【摘要】 研究了口服单剂量维拉帕米后,维拉帕米及其主要代谢物在正常中国人体内的处置动力学。采用药物及其代谢物的药动学结合模型描述两者在正常人体内的经时过程。口服给药后,维拉帕来迅速代谢,约3h其代谢物去甲维拉帕米达到血浓度峰值,去甲维拉帕米的C_max为123.1±62.6 ng/ml。维拉帕来和去甲维拉帕米的平均消除半衰期分别为3.70±0.63和6.26±1.69 h,混合参数K_1m V₁/V_m 为0.11±0.06h^-1。更多还原

【Abstract】 The pharmacokinetics of verapamil and its major metabolite following the oral administration of verapamil to ten healthy male volunteers are described. The drug and metabolite （norverapamil）plasma concentration data are fitted to the same pharmacokinetic model with two-compartment （drug） plus one metabolite compartment. After oral administration verapamil was rapidly metabolized to norverapamil. The plasma norverapamil concentration reached its maximum at about 3. 0 h and the mean C_max for norverapamil was 123.1±62. 6ng·ml^-1. The mean terminal elimination half- lives for verapamil and norverapamil were 3.70±0.63 and 6.26±1.69 h respectively. The value of hybrid parameter K_1mV₁V_m^-1 was 0.11±0. 06 h^-1.更多还原