抗癌制剂优福定在比格犬体内的相对生物利用度

抗癌制剂优福定在比格犬体内的相对生物利用度

初大丰^{1, 2}，顾景凯¹，刘万卉²，傅学奇¹

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

收稿日期:2004-07-13 修回日期:1900-01-01 出版日期:2005-03-26 发布日期:2005-03-26
通讯作者: 顾景凯

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

CHU Da-feng^1,2, GU Jing-kai¹, LIU Wan-hui², FU Xue-qi¹

1. Research Center for Drug Metabolism, College of Life Science, Jilin University, Changchun 130023, China; 2. Department of Pharmaceutical Analysis, School of Pharmacy, Yantai University, Yantai 264003, Shandong Province, China

Received:2004-07-13 Revised:1900-01-01 Online:2005-03-26 Published:2005-03-26
Contact: GU Jing-kai

摘要/Abstract

摘要： 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.

关键词: 相对生物利用度, 优福定, 替加氟, 5-氟尿嘧啶

Abstract: 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).

Key words: relative bioavailability, tegafur, 5-fluorouracil

中图分类号:

R969.1

初大丰，顾景凯，刘万卉，傅学奇. 抗癌制剂优福定在比格犬体内的相对生物利用度[J]. J4, 2005, 43(02): 232-234.

CHU Da-feng, GU Jing-kai, LIU Wan-hui, FU Xue-qi. Relative Bioavailability of UFT, an Oral Fluorouracil Antitumor Agent, in Beagle Dogs[J]. J4, 2005, 43(02): 232-234.

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