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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

STUDIES ON THE PHARMACDKINETICS AND ABSOLUTE BIO- AVAILABILITY OF 1-HEXYLCARBAMOYL-5-FLUOROURACIL TABLET IN DOGS
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摘要 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%。 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.
出处 《中国药理学通报》 CAS CSCD 北大核心 1992年第1期49-52,共4页 Chinese Pharmacological Bulletin
关键词 卡莫氟 药代动力学 高效液相色谱 1-Hexylcarbamoyl-5-fluorouracil Absolute bioavai-lability PharmacokineticS Reversed-phase high performance liquid chromatography
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参考文献1

  • 1M. Iigo,A. Hoshi,A. Nakamura,K. Kuretani. Antitumor activity of 1-alkylcarbamoyl derivatives of 5-fluorouracil in a variety of mouse tumors[J] 1978,Cancer Chemotherapy and Pharmacology(4):203~208

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