Piovan D, Padrini R, Furlanut M, Moretto R, Ferrari M
Pharmacol Res Commun. 1986 Aug;18(8):739-45. doi: 10.1016/0031-6989(86)90115-3.
The time-courses of flecainide plasma and tissue levels were studied in Wistar male rats after i.v. administration (4 mg/Kg). Drug assay in plasma and tissue was performed with a specific and accurate HPLC technique. The final half lives in plasma and tissues were about 4 hours, except in the brain where the half life value was 9.8 hours. The mean tissue/plasma (T/P) ratios in myocardial, kidney, liver, skeletal and muscle tissues were 9.11, 13.8, 14.37, 6.31 respectively, while in the brain the T/P ratio rose progressively over the sampling time to 10.0. These data suggest that flecainide may accumulate in the central nervous system during prolonged treatment. Flecainide levels in adipose tissue were very low. Finally, there was an early "bulge" in the concentration curve, possibly reflecting enterohepatic circulation or non-linear elimination kinetics.
在静脉注射(4毫克/千克)后,对雄性Wistar大鼠进行了氟卡尼血浆和组织水平的时间进程研究。采用特异且准确的高效液相色谱技术对血浆和组织中的药物进行测定。血浆和组织中的最终半衰期约为4小时,但在大脑中半衰期值为9.8小时。心肌、肾脏、肝脏、骨骼肌组织中的平均组织/血浆(T/P)比值分别为9.11、13.8、14.37、6.31,而在大脑中,T/P比值在采样期间逐渐上升至10.0。这些数据表明,在长期治疗期间,氟卡尼可能会在中枢神经系统中蓄积。脂肪组织中的氟卡尼水平非常低。最后,浓度曲线出现早期“凸起”,可能反映了肠肝循环或非线性消除动力学。