Shyr M H, Tsai T H, Tan P P, Chen C F, Chan S H
Department of Anaesthesia, Chang Gung Memorial Hospital, Taipei, Taiwan, Republic of China.
Neurosci Lett. 1995 Jan 30;184(3):212-5. doi: 10.1016/0304-3940(94)11209-2.
We evaluated the pharmacokinetics and regional distribution of propofol in the brain and spinal cord during propofol anesthesia in Sprague-Dawley rats, using high-performance liquid chromatographic determination of propofol concentration in brain, whole blood and plasma. We found that the concentration of propofol in the brain increased and decreased expeditiously during and after a 15-min and 30-min period of i.v. infusion of an anesthetic dose (60 mg/kg per h) of propofol. Furthermore, propofol was evenly distributed in the brain and spinal cord during infusion, with a significant inter-individual variation. Upon the establishment of anesthesia 15 and 30 min following intravenous infusion of propofol, the concentration of propofol in the brain, whole blood and plasma was respectively 15.7 +/- 1.9 and 39.4 +/- 2.7 micrograms/g, 4.5 +/- 1.2 and 13.6 +/- 1.3 micrograms/ml and 1.8 +/- 0.5 and 5.1 +/- 0.9 micrograms/ml (mean +/- SEM, n = 6 or 7). These high brain/blood and brain/plasma ratios during anesthesia suggest that propofol manifests a pharmacokinetic profile that is different from at least thiopental.
我们使用高效液相色谱法测定大脑、全血和血浆中丙泊酚的浓度,评估了丙泊酚在Sprague-Dawley大鼠丙泊酚麻醉期间在大脑和脊髓中的药代动力学及区域分布。我们发现,在静脉输注麻醉剂量(60毫克/千克每小时)的丙泊酚15分钟和30分钟期间及之后,大脑中丙泊酚的浓度迅速上升和下降。此外,输注期间丙泊酚在大脑和脊髓中分布均匀,但个体间存在显著差异。在静脉输注丙泊酚后15分钟和30分钟建立麻醉时,大脑、全血和血浆中丙泊酚的浓度分别为15.7±1.9和39.4±2.7微克/克、4.5±1.2和13.6±1.3微克/毫升以及1.8±0.5和5.1±0.9微克/毫升(平均值±标准误,n = 6或7)。麻醉期间这些高的脑/血和脑/血浆比值表明,丙泊酚表现出至少与硫喷妥钠不同的药代动力学特征。