抗癌制剂优福定在比格犬体内的相对生物利用度

采用HPLC法测定Beagle犬单剂量口服含替加氟100 mg、 尿嘧啶224 mg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.

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

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).