Hou D Y, Hoch H, Johnston G S, Tsou K C, Farkas R J, Miller E E
Eur J Nucl Med. 1983;8(12):535-40. doi: 10.1007/BF00251616.
111Indium-bleomycin (111In-BLM) and 57Co-bleomycin (57Co-BLM) were prepared and their distributions were compared in the tissues, blood, and urine in tumor-bearing and in untreated mice and rats. Autoradiographs of electrophoresis gels showed that patterns for urine from untreated and tumor-bearing animals, collected 1-3 h or 48 h after injection of 111In-BLM were similar to those for in vitro mixtures of urine and 111In-BLM, but differed from the patterns obtained with 111InCl3 under in vivo or in vitro conditions. In rats bearing mammary adenocarcinoma, 48 h after administration of the radiopharmaceutical, the activity ratio of tumor to eleven different tissues was 1.2-4.6 times higher for injected 111In-BLM than for 111InCl3 (P less than or equal to 0.001 or P less than or equal to 0.05). Imaging with a gamma camera depicted tumors in mice more distinctly with 111In-BLM than with 111InCl3. These findings were interpreted as reflecting the stability of 111In-BLM in vivo. The tumor concentration (%dose/g) was higher for the viable area than for the necrotic area for 111In-BLM, but the reverse was true for 57Co-BLM.
制备了铟 - 111博来霉素(¹¹¹In - BLM)和钴 - 57博来霉素(⁵⁷Co - BLM),并比较了它们在荷瘤小鼠和大鼠以及未处理小鼠和大鼠的组织、血液和尿液中的分布情况。电泳凝胶放射自显影片显示,在注射¹¹¹In - BLM后1 - 3小时或48小时收集的未处理动物和荷瘤动物尿液的图谱,与尿液和¹¹¹In - BLM的体外混合物的图谱相似,但与在体内或体外条件下用¹¹¹InCl₃获得的图谱不同。在患有乳腺腺癌的大鼠中,给予放射性药物48小时后,注射的¹¹¹In - BLM的肿瘤与11种不同组织的活性比,比¹¹¹InCl₃高1.2 - 4.6倍(P≤0.001或P≤0.05)。用γ相机成像显示,¹¹¹In - BLM比¹¹¹InCl₃更能清晰地描绘小鼠体内的肿瘤。这些发现被解释为反映了¹¹¹In - BLM在体内的稳定性。¹¹¹In - BLM的存活区域肿瘤浓度(%剂量/克)高于坏死区域,但⁵⁷Co - BLM则相反。