Korolev G K
Vopr Onkol. 1975;21(11):50-6.
On rats with sarcoma M-1 the peculiarities of accumulation and elimination of the folic acid antagonist-pyrimido (4,5-b), (1,4) thiazinon-35S, called "thomizine", have been studied. In travenous injection of thomizine-35S with the activity of 5 muc per animal the highest initial concentration of radioactivity was observed 5-15 minutes after the injection. While decreasing, the radioactivity absorption coefficients in organs were distributed as follows: the kidneys, pancreas, organs of the endocrinous system, lymph nodes, the stomach, liver, small intestine, brain. Thomizine-35S accumulation in rat organs proceeded not only on account of its intake with blood but also due to penetration and subsequent deposition in structural tissue elements. Lessening of radioactivity in the organism of rats was dependent exponentially. Elimination of the drug was realized mainly via the kidneys. 89 per cent of the absorbed radioactivity was eliminated from the organism with a period of semielimination of 1 hour, 11 per cent - with a period of semielimination of 36 hours.
对患有肉瘤M-1的大鼠,研究了叶酸拮抗剂嘧啶并(4,5-b),(1,4)噻嗪酮-35S(称为“托米嗪”)的蓄积和消除特性。给每只动物静脉注射活性为5微居里的托米嗪-35S后,在注射后5-15分钟观察到放射性的最高初始浓度。随着浓度降低,各器官中的放射性吸收系数分布如下:肾脏、胰腺、内分泌系统器官、淋巴结、胃、肝脏、小肠、脑。托米嗪-35S在大鼠器官中的蓄积不仅是由于其随血液摄入,还由于其渗透并随后沉积在结构组织成分中。大鼠体内放射性的降低呈指数关系。药物的消除主要通过肾脏实现。89%的吸收放射性在1小时的半消除期内从体内消除,11%在36小时的半消除期内消除。