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目的探讨大鼠口服放射性氚标记盐酸川丁特罗([3H]SPFF)后经尿、粪和胆汁的排泄动力学特征。方法采用化学法合成[3H]SPFF,并进行放化纯度鉴定。粪尿排泄实验观察SD大鼠经口45.5 MBq·kg-1(1 mg·kg-1)给药后168 h内经尿和粪累积放射性排出率。胆汁排泄实验观察胆汁引流模型大鼠给药后,72 h内胆汁累积放射性排出率。HPLC-放射性检测法鉴定单只大鼠尿和胆汁中放射性成分组成。结果化学法合成获得5 m L[3H]SPFF甲醇溶液(比活度403 GBq·g-1),化学纯度>96%,放化纯>97%。粪尿排泄实验的结果表明,经口给药后,SD大鼠体内放射性物质经泌尿系统排出较快,168 h经尿粪累积排出率达84.74%,其中尿回收56.63%,粪回收28.10%。胆汁排泄实验显示,给药后3 d,经胆汁放射性累积排出率为29.3%。放射性组成分析结果显示,单只SD大鼠给药后72 h尿液中累积总放射性排出量占给药量的48.61%,其中原型占4.71%,产物占42.62%。72 h胆汁中累积总放射性排出量占给药量的28.14%,其中原型占9.51%,产物占18.63%。结论大鼠经口盐酸川丁特罗后吸收完全,主要经尿液以代谢物形式排泄。
Objective To investigate the kinetic characteristics of excretion of urine, feces and bile in rats after oral administration of radioactive tritiated cholebuterol ([3H] SPFF). Methods [3H] SPFF was synthesized by chemical method and identified by radiochemical purity. Excretion of excretion was observed in 168 h after oral administration of 45.5 MBq · kg-1 (1 mg · kg-1) in SD rats. Bile excretion experiment was used to observe the cumulative bile excretion rate within 72 h after bile drainage model administration in rats. HPLC - radioactive detection method to identify single rat urine and bile radioactive composition. Results 5 mL of [3H] SPFF methanol solution (403 GBq · g-1) was obtained by chemical method. The chemical purity was> 96% and the radiochemical purity was> 97%. Urine excretion test results show that, after oral administration, SD rats in vivo radioactive material excreted faster through the urinary system, 168 h by urine excretion cumulative discharge rate of 84.74%, of which urine 56.63% recovery, manure recovery 28.10%. Bile excretion experiments showed that 3 days after administration, the bile radioactive cumulative discharge rate was 29.3%. The results of radioactive composition analysis showed that the total radioactive discharge in urine of single SD rats accounted for 48.61% of the dose at 72 hours after administration, of which the prototype accounted for 4.71% and the product accounted for 42.62%. The total radioactive discharge in bile during 72 h accounted for 28.14% of the dosage, of which the prototype accounted for 9.51% and the product accounted for 18.63%. Conclusion After oral chuanbuterol hydrochloride is absorbed completely, it is excreted mainly as metabolites in the urine.