抗癌制剂优福定在比格犬体内的相对生物利用度  

Relative Bioavailability of UFT, an Oral Fluorouracil Antitumor Agent, in Beagle Dogs

作　　者：初大丰[1] 顾景凯[1] 刘万卉[2] 傅学奇[1] 

机构地区：[1]吉林大学生命科学学院药物代谢研究中心,长春130021 [2]烟台大学药学院药物分析教研室,山东省烟台264003

出　　处：《吉林大学学报（理学版）》2005年第2期232-234,共3页Journal of Jilin University:Science Edition

基　　金：国家自然科学基金(批准号:30070879)

摘　　要：采用HPLC法测定Beagle犬单剂量口服含替加氟100mg、尿嘧啶224mg的参比优福定胶囊与受试优福定胶囊后替加氟与其活性代谢产物5氟尿嘧啶的血药浓度,然后进行犬体相对生物利用度与生物等效性研究.结果表明:受试制剂在犬体内替加氟与5氟尿嘧啶的相对生物利用度分别为(106.89±21.74)%与(102.32±24.02)%,两种制剂具有生物等效性.Tegafur [1-(tetrahydro-2-furanyl)-5-fluorouracil](TF), a masked form of 5-fluorouracil (5-FU), is an effective antitumor agent. Oral administration of TF plus uracil (U) (14 mole/mole) (UFT) is more effective than that of TF alone. The relative bioavailability of UFT was studied in beagle dogs. A single oral administration of UFT test capsules or reference capsules containing 100 mg TF and 224 mg U was given to each dog according to a random crossover design. The drug concentrations in plasma were determined by high performance liquid chromatography (HPLC). The relative bioavailabilities of TF and 5-FU were ( 106.89± 21.74)% and ( 102.32± 24.02)%, respectively. The pharmacokinetic parameters, including C_ max, AUC_ 0~t and AUC_ 0~∞, show no significant difference (P> 0.05). Statistical results show that the two preparations are bioequivalent ( P>0.05).

关 键 词：相对生物利用度 优福定 替加氟 5-氟尿嘧啶 

分 类 号：R969.1[医药卫生—药理学]