摘要
目的:研究染料木素自微乳在大鼠的在体肠吸收机制。方法:采用大鼠在体肠回流装置,UV,HPLC分别测定酚红和染料木素的含量。考察药物浓度、pH、不同肠段及P-糖蛋白(P-gp)抑制剂维拉帕米对染料木素吸收的影响。结果:染料木素自微乳在药物浓度为0.05～0.5 g·L^(-1)和pH为5.4～7.8时小肠吸收速率常数K_a均无统计差异;各肠段的吸收速率常数K_a空肠>回肠>十二指肠>结肠,空肠与其他肠段有统计差异(P<0.05);维拉帕米显著增加染料木素的肠吸收(P<0.05)。结论:染料木素自微乳在大鼠肠道的吸收呈一级动力学过程,吸收机制为被动扩散,在整个肠段都有吸收,最佳吸收部位在空肠。药物吸收受P-糖蛋白外排影响,而pH对药物吸收无显著影响。
Objective： To investigate the absorption mechanism of genistein self-microemulsifying system in rat intestines. Method： The concentrations of phenol red and genistein by in situ perfusion in rats were determined by UV and HPLC, respectively. The effects of drug concentrations, pH, various intestinal segments and P-glycoprotein （P-gp） inhibitor verapamil on the absorption had been studied. Result： The absorption rate constant （Ka ） of genistein had no significant difference at concentrations of 0. 05 ～ 0. 5 mg · mL^-1 and pH of 5.4 ～ 7.8 in perfusion. It was Ka of jejunum 〉 ileum 〉 duodenum 〉 colon. The absorption of genistein in jejunum had significant difference （P 〈 0.05 ） compared with other parts of intestines. Ko was increased obviously when verapamil was coperfused with genistein （ P 〈 0. 05 ）. Conclusion： The absorption of genistein seff-microemulsifying system is a first order process with passive diffusion mechanism related to P-gp efflux. It can be absorbed at all segments of rat intestine, and the jejunum is the best absorption segment, pH had no special effect on the absorption of genistein self-microemulsifying system in rat intestime.
出处
《中国中药杂志》
CAS
CSCD
北大核心
2008年第12期1406-1409,共4页
China Journal of Chinese Materia Medica
基金
国家“十五”科技攻关项目(2004BA721A46)
关键词
染料木素自微乳
肠吸收动力学
P-糖蛋白抑制剂
genistein self-microemulsifying system
intestinal absorption kinetics
P-glycoprotein inhibitor
