【摘要】 甘磷酰芥口服对所试10种动物肿瘤中的5种有明显抑制作用,对大鼠吉田肉及瘤Walker癌肉瘤256的抑制率高达82～100％;外敷对大鼠Jensen肉瘤及walker256亦有明显抑制作用;对小鼠的LD₅₀ 为口服580±40mg/kg,腹腔注射360±5mg/kg;狗口服20mg/kg为安全量;对HeLa细胞有丝分裂有显著抑制作用;在血中分布8小时达高峰,在正常及肿瘤大鼠组织中的分布均以胃肠、肝、肾中最高,在瘤中也有一定含量,96小时从粪尿的累积排出率为32.54％。更多还原

【Abstract】 Oral glyciphosphoramide showed apparent antitumor action in 5 of 10 animal tumors, among them effects on Yoshida sarcoma and Walker 256 being the highest(82-100%). Jensen sarcoma and Walker 256 were also inhibited by smear ing DMSO solution of the drug. The LD5U for oral and ip glyciphosphormide were 580 ±40 and 360±5mg/kg respectively. The maximum tolerated dose for oral glyciphosphoramide in dogs was 20 mg/kg/d. Apparent inhibition on mitosis of HeLa cells was noticed. Results of physiological disposition showed that 14C-radioactivity in blood reached the peak value 8 hrs after oral administration. The tissue distribution in normal and tumor-bearing rats was similar, the radioactivity being higher in liver, kidney and CI tract and high to a certain extent in tumor tissue. The cumulative excretion of 14C-radioactitviy in urine and feces within 96 hrs. was 32.54%.更多还原