Yamamoto Y, Amano T, Imada T, Tamura S, Abe M, Matsumoto A
1st Dept of Surgery, Yokohama City Univ. School of Med.
Gan No Rinsho. 1988 May;34(6):749-54.
An experiment to gauge the effect of OK-432 on UFT activation under a combined administration of UFT and OK-432 at a therapeutic dose has been pursued clinically by determining the blood and intratumoral 5-FU concentrations after administration of UFT. UFT was administered orally to a group of AH-130-bearing rats at a dose of 12 mg/kg or 8 mg/kg. In another group that was given combined treatment with OK-432, the OK-432 was administered subcutaneously at a dose of 0.1 KE/kg together with UFT. The intratumoral 5-FU concentration at 4 hours after UFT 12 mg/kg administration showed higher values in th single UFT treated group than in the combined treated group, but at 8 hours no significant difference was found between these two groups as the concentrations were 0.133 +/- 0.027 microgram/g and 0.128 +/- 0.021 microgram/g, respectively. Further, no significant differences were noticed in the blood and intratumoral 5-FU concentrations between both groups after administration of UFT at a dose of 8 mg/kg. Clinically, the blood FT-207 and 5-FU concentrations after UFT administration showed no significant difference between the single UFT treated group and the combined OK-432 treated group, nor was there a significant difference in the intratumoral concentration. In summary, it is considered that OK-432 has little effect on UFT activation when UFT and OK-432 are administered in combination.
通过测定服用优福定(UFT)后血液和肿瘤内5-氟尿嘧啶(5-FU)的浓度,临床上开展了一项实验,以评估在治疗剂量下联合使用优福定和沙培林(OK-432)时OK-432对优福定激活的影响。给一组荷AH-130大鼠口服优福定,剂量为12mg/kg或8mg/kg。在另一组接受OK-432联合治疗的大鼠中,将OK-432以0.1KE/kg的剂量与优福定一起皮下注射。服用12mg/kg优福定后4小时,单药优福定治疗组的肿瘤内5-FU浓度高于联合治疗组,但在8小时时,两组之间未发现显著差异,浓度分别为0.133±0.027微克/克和0.128±0.021微克/克。此外,给大鼠服用8mg/kg优福定后,两组之间的血液和肿瘤内5-FU浓度均未发现显著差异。临床上,服用优福定后,单药优福定治疗组和OK-432联合治疗组的血液中FT-207和5-FU浓度均无显著差异,肿瘤内浓度也无显著差异。总之,当联合使用优福定和OK-432时,认为OK-432对优福定的激活几乎没有影响。