Weaver B M, Staddon G E, Mapleson W W
The Veterinary School, University of Bristol, Langford, UK.
Br J Anaesth. 2001 May;86(5):693-703. doi: 10.1093/bja/86.5.693.
The primary objective of this study was to determine in vivo tissue/blood partition coefficients of propofol for use in physiological modelling of its pharmacokinetics. The sheep was used as an animal model. In the main series of experiments, crossbred ewes received a bolus of propofol 1% (Diprivan) followed by an infusion during which blood concentrations were measured at intervals. After 2 h, the sheep were killed with an injection of potassium chloride, and tissue samples were taken for storage at -20 degrees C and subsequent analysis. Tissue/blood partition coefficients depend on the amount of triglyceride which accumulates in blood from the propofol vehicle; for blood, free of added triglyceride, the following coefficients were calculated: brain, 3.23; heart, 5.94; kidney, 2.46; spleen, 1.86; semimembranosus muscle, > or = 1.61; triceps muscle, > or = 1.47. Calculated tissue/water coefficients were 35 times greater. There was indirect evidence of extraction of propofol by the lungs.
本研究的主要目的是确定丙泊酚的体内组织/血液分配系数,以用于其药代动力学的生理建模。选用绵羊作为动物模型。在主要系列实验中,杂种母羊静脉注射一剂1%丙泊酚(得普利麻),随后进行输注,期间定期测量血药浓度。2小时后,注射氯化钾处死绵羊,采集组织样本并储存于-20℃,随后进行分析。组织/血液分配系数取决于丙泊酚载体中积累在血液中的甘油三酯量;对于未添加甘油三酯的血液,计算出以下系数:脑,3.23;心脏,5.94;肾脏,2.46;脾脏,1.86;半膜肌,≥1.61;肱三头肌,≥1.47。计算出的组织/水系数大35倍。有间接证据表明肺对丙泊酚有摄取作用。