Fernández J, Lligoña L, Puigdemont A, Guitart R, Riu J L, Arboix M
Department of Pharmacology, Veterinary Faculty, Universitat Autònoma de Barcelona, Spain.
Eur J Drug Metab Pharmacokinet. 1991 Jan-Mar;16(1):23-7. doi: 10.1007/BF03189870.
Tissue distribution of propafenone has been studied in the rat. Measurement of propafenone was made in several tissues: plasma, heart, kidney, lung, liver, muscle, fat and brain, after i.v. administration of 2 mg/kg of the drug. The plasma propafenone kinetics profile can be described by a two-compartmental model. The pharmacokinetic parameters, derived from plasma levels, showed a t1/2 beta of 55.4 min, the central Vd/kg of 2.4 ml/kg, the Cl of 62.8 ml/min.kg and the AUC0-oo of 31.6 micrograms.min/ml. The analysis of the propafenone tissue distribution showed the highest concentration of drug in the lung, followed by the heart and kidneys. A significant concentration was found in brain, muscle and adipose tissue, with concentration ratios (tissue/plasma) above 1. The half-life values obtained for individual organs and tissues are similar to those obtained in plasma, around 1 h. In the post-distributive phase, plasma and tissue concentrations decline in parallel.
已在大鼠中研究了普罗帕酮的组织分布。静脉注射2mg/kg药物后，在几个组织中测定了普罗帕酮：血浆、心脏、肾脏、肺、肝脏、肌肉、脂肪和脑。血浆普罗帕酮动力学曲线可用二室模型描述。从血浆水平得出的药代动力学参数显示，β半衰期为55.4分钟，中央分布容积为2.4ml/kg，清除率为62.8ml/min.kg，AUC0-∞为31.6μg.min/ml。普罗帕酮组织分布分析显示，肺中药物浓度最高，其次是心脏和肾脏。在脑、肌肉和脂肪组织中发现有显著浓度，浓度比（组织/血浆）大于1。各个器官和组织获得的半衰期值与血浆中获得的值相似，约为1小时。在分布后阶段，血浆和组织浓度平行下降。
