摘要
目的:研究大黄酸在大鼠不同肠段的吸收特性,并考察P-糖蛋白(P-gp)和多药耐药相关蛋白(MRP2)对其肠吸收的影响。方法:采用在体单向肠灌流法考察大黄酸在不同肠段的吸收,用高效液相色谱法测定肠灌流液中大黄酸的含量;分别计算大黄酸单独在大鼠各肠段的吸收速率常数(Ka)和表观吸收系数(Papp),以及在P-gp抑制剂盐酸维拉帕米和MRP2抑制剂吲哚美辛存在的情况下,在大鼠肠中吸收的Ka和Papp值;比较计算结果之间的差异。结果:大黄酸在十二指肠、空肠、回肠和结肠中的吸收均具有较高的Ka和Papp值,并且随肠道的生理走向吸收率降低,但无明显的统计学差异;当加入不同浓度P-gp抑制剂和MRP2抑制剂后,与空白组比较大黄酸的吸收无显著性改变。结论:大黄酸属于易吸收化合物,并且在大鼠十二指肠、空肠和结肠具有相似的吸收特性;其在大鼠肠内的吸收不受P-gp抑制剂和MRP2抑制剂的影响,因此推测大黄酸的吸收不受P-gp和MRP2的外排的影响。
Objective：To research the absorption characteristics of rhein in different intestinal sections,and to study the impact of P-glycoprotein（P-gp） and multidrug resistance-associated protein 2（MRP2） on the rhein absorption.Methods：One-way in vivo intestinal perfusion was used to reveal the absorption character of rhein;high performance liquid chromatography was used to determine the content of rhein in the intestinal perfusate;the absorption rate constant（Ka） and the apparent absorption coefficient（Papp） in each intestinal section were calculated separately,compared with the existence of P-gp inhibitor（verapamil hydrochloride） or MRP2 inhibitor（indomethacin）.Results：The absorption of rhein in the duodenum,jejunum,ileum and colon showed high values of the Ka and Papp.Although differences were observed,they showed no statistically significant（p〉0.05）.Each value was not changed significantly after adding the P-gp inhibitor or the MRP2 inhibitor.Conclusion：Rhein is easily absorbed in rat and the absorption characteristics in different intestinal sections demonstrated almost the same.The absorption action of rhein is not affected by the P-gp inhibitor or the MRP2 inhibitor,thus rhein is not the substrate of P-gp and MRP2.
出处
《中药药理与临床》
CAS
CSCD
北大核心
2011年第5期31-34,共4页
Pharmacology and Clinics of Chinese Materia Medica
基金
国家自然科学基金(No:81001689)
教育部博士点基金(No:20095132110003)
关键词
大黄酸
肠吸收
P-糖蛋白
多药耐药相关蛋白
rhein
intestinal absorption
P-glycoprotein
multidrug resistance-associated protein
