【摘要】 目的:研究双硒唑烷(1,2-[二(1,2-苯并异硒唑酮-3(2H)-酮)]乙烷,Eb)及其羟丙基-β-环糊精(HP-β-CD)包合物在大鼠胃肠道的吸收特性,比较包合对Eb胃肠道吸收的影响。方法:采用大鼠在体结扎灌注法考察Eb及Eb-HP-β-CD包合物溶液在消化道各部位的吸收情况;采用大鼠离体翻肠囊法研究Eb-HP-β-CD包合物在小肠中的吸收速度及吸收机制。结果:Eb主要在小肠吸收,而包合物在小肠、结肠和直肠中均有较大吸收,Eb及其包合物在胃内的吸收均很少,Eb经包合后吸收明显增加。离体翻转肠囊实验显示不同浓度Eb-HP-β-CD包合物溶液在空肠和回肠的平均吸收速率常数(Ka)分别为(0．601±0．024)和(0．615±0．021)h-1;肠囊内的Eb浓度与取样时间存在线性关系;各浓度Eb的溶液的Ka基本不变。结论:Eb口服的主要吸收部位在小肠,经HP-β-CD包合后吸收明显增加,在整个肠道(包括小肠、结肠和直肠)均有较大吸收。Eb的吸收符合一级吸收模型,以被动扩散方式吸收。更多还原

【Abstract】 Objective: To investigate the absorption of Eb ( 1,2-[ bis( 1 ,2-benzisoselenazolone-3 (2H) -ketone) ] ethane) versus Eb-HP-B-CD inclusion complex in rat gastrointestinal tract. Methods; The absorption of Eb and Eb-HP-B-CD inclusion complex in GI portions was investigated using ligated perfusion technique in situ and in small intestinal using gut exstrophy in vitro. Results:The Eb was mainly absorbed at small intestinal portion, and Eb-HP-B-CD at small intestine, colon and rectum. Both Eb and Eb-HP-B-CD inclusion were less absorbed at gastric portion. The absorption rate constant (Ka) of Eb-HP-B-CD inclusion was significantly higher than the one of Eb alone when variable doses, showing a mean Ka of (0. 601±0. 024) and (0. 615±0. 021 )h-1 at jejunum and ileum, respectively, in the gut exstrophy examination. A calibrated linear curve showing the accumulative uptake of Eb versus Eb concentration at jejunum and ileum was found. The Ka remained constant when variable doses. Conclusion; The Eb absorption obeyed first-order kinetics and a passive diffusion mechanism.更多还原