Takeshita T, Iwasaki M, Narita M, Sou M, Sato M, Hashimoto T, Kameya S, Iigima N
Second Dept. of Surgery, St. Marianna University School of Medicine.
Gan To Kagaku Ryoho. 1988 Nov;15(11):3053-8.
The blood and tissue concentrations of tegafur (TGF), 5-fluorouracil (5-FU) and uracil were tested by administering 6 capsules of UFT (600 mg as tegafur (TGF)) per day to 21 patients awaiting operation for stomach cancer. At the same time, comparative tests were performed by dividing the patients into two groups, giving UFT before meals in one group and in another after meals. Both 5-FU and uracil levels tend to reach to the maximum blood concentration after one hour, while showing similar variations with time lapse. Furthermore, a significantly positive relationship was observed between 5-FU and uracil in the rate of changes of blood concentration during six hours after administration of UFT. The 5-FU concentration within tumor tissue was 10 times higher than that within the blood and 2 times higher than that within normal tissue. A similar tendency was observed with uracil, which was of value in the clinical determination of the effect of uracil in inhibiting decomposition of 5-FU. With regard to the comparative test between the groups of pre- and post-meal UFT administration, the concentration of tegafur (TGF) and 5-FU in tumor tissue tended to be higher in the pre-meal group which indicates a need for further study of the phenomenon.
对21例等待胃癌手术的患者,每日给予6粒优福定胶囊(替加氟600mg),检测替加氟(TGF)、5-氟尿嘧啶(5-FU)和尿嘧啶的血药浓度及组织浓度。同时,将患者分为两组进行对比试验,一组在饭前服用优福定,另一组在饭后服用。5-FU和尿嘧啶血药浓度均在1小时左右达到峰值,且随时间变化趋势相似。此外,服用优福定后6小时内,5-FU与尿嘧啶血药浓度变化率之间呈显著正相关。肿瘤组织内5-FU浓度比血液中高10倍,比正常组织中高2倍。尿嘧啶也呈现类似趋势,这对临床判断尿嘧啶抑制5-FU分解的效果具有参考价值。关于饭前和饭后服用优福定两组的对比试验,饭前组肿瘤组织中替加氟(TGF)和5-FU浓度更高,这一现象有待进一步研究。