STUDIES ON THE PHARMACDKINETICS AND ABSOLUTE BIO- AVAILABILITY OF 1-HEXYLCARBAMOYL-5-FLUOROURACIL TABLET IN DOGS / 中国药理学通报

ABSTRACT

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. T1/2?=1 .67 min, T1/2? = 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.