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目的 比较大鼠硬膜外 (ed)和iv [12 5I]标记虎纹毒素 Ⅰ ([12 5I]HWTX Ⅰ )后分布的差异。方法Iodogen法制备 [12 5I]HWTX Ⅰ ,膈神经 膈肌法测定生物活性。反相高效液相色谱法鉴定放射化学纯度 ,三氯醋酸沉淀法测定放射性药物浓度。结果[12 5I]HWTX Ⅰ生物活性标记前后相近 ,放射化学纯度为 98.5 %。给药后 2h ,ed组椎管局部放射性明显高于iv组 (P <0 .0 5 ) ,ed和iv后组织放射性分别在 2h和 10min达峰值。泌尿系统放射性含量最高 ,脂肪、肌肉和脑放射性最低。放射性主要经尿排泄。结论 ed后椎管局部放射性高 ,维持时间较长 ,血清峰浓度较iv组低 ,有利于发挥局部镇痛作用 ,减少全身副作用。
OBJECTIVE: To compare the postdistribution of the epidural (ed) and iv [12 5 I]-labeled huwenxin I ([12 5 I]HWTX I ). Methods Iodogen method was used to prepare [12 5 I]HWTX I. The phrenic nerve was used to determine the biological activity. The radiochemical purity was determined by RP-HPLC, and the concentration of radiopharmaceuticals was determined by trichloroacetic acid precipitation. Results The bioactivity markers of [12 5 I]HWTX I were similar before and after, and the radiochemical purity was 98.5%. At 2h after administration, local radioactivity of the edema was significantly higher in the ed group than in the iv group (P < 0.05), and the radioactivity of the ed and iv groups peaked at 2h and 10min, respectively. The urinary system has the highest radioactive content and has the lowest radioactivity in fat, muscle and brain. Radioactivity is mainly excreted in the urine. Conclusion After the ed local spinal canal was highly radioactive, maintained for a long time, and the serum peak concentration was lower than that of the iv group, which was conducive to local analgesia and reduced systemic side effects.