论文部分内容阅读
近几年我国利用血卟啉并结合激光照射来诊断和治疗恶性肿瘤,得到良好的效果。为了用血卟啉衍生物进行体内药代动力学及其它医学示踪研究,用暗室放电曝射和催化放电曝射法分别对北京试制的血卟啉衍生物HPD、HPS和美国Sigma公司的HPD进行了氚标记。催化剂用与标记品同量的三氯化铑。氚标记的粗样品须用薄板层析法纯化和分离。~3H-HPD(HPS)的比活度提高了0.5—1.0倍。暗室放电曝射~3H-HPS的比活度为222MBq/mg,~3H-MPD为62.9MBq/mg;催化放电曝射~3H-HPS的比活度为337MBq/mg,~3H-HPD为130MBq/mg。标记和未标记样品,经紫外和红外吸收光谱测定,其光谱图基本一致。经高压液相色谱:色谱柱YWG-C_(18),溶剂为甲醇:水(pH=2.5)=9:1(V/V),流速2.0ml/min,以及硅胶G薄板层析,推进剂为苯:甲醇=3:2(V/V),观察到HPD和HPS仍存有少量血卟啉单乙烯基异构体和羟基乙酸酯等。
In recent years, China’s use of hematoporphyrin combined with laser irradiation to diagnose and treat malignant tumors, get good results. In order to use hematoporphyrin derivatives for in vivo pharmacokinetics and other medical tracing studies, the effects of hematoporphyrin derivatives HPD, HPS and HPD Tritium labeling was performed. Catalysts with the same amount of labeled rhodium trichloride. Tritiated crude samples should be purified and separated by thin layer chromatography. ~ 3H-HPD (HPS) specific activity increased 0.5-1.0 times. The specific activity of ~ 3H-HPS in darkroom was 222MBq / mg and ~ 3H-MPD was 62.9MBq / mg. The specific activity of ~ 3H-HPS was 337MBq / mg and ~ 3H-HPD was 130MBq / mg. Labeled and unlabeled samples, measured by UV and IR absorption spectroscopy, the spectra are basically the same. The high pressure liquid chromatography column YWG-C 18 with methanol: water (pH = 2.5) = 9: 1 (V / V) and flow rate 2.0ml / Benzene: methanol = 3: 2 (V / V), HPD and HPS observed a small amount of hematoporphyrin monovinyl isomers and hydroxy acetate and so on.