拉马宁碱的大鼠在体肠吸收机制研究  

Intestinal absorption of lehmannine in rat

作　　者：王丹[1,2] 魏玉辉[1] 张帆[1,2] 李育卿[1,2] 武新安[1] 

机构地区：[1]兰州大学第一医院药剂科,甘肃兰州730000 [2]兰州大学药学院,甘肃兰州730000

出　　处：《中成药》2012年第5期828-831,共4页Chinese Traditional Patent Medicine

摘　　要：目的研究拉马宁碱大鼠在体肠吸收机制。方法采用大鼠在体单向肠灌流吸收实验模型,应用重量法校正灌流液体积,通过反相高效液相色谱法测定灌流液中药物浓度,并考察吸收部位、药物质量浓度、P-糖蛋白(P-gp)抑制剂及有机阳离子转运蛋白(OCTs)抑制剂对药物吸收的影响。结果拉马宁碱在整肠段均有吸收,吸收速率常数(Ka)和表观吸收系数(Papp)分别按照回肠、结肠、空肠、十二指肠的顺序下降;2～20μg/mL的药物质量浓度对Ka和Papp无显著影响(P>0.05);含P-gp抑制剂组与不含P-gp抑制剂组相比,Ka和Papp无显著性差异(P>0.05);含OCTs抑制剂组与不含OCTs抑制剂组相比,Ka和Papp也无显著性差异(P>0.05)。结论拉马宁碱为全肠段吸收,吸收机制为被动扩散,且P-gp及OCTs对药物的小肠吸收基本无影响。AIM To investigate the rat＇s intestinal absorption of lehmannine extracted from Sophora alopecuroides L.METHODS Single-pass perfusion was applied and the gravimetry was used to correct the perfusion volume.The concentrations of lehmannine in intestinal fluid was measured by HPLC.Absorption site,drug concentration,inhibiting effect of P-glycoprotein（P-gp） and organic cation transporters（OCTs） were studied.RESULTS Lehmannine was absorbed in the whole intestine.Its absorption constant（Ka） and apparent absorption coefficient（Papp） were as follows： ileumcolonjejunumduodenum.Drug concentration had little connection with Ka and Papp（P〈0.05）.There was no significant difference in Ka and Papp between presence of P-gp/OCTs inhibitor and no P-gp /OCTs inhibitor（P〈0.05）.CONCLUSION Lehmannine is absorbed in the whole intestine,belonging to a passive diffusion process,and does not relate to lehmannine concentrations,P-gp and OCTs.

关 键 词：拉马宁碱 在体单向肠灌流 肠吸收 

分 类 号：R966[医药卫生—药理学]