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目的 :研究赛诺吉宁 ( Suanordrin,SR)在大鼠体内过程和药代动力学 ,为临床合理用药提供科学依据。 方法 :取大鼠 12只 ,雌雄各半 ,经胃灌给 14 C标记的 SR[( 14 C- SR)为 3.7MBq/( 10 mg/ kg) ]后 ,每 2只同性大鼠饲养同一代谢笼中 ,待 12、2 4、72 h及 1、2、3周后 ,采用整体放射自显影等技术测定 SR在大鼠体内组织中的分布和尿、粪、胆汁中的排泄。 结果 :胃灌药后不同时相的放射自显影图中可见 14 C- SR在胃肠道中的动态分布 ,3周时已消除 ,各时相组织中放射性分布 ,以肝脏为最高 ,依次是肾、心、肺、肾上腺、脾等脏器 ,体内消除较缓慢 ,2 1d内尿粪排泄占给药量的 98.8% ,以尿排泄为主 (占 77.6% ) ,2 4 h内胆汁排泄为 2 8.6% ,以药物原形排泄为主。 结论 :所测 14 C- SR的层析板上 Rf值其放射性与标准品 14 C- SR相当 Rf值的放射性相符 ,表明该方法灵敏、稳定、特异性好 ;14 C- SR在组织中分布结果与液体闪烁仪测定结果相吻合 ,提示在短时间内多次给药 ,可能会产生蓄积
Objective: To study the process and pharmacokinetics of Suanordrin (SR) in rats and to provide a scientific basis for clinical rational drug use. METHODS: Twelve male and female rats, each male and female, were fed the same metabolism with 14 C-labeled SR [(14 C-SR) 3.7 MBq / (10 mg / kg)] Cage, to be 12,2 4,72 h and 1, 2, and 3 weeks later, the whole autoradiography and other techniques were used to determine the distribution of SR in tissues of rats and excretion in urine, feces and bile. Results: The dynamic distribution of 14 C-SR in the gastrointestinal tract was observed at different phases after gastric perfusion. The distribution of 14 C-SR in the gastrointestinal tract was eliminated at 3 weeks. The radioactivity distribution in each phase and phase was highest in the liver, followed by the kidney , Heart, lung, adrenal, spleen and other organs, the body to eliminate more slowly, within 21 days urinary excretion accounted for 98.8% of the dose, urinary excretion (77.6%), 24 hours bile excretion of 2 8.6%, the main form of drug excretion. CONCLUSIONS: The Rf values of the 14 C-SR chromatograms agree well with those of the standard 14 C-SR equivalent Rf values, indicating that the method is sensitive, stable, and specific; 14 C-SR is distributed throughout the tissue Results and liquid scintillation assay results agree, suggesting that in a short period of time multiple administration, may produce accumulation