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按随机交叉实验设计法,对5尺犬口服和静脉注射卡莫氟(10mg/kg)的药代动力学及绝对生物利用度进行了研究,应用反相高效波相色谱法测定血清药物浓度。结果表明静注给药的药时曲线符合二室开放规型,T1/2α=1.67min,T1/2β=34.55min,Vc=0.2525L/kg,C1=0.3205L/kg/h,AuCiv=498.44μg·min/m;口服卡莫氟片的药时曲线符合一室开放模型,T1/2a=12.min,T1/2e=38.51minTmax=28.46min,Cmax=2.09μg/m1,AuCpo=407.90μg.min/m1;由AuCiv和AuCpo算得绝对生物利用度F=82.14％。
Randomized crossover design was used to study the pharmacokinetics and absolute bioavailability of oral and intravenous injection of carmofur (5 mg / kg) to 5-foot dogs. Serum drug concentrations were determined by RP-HPLC. The results showed that the pharmacokinetics curve of intravenous injection conformed to the two-compartment open type with T1 / 2α = 1.67min, T1 / 2β = 34.55min, Vc = 0.2525L / kg, C1 = 0.3205L / kg / h, AuCiv = 498.44 μg · min / m. The pharmacokinetic profile of oral carmofur tablet was in accordance with the one-compartment open model with T1 / 2a = 12.min, T1 / 2e = 38.51minTmax = 28.46min, Cmax = 2.09μg / ml and AuCpo = 407.90μg .min / m1; absolute bioavailability calculated from AuCiv and AuCpo F = 82.14%.