坤复康片中异泽兰黄素小肠吸收特征研究  

Study on the small intestinal absorption characteristics of eupatilin in Kunfukang tablets

作　　者：徐人杰 张涛[2] 潘海滔 钦博 周萍[4] XU Renjie;ZHANG Tao;PAN Haitao;QIN Bo;ZHOU Ping(Center for Medical Research and Achievement Transformation,Shaoxing Women and Children’s Hospital in Zhejiang Province,Shaoxing 312000,China;Genetic Laboratory,Shaoxing Women and Children’s Hospital in Zhejiang Province,Shaoxing 312000,China;Department of Clinical Laboratory,Shaoxing Women and Children’s Hospital in Zhejiang Province,Shaoxing 312000,China;Clinical Pharmacy Room,Shaoxing Women and Children’s Hospital in Zhejiang Province,Shaoxing 312000,China)

机构地区：[1]浙江省绍兴市妇幼保健院医学研究与成果转化中心,浙江绍兴312000 [2]浙江省绍兴市妇幼保健院遗传实验室,浙江绍兴312000 [3]浙江省绍兴市妇幼保健院检验科,浙江绍兴312000 [4]浙江省绍兴市妇幼保健院临床药学室,浙江绍兴312000

出　　处：《中国现代医生》2022年第6期38-42,共5页China Modern Doctor

基　　金：国家自然科学基金委员会资助项目(81701522);浙江省自然科学基金(LQ21H040003)。

摘　　要：目的研究坤复康片中的异泽兰黄素小肠吸收和坤复康片对其吸收的影响。方法Caco-2细胞模型研究不同药物浓度、pH值、温度和抑制剂对异泽兰黄素双向渗透吸收的影响。采用药动学实验研究坤复康片在体内对异泽兰黄素吸收的影响。结果数据表明,异泽兰黄素在Caco-2细胞模型中吸收较差,三种待测浓度下其吸收仅为3.27×10^(-7)cm/s至5.37×10^(-7)cm/s[从顶膜端(AP)到底膜端(BL)]和从6.27×10^(-7)cm/s至9.63×10^(-7)cm/s(从BL到AP),其转运具有pH和温度依赖性。异泽兰黄素的细胞通透性受多耐药蛋白抑制剂MK571和吲哚美辛的影响。当坤复康溶液加入后,异泽兰黄素的吸收显著性增加,从4.41×10^(-7)cm/s至6.43×10^(-7)cm/s(从AP到BL)。在药动学实验中,坤复康组的异泽兰黄素相对于单体组有更大的吸收入血暴露量。结论坤复康片中某些成分会显著促进异泽兰黄素的吸收。Objective To study the small intestinal absorption of eupatilin in Kunfukang tablets and the effect of Kunfukang tablets on its absorption.Methods Caco-2 cell model was used to study the effects of different drug concentrations,pH values,temperatures,and inhibitors on the bidirectional permeation and absorption of eupatilin.Pharmacokinetic experiments were used to study the effect of Kunfukang tablets on the absorption of eupatilin in vivo.Results Data showed that eupatilin was poorly absorbed in the Caco-2 cell model,and its absorption was 3.27×10^(-7)cm/s to 5.37×10^(-7)cm/s(from AP to the BL)and from 6.27×10^(-7)cm/s to 9.63×10^(-7)cm/s(from BL to AP)at three concentrations to be measured.Its transport was pH and temperature-dependent.The cell permeability of eupatilin was affected by the multidrug resistance protein inhibitors MK571 and indomethacin.After the addition of Kunfukang solution,the absorption of eupatilin significantly increased,from 4.41×10^(-7)cm/s to 6.43×10^(-7)cm/s(from AP to BL).In the pharmacokinetic experiment,the absorption exposure of eupatilin in the Kunfukang group was greater than that in the monomer group.Conclusion Some components in Kunfukang tablets can significantly promote the absorption of eupatilin.

关 键 词：异泽兰黄素 CACO-2 口服 吸收机制 坤复康片 

分 类 号：R969.2[医药卫生—药理学]