Kamath B L, Lai C M, Gupta S D, Durrani M J, Yacobi A
J Pharm Sci. 1981 Mar;70(3):299-302. doi: 10.1002/jps.2600700319.
The pharmacokinetics of distribution and elimination of procainamide and its major metabolite, N-actylprocainamide, were studied in rats. Eight rats were selected randomly, and each received intravenously 14C-labeled procainamide hydrochloride (75 mg/kg) or 14C-labeled N-acetylprocainamide hydrochloride (86 mg/kg) according to a two-way crossover design. Serial blood samples were withdrawn for 8 hr, and cumulative urine and feces were collected for 48 hr. The plasma concentration-time relationships of procainamide and N-acetylprocainamide were characterized by one- and two-compartment open models, respectively. A pseudo-three-compartment model was necessary to characterize the time course of N-acetylprocainamide in plasma formed after administration of procainamide. The biological half-lives of procainamide and N-acetylprocainamide averaged 0.66 and 2.1 hr, respectively. The urinary excretion profiles of these drugs and the ratio of their biological half-lives in rats were similar to those in humans.
在大鼠中研究了普鲁卡因胺及其主要代谢产物N - 乙酰普鲁卡因胺的分布和消除的药代动力学。随机选择8只大鼠，根据双向交叉设计，每只大鼠静脉注射14C标记的盐酸普鲁卡因胺（75mg/kg）或14C标记的盐酸N - 乙酰普鲁卡因胺（86mg/kg）。连续8小时采集血样，并收集48小时的累积尿液和粪便。普鲁卡因胺和N - 乙酰普鲁卡因胺的血浆浓度 - 时间关系分别用一室和二室开放模型表征。需要一个伪三室模型来表征给予普鲁卡因胺后血浆中N - 乙酰普鲁卡因胺的时间过程。普鲁卡因胺和N - 乙酰普鲁卡因胺的生物半衰期平均分别为0.66小时和2.1小时。这些药物在大鼠中的尿排泄情况及其生物半衰期之比与人类相似。
