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大鼠口服C~(14)标記的N-甲酰溶肉瘤素(簡称N-甲C~(14))后,C~(14)很快进入血液,口服后1小时血C~(14)濃度达最高,此后緩慢下降。C~(14)在腎脏含量最高,肝、脾、肺、血等次之, 肉瘤含量并不比血中者高,心、肌肉、脑及睾丸含量很低。C~(14)在正常动物組織的分布形式与接种吉田肉瘤大鼠或梭形細胞肉瘤B_(22)小鼠者很相似。給药后不同时間(5小时或24小时)处死的动物彼此間,或不同途徑(口服、腹腔或靜脉注射)給药的动物彼此間,在相应粗織內,除C~(14)含量稍不同外,分布形式基本相同。正常大鼠靜脉注射N-甲C~(14)后3分钟,或吉田肉瘤大鼠腹腔注射后5小时,血浆的放射活性約为血球的5.6—6.8倍。将N-甲C~(14)在体外加入新鮮大鼠全血后,血浆与血球放射活性之比亦在此范圍內。 N-甲C~(14)腹腔注射(正常大鼠、肿瘤大员或小鼠)或靜脉注射(正常大鼠)后,C~(14)主要自尿排出,給药后5小时內,自尿排出的放射性为剂量的41.8—54.3％,主要是前2小时排出的。腹腔注射后24小时內,自粪排出者不超过剂量的6％。但給药后5小时却可自胃腸道内回收剂量的20.6％,其中几乎全由胆管而来。口服N-甲C~(14)后5小时及24小时,分別自尿排出剂量的7.2％及17.4％,自粪排出3.8％及38.9％,自胃腸道內容物却回收了剂量的80.4％及11.0％。无論口服或注射后,24小时內呼出的放射性不超过剂量的9％。
After oral administration of C ~ (14) labeled N-formylcysarginin (abbreviated as N-methyl C ~ (14)), C ~ (14) 14) The highest concentration, then slowly decline. C ~ (14) in the highest kidney content, liver, spleen, lung, blood and other times, sarcoma content is not higher than the blood, heart, muscle, brain and testis content is very low. The distribution pattern of C ~ (14) in normal animal tissues was similar to that of Yoshida sarcoma or B? (22) spindle cell sarcoma. The animals administered at different times (5 hours or 24 hours) after administration, among animals administered with each other or by different routes (oral, intraperitoneal or intravenous injection), in addition to the content of C ~ (14) Slightly different, the distribution of the same form. Normal rats intravenous injection of N-C ~ (14) 3 minutes, or Yoshida sarcoma 5 hours after intraperitoneal injection, the plasma radioactivity of about 5.6-6.8 times the blood cells. The N-methyl C ~ (14) added fresh rat whole blood in vitro, plasma and blood cell radioactivity ratio within this range. After intraperitoneal injection of N-methyl-C ~ (14) into normal rats, tumor chiefly or mice or intravenous injection (normal rats), C14 mainly excreted from the urine. Within 5 hours after administration, Urinary radioactivity was 41.8-54.3% of the dose, mainly excreted in the first two hours. Within 24 hours after intraperitoneal injection, self-excretion does not exceed 6% of the dose. However, 5 hours after administration, 20.6% of the dose can be recovered from the gastrointestinal tract, almost entirely from the bile duct. At 5 and 24 hours after oral administration of N-methyl-C (14), 7.2% and 17.4% of the urine excretion and 3.8% and 38.9% of the self-excretion were discharged respectively from the gastrointestinal tract and 80.4% 11.0%. The radioactivity exhaled within 24 hours after oral or injection does not exceed 9% of the dose.