美托洛尔剂量对其在体外大鼠离体灌注肝脏中消除的影响。
Effect of dose of metoprolol on its elimination by isolated perfused rat liver in vitro.
作者信息
Shen G S, Zhang Y D, Li M Y, Shen J P, Ding Y, Huang D K
机构信息
Department of Pharmacology, Nanjing Medical College, China.
出版信息
Zhongguo Yao Li Xue Bao. 1993 Nov;14(6):539-42.
The effects of dose of metoprolol (Met) on hepatic elimination was studied in isolated rat liver perfused at a flow of 25 ml.min-1. The results showed that Met was eliminated by rat liver in accordance with one-compartment model. Linear kinetic eliminating processes (apparent first-order kinetics) were found in doses of Met 0.2, 0.5, 1.0, and 2.0 mg, T1/2 were 8.3, 8.8, 9.6, and 10.6 min and the clearance rate were 11.7, 11.8, 9.6, and 8.6 ml.min-1, respectively. Nonlinear eliminating processes were found in doses of Met 4, 8, and 12 mg. Vm and Km were 0.98, 1.05, and 0.94 microgram/min-1.ml-1 and 15.6, 16.9, and 14.6 micrograms.ml-1, respectively. It is concluded that hepatic Met elimination is independent on lower doses, but rested upon high doses.
在流速为25 ml·min⁻¹的离体大鼠肝脏灌注模型中研究了美托洛尔（Met）剂量对肝脏清除率的影响。结果表明，大鼠肝脏对美托洛尔的清除符合一室模型。在美托洛尔剂量为0.2、0.5、1.0和2.0 mg时发现线性动力学消除过程（表观一级动力学），半衰期分别为8.3、8.8、9.6和10.6分钟，清除率分别为11.7、11.8、9.6和8.6 ml·min⁻¹。在美托洛尔剂量为4、8和12 mg时发现非线性消除过程。最大消除速率（Vm）和米氏常数（Km）分别为0.98、1.05和0.94 μg/min⁻¹·ml⁻¹以及15.6、16.9和14.6 μg/ml⁻¹。结论是，肝脏对美托洛尔的清除在低剂量时是独立的，但在高剂量时则依赖于此。
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