdss),血浆清除率879±135毫升/分钟。快速性和大分布容积表明组织摄取较高。依托咪酯从中央室迅速重新分布到外周室,并通过代谢迅速消除。