甲氧氯普胺在家兔体内的药物动力学

Pharmacokinetics of Metoclopramide in Rabbits

研究甲氧氯普胺在家兔体内的药物动力学过程。按5mg/kg的剂量给家兔静脉注射给药,用紫外分光光度法研究甲氧氯普胺注射液在家兔体内的血药质量浓度。结果表明,甲氧氯普胺在家兔体内的药物动力学符合开放性二室模型。其最佳药-时曲线方程为ρ=1 048.38e-5.737 9t+48.0e-0.301 6t;分布相半衰期(t1/2α)为(0.120 9±0.003 1)h,消除相半衰期(t1/2β)为(3.320 8±0.256 9)h,药-时曲线下面积(AUC)为(6.144 1±0.539 8)mg/(L.h),体清除率(CLB)为(1.454 2±0.145 9)L/(kg.h),表观分布容积(Vd)值为(1.945 2±0.337 1)L/kg。结果显示,甲氧氯普胺在家兔体内分布快、分布广、代谢较快。

Pharmacokinetic parameters of metoclopramide（MCP） in 6 rabbits were calculated.Rabbits were treated with a dose of MCP（5 mg/kg） intravenously.The concentrations of MCP in serum were determined by ultraviolet spectrophotometry.The result showed that the two-compartment open model adequately describes whole blood MCP disposition and the best concentration-time equation is ρ=1 048.38e-5.737 9t＋48.0e-0.301 6t.The primary pharmacokinetic parameters of MCP are： alum half life time（t1/2α） was（0.120 9±0.003 1） h,elimination half time（t1/2β） was（3.320 8±0.256 9） h,area under the curve（AUC） was（6.144 1±0.539 8） mg/（L·h）,body clearance rate（CLB） was（1.454 2±0.145 9） L/（kg·h）,apparent volume of distribution（Vd） was（1.945 2±0.337 1） L/kg.It is indicated that the distribution of metoclopramide in vivo is rapid and abroad,and the elimination of metoclopramide in vivo is rapid.