【摘要】 目的 :研究碘 12 5标记的双峰驼诱导排卵因子在母驼体内的生物分布特性及药代动力学模型 .方法 :采用高效碘标法 (NBS法 )进行12 5I OIF的标记 ,并于标记后不同时间测定其标记率以观察标记物的稳定性 .将12 5I OIF经母驼阴道输入给药 ,给药后不同时间采血 ,测定其放射性计数 ,用3P97药代动力学软件求取药代动力学参数 ;给药后处死骆驼 ,分别取主要脏器 ,经物理衰变校正后计算每克组织的放射性百分注射量 (%ID·g-1) .结果 :12 5I OIF的标记率 80 % ,放化纯度 95 % .将标记物室温下放置 96h ,测得其标记率为70 % ;12 5I OIF在母驼体内的生物学分布在肝中的浓集较高(肝脏代谢 ) ,在脑组织中以垂体的放射性浓聚最高 ;12 5I OIF的药代动力学参数分别为T1/ 2 (ka) 11.8h ,T1/ 2 (ke) 2 6 .4h ,AUC 11.0 6 1× 10 12 Bq·L-1.结论 :采用NBS法碘标的标记率高 ,稳定性好 ,操作简便 .12 5I OIF的药代动力学最佳数学模型符合一级吸收二室开放模型 ,主要经肠道排出体外更多还原

【Abstract】 AIM: To investigate the pharmacokinetics and bio distribution characteristics of 125 I labeled ovulation inducing factor (OIF) in bactrian camels. METHODS: OIF was iodinated by using N bromosuccinimide (NBS) as oxidant and the yield was detected at different times after injection of 125 I OIF so as to evaluate its stability in vitro . The blood and organs radio activities were measured. The concentrations of 125 I OIF were evaluated with pharmacokinetic 3P97 software. RESULTS: The yield of 125 I OIF was 80% and radiochemical purity was 95% and even after 96 h at room temperature, the yield was still 70%. The bio distribution of 125 I OIF was characterized by a relatively high concentration in liver and the highest concentration was found in pituitary. The parameters of 125 I OIF were T 1/2 (ka) 11.8 h, T 1/2 (ke) 26.4 h, and AUC 11.06 1×1012 Bq·L -1 respectively. CONCLUSION: The iodination by NBS is highly efficient, stable and easy to operate. Pharmacokinetics of 125 I OIF are in consistence with 1st absorption and two compartment model. 125 I OIF is eliminated mainly through gastrointestinal tract.更多还原