摘要
考察了杜仲提取物中京尼平苷酸（1）、新绿原酸（2）、绿原酸（3）和隐绿原酸（4）在大鼠小肠的吸收动力学特性。采用大鼠在体肠循环灌流模型,建立了UPLC-MS/MS法测定1~4,考察了p H值、样品浓度、胆汁和P-糖蛋白（P-gp）抑制剂对1~4在体肠吸收的影响。结果显示,1在p H 7.4条件下吸收较差,2、4在不同p H值下的吸收有显著差异,而3对p H值不敏感。2、3在中浓度样品溶液（4.0 mg/ml）的3 h累积吸收率（A）显著高于高浓度样品（8.0 mg/ml）,两者在高浓度下的吸收存在饱和现象。胆汁对1~4的吸收均有显著抑制作用。1~4在整个肠段均有吸收,主要吸收部位在小肠;P-gp抑制剂不影响杜仲提取物的肠吸收,提示1~4可能不是P-gp的底物。
The absorption kinetic characteristics of the main active components in extract of Cortex Eucommiae, including geniposidic acid （1）, neochlorogenic acid （2）, chlorogenie acid （3） and cryptochlorogenic acid （4） in rats＇ intestine, were investigated by adopting the in situ rat circulation intestinal perfusion model. A UPLC-MS/MS method was established for the determination of I - 4, and their absorption at different conditions, including pH values, sample concentrations, bile and P-gp inhibitors was investigated. As a result, the absorption of I was poor at pH 7.4, while that of 2 and 4 was significantly different at different pH values. But 3 was insensitive to pH values. The accumulated absorption rates （3 h, A） of 2 and 3 at middle concentrations （4.0 mg/ml） were higher than that at high concentrations （8.0 mg/ml）. There was saturation phenomenon of absorption when they were at high concentrations. The bile significantly inhibited the absorption of I - 4. However, P-gp inhibitor had no effect on the absorption of the Cortex Eucommiae extract. The results indicated that the absorption of 1 - 4 existed in the whole intestinal segments, while the main absorption site was at the small intestine. It also suggested that 1 - 4 might not be the substrates of P-gp.
出处
《中国医药工业杂志》
CAS
CSCD
北大核心
2015年第7期730-735,共6页
Chinese Journal of Pharmaceuticals
基金
贵州省科技重大专项(黔科合重大专项字[2012]6009)
贵州省中药现代化研究开发专项(黔科合中药字[2013]5062、黔科合重G字[2013]4001)
贵州省高等学校创新能力提升计划(黔教合协同创新字[2013]04)
