中国中药杂志

2008, (12) 1406-1409

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染料木素自微乳的大鼠在体肠吸收机制研究
Study on absorption mechanism of genistein self-microemulsifying system in rat intestines

杜先华;牛欣;冯前进;杜红;李海燕;
DU Xian-hua~1 NIU Xin~1 FENG Qian-jin~2 DU Hong~1 LI Hai-yan~1 (1.Beijing University of Chinese Medicine,Beijing 100029,China; 2.Shanxi College of Traditional Chinese Medicine,Taiyuan 030024,China)

摘要(Abstract):

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-glyeoprotein(P-gp)inhibitor verapamil on the absorption had been studied.Result:The absorption rate constant(K_a)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 K_a of jejunum>ileum>duodenum>colon.The absorption of genistein in jejunum had significant difference(P<0.05)compared with other parts of intestines.K_a was increased obviously when verapamil was coper- fused with genistein(P<0.05).Conclusion:The absorption of genistein self-microemulsifying system is a first order process with passive diffusion mechanism related to P-gp efllux.It can be absorbed at all segments of rat intestine,and the jejunum is the best ab- sorption segment,pH had no special effect on the absorption of genistein seff-mieroemulsifying system in rat intestime.

关键词(KeyWords): 染料木素自微乳;肠吸收动力学;P-糖蛋白抑制剂
genistein self-mieroemulsifying system;intestinal absorption kinetics;P-glycoprotein inhibitor

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基金项目(Foundation): 国家“十五”科技攻关项目(2004BA721A46)

作者(Author): 杜先华;牛欣;冯前进;杜红;李海燕;
DU Xian-hua~1 NIU Xin~1 FENG Qian-jin~2 DU Hong~1 LI Hai-yan~1 (1.Beijing University of Chinese Medicine,Beijing 100029,China; 2.Shanxi College of Traditional Chinese Medicine,Taiyuan 030024,China)

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