Nakae H, Muranishi S, Asada S, Takada K
J Pharmacobiodyn. 1981 Aug;4(8):584-9. doi: 10.1248/bpb1978.4.584.
Pharmacokinetic analysis of plasma concentration of acetyl procainamide ethobromide (APAEB) after single injection of 1.5, 8.8 and 20 mumol/300 g rat of APAEB showed that its elimination from plasma followed saturation kinetics. The existence of saturable step in transport of APAEB from blood to bile was also evident from the data of the biliary excretion at three dose levels. The data of the biliary excretion were well fitted to two compartment model with two saturable processes at the hepatic uptake and the biliary excretion. The Michaelis-Menten parameters were calculated according to that model. The model was also applicable to the data of biliary excretion obtained by constant infusion of APAEB Simulation of liver and plasma content gave a good agreement to the experimental data. All these results indicate that the pharmacokinetics of APAEB is satisfactorily represented by the proposed model.
单次注射1.5、8.8和20微摩尔/300克大鼠乙酰普鲁卡因胺乙溴化物（APAEB）后，对其血浆浓度进行药代动力学分析表明，它从血浆中的消除遵循饱和动力学。从三个剂量水平的胆汁排泄数据也可明显看出，APAEB从血液到胆汁的转运存在饱和步骤。胆汁排泄数据很好地拟合了具有肝脏摄取和胆汁排泄两个饱和过程的二室模型。根据该模型计算了米氏参数。该模型也适用于通过持续输注APAEB获得的胆汁排泄数据。肝脏和血浆含量的模拟与实验数据吻合良好。所有这些结果表明，所提出的模型能令人满意地反映APAEB的药代动力学。
