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本文报道7例健康青年志愿者口服50mg丙咪嗪的药代动力学参数。丙咪嗪药时曲线符合二室线性动力学。其V/F(c)=1088±157 1;t1/2β=28.6±11.5h;t1/2Ka=0.688±0.280h;CL(s)=70.56±18.90 l/h。主要代谢产物去甲丙咪嗪药时曲线符合一室线性动力学。其t1/2=44.5±33.9h;t1/2Ka=2.01±1.60h;CL(s)=16O±118 l/h。统计学处理表明,去甲丙咪嗪的达峰时间较丙咪嗪显著延迟,其t1/2Ka相应延长,峰浓度亦低于原型药物。本文讨论了代谢产物药代动力学参数的临床意义。
This article reports 7 healthy young volunteers oral administration of 50mg imipramine pharmacokinetic parameters. Imipramine drug curve in line with two-compartment linear kinetics. Its V / F (c) = 1088 ± 157 1; t1 / 2β = 28.6 ± 11.5 h; t1 / 2Ka = 0.688 ± 0.280 h; CL (s) = 70.56 ± 18.90 l / h. The main metabolite of desipramine when the drug curve in line with a linear dynamics chamber. T1 / 2 = 44.5 ± 33.9 h; t1 / 2Ka = 2.01 ± 1.60 h; CL (s) = 16 ± 118 l / h. Statistical analysis showed that the peak time of desipramine was significantly delayed compared with imipramine, the t1 / 2Ka correspondingly extended, the peak concentration is also lower than the prototype drug. This article discusses the clinical significance of metabolite pharmacokinetic parameters.