国产卡莫氟在犬体内的药动学及片剂绝对生物利用度研究

按随机交叉实验设计法,用反相高效液相色谱法测定血清药物浓度。对5只犬po和iv卡莫氟(10mg/kg)的药动学及其片剂绝对生物利用度进行了研究。结果表明,静注给药的药时曲线符合二室开放模型,T_(1/2α)=1.67min,T_(1/2β)=34.55min,Vc=0.2525 L/kg,Cl=0.3205 L/kg·h~(-1),AUC_(iv)=1.9375 mmol·min/L;口服卡莫氟片的药时曲线符合一室开放模型,T_(1/2ka)=12.13min,T_(1/2ke)=38.51min,T_(mix)=28.46min,C_(max)=8.1396×10~(-3)mmol/L,AUC_(po)=1.5856 mmol·min/L;由AUC_(iv)和AUC_(po)算得绝对生物利用度F=82.14%。

STUDIES ON THE PHARMACDKINETICS AND ABSOLUTE BIO- AVAILABILITY OF 1-HEXYLCARBAMOYL-5-FLUOROURACIL TABLET IN DOGS

The pharmacokinetics and absolute bioavailability of 1-hexyl-carbamoyl-5-fluorouracil ( HCFU ) (10 mg/kg ) after oral and intravenous administration were studied in 5 dogs with cross-over design. The concentration of HCFU in serum was determined by reversed-phase high performanee liquid chromatography. After intravenous administration, the curve of serum HCFU concentration vs time was fit to a two-compartment opened model and the phar-macokinetic parameters were. T1/2α=1 .67 min, T1/2β = 34.55 min, Vc= 0.2525L/kg,C1 = 0.3205 L/kg·h~-1 & AUCiv =1.9375 mmol/min·L~-1. When HCFU tablets were tiken orally, the curve of concentration vs time was fit to an one-compartment opened model and its pharmacokinetie parameters were: T1/2ke=12.13 min, T1/2ke=38.51 min, Tmax=23.46 min,Cmax=8.140×10~-3mmol/L & AUCpo=1.5856 mmol/min·L~-1 . The absolute bioavailability calculated from AUCpo and AUCiv was 0.8214.