双硒唑烷及其羟丙基-β-环糊精包合物在大鼠胃肠道的吸收特性  

Absorptions of Eb versus its HP-β-CD inclusion complex in rat gastrointestinal tract

作　　者：崔翰明[1] 武凤兰[1] 

机构地区：[1]北京大学药学院

出　　处：《中国新药杂志》2006年第21期1837-1841,共5页Chinese Journal of New Drugs

基　　金：国家自然科学基金(30472036);北京自然科学基金(7021001);北京科委基金(H020220060190)

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。Objective：To investigate the absorption of Eb （ 1,2-[ bis（ 1,2-benzisoselenazolone-3 （2H）-ketone） ] ethane） versus Eb-HP-β-CD inclusion complex in rat gastrointestinal tract. Methods： The absorption of Eb and Eb-HP-β-CD inclusion complex in G1 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-β-CD at small intestine, colon and rectum. Both Eb and Eb-HP-β-CD inclusion were less absorbed at gastric portion. The absorption rate constant （Ka） of Eb-HP-β-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.

关 键 词：双硒唑烷 羟丙基-Β-环糊精 包合物 翻转肠囊 吸收机制 

分 类 号：R945[医药卫生—微生物与生化药学] R979.1[医药卫生—药剂学]