摘要
背景：碘-131-MIBG(131I-meta-iodobenzylguanidine)在臨床上已被公認對於神經元源起之腫瘤及甲狀腺髓質瘤具十分有效的診斷功效，長久以來國內使用之碘-131-MIBG皆仰賴進口。核研所已成功研製碘-131-MIBG，本研究目的在測試核研所製備MIBG之毒性範圍及其在生物體內之分佈情形。 方法：我們分別使用兩種動物(大鼠和鼷鼠)經由兩種途徑(口服及靜脈注射)分別施予MIBG測試LD50。八隻公狗接受靜脈注射0.5mCi碘-131-MIBG之後，測試體內之生生物體分佈。四隻紐西蘭成兔在經過靜脈注射0.2mCi碘-131-MIBG之後進行全身造影。 結果：口服MIBG之LD50，Sprague Dawley大鼠為220mg/kg，鼷鼠為225mg/kg；靜脈注射MIBG之LD50，大鼠為42mg/kg，鼷鼠為34.5mg/kg。生物體分佈研究顯示靜脈注射一小時後，甲狀腺及腎上腺髓質聚積之碘-131-MIBG最多，甲狀腺的活度於48小時後下降，其他器官在24小時後僅剩微小量。碘-131-MIBG在血中清除率甚快。其半量期僅有5.95小時。 結論：碘-131-MIBG在臨床上診斷及治療功效已被肯定，本研究確認MIBG的低毒性，其安全性無庸置疑，核研所產制的碘-131-MIBG在通過衛生署查驗登記之後，對國內患者將有莫大助益。
並列摘要
Background: 131I-MIBG has been developed for imaging pheochomocytoma, medullary thyroid carcinoma, neuroblastoma and a wide range of tumors originated from the neural crest. The Institute of Nuclear Energy Research in Taiwan (INER) has produced 131I-MIBG successfully. This study tested the toxicity and biodistribution of INER-produced MIBG in animals. Methods: LD50 was determined in Sprague Dawley rats and ICR mice via intravenous and oral route. Following intravenous injection of 131I-MIBG, the biodistribution study was performed in 8 dogs, and the whole body gamma images were taken in rabbits. Results: LD50 in rats were 220 mg/kg (oral route) and 42 mg/kg (intravenous route), respectively. LD50 in mice were 225 mg/kg (oral route) and 34.5 mg/kg (intravenous route), respectively. The biodistribution study revealed high uptake of tracer in the thyroid and adrenal gland. There was only trace of radioactivity in the other organs 24 h postinjection. The decline of radioactivity in the thyroid was noted at 48 h. The blood clearance half-life (T 1/2) of 131IMIBG was 5.95 h. Conclusions: MIBG scintigraphy plays a prominent role in diagnosing pheochromocytoma, medullary thyroid carcinoma and neuroblastoma. Since the low toxicity of MIBG was confirmed in this study, the approval of New Drug Application (NDA) for 131I-MIBG produced by INER will be of great benefit to the patients in Taiwan.
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