论文部分内容阅读
本文报告用分光光度计,采用三波长法在生物样品(血、尿、组织、胆汁及粪等)中测定N-甲酰溶肉瘤素(简称 N-甲)的方法;并用此法观察了 N-甲在动物及人体内的吸收、分布及排泄。本法特异性高,灵敏度为0.10 O.D.相当于样品中含 N-甲11.5微克。大鼠口服 N-甲200毫克/公斤后5小时,由胃肠道内容物可回收剂量的7.9%,而在所排出的粪中并无可测定的药物存在。体外实验证明 N-甲在胃肠道内容物的代谢很快。可见,药物由胃肠道消失的速度并不能反映其自胃肠道吸收的情况。静脉注射后,N-甲在大鼠及家兔的血中消失很快。其在血中的生物半衰期大鼠为12分钟,家兔为15分钟。给正常或肿瘤大鼠静脉注射 N-甲100毫克/公斤后1小时,药物含量以肾脏最高,肝次之,脾、肺、心等组织仅含痕迹量。肿瘤组织的药物含量亦很低。大鼠静脉注射 N-甲100毫克/公斤后5小时,由尿可回收剂量的23.8%,其中96.3%为前两小时所排出。由胆汁亦可回收剂量的12.4%。家兔静脉注射 N-甲50毫克/公斤后,12小时内可自尿排出剂量的12.5%,其中92.6%为前两小时所排出。成年男性肿瘤患者一次口服 N-甲300毫克后5小时内,血中的药物浓度很低,但给药后12小时内可自尿排出剂量的7.1%,其中82.6%为前两小时所排出。用纸层离法证明,大鼠及肿瘤病人口服 N-甲后尿中的代谢物主要为羟基水解产物
This article reports the method for the determination of N-formylcystein (referred to as N-formyl) in biological samples (blood, urine, tissue, bile and feces) using a spectrophotometer and a three- - A in animal and human body absorption, distribution and excretion. This method is highly specific and has a sensitivity of 0.10 O.D. This corresponds to a sample containing N-A 11.5 μg. Five hours after oral administration of N-methyl 200 mg / kg, 7.9% of the dose was recovered from the gastrointestinal tract contents and no measurable drug was present in the excreted feces. In vitro experiments show that N-methyl metabolites in the gastrointestinal tract quickly. Visible, the rate of disappearance of drugs from the gastrointestinal tract does not reflect its absorption from the gastrointestinal tract. After intravenous injection, N-A disappeared quickly in the blood of rats and rabbits. Its biological half-life in blood is 12 minutes for rats and 15 minutes for rabbits. One hour after intravenous injection of N-methyl 100 mg / kg into normal or tumor rats, the drug content was the highest in kidney, followed by liver, spleen, lung, heart and other tissues. Tumor tissue drug content is also very low. Five hours after intravenous injection of N-methyl 100 mg / kg, 23.8% of the recoverable dose from the urine was excreted in 96.3% of the first two hours. Bile can also be recovered from the dose of 12.4%. Intravenous injection of N-methyl 50 mg / kg, 12 hours can be discharged from the urine 12.5%, of which 92.6% of the first two hours of discharge. Within 5 hours after oral administration of N-methyl 300 mg, the concentration of the drug in the blood of the adult male cancer patient is very low, but 7.1% of the urine can be discharged from the urine within 12 hours after administration, of which 82.6% is discharged in the first two hours. Paper layer separation method to prove that rats and tumor patients after oral administration of N- metabolites in the urine mainly hydroxyl hydrolyzate