文献类型：期刊文献

中文题名：高效液相色谱-超滤法测定常氧及缺氧大鼠血浆中毛蕊花糖苷的蛋白结合率

英文题名：Determination of Plasma Protein Binding Rate of Verbascoside in Normoxic and Hypoxic Rats by HPLC-ultrafiltration Method

作者：王维刚[1,2,3];王芃[1,2,3];李晓琳[2,3];王俊丽[4];刘天龙[2,3];陈升富[1,2,3];李茂星[1,2,3,5];阳志强[2,5]

第一作者：王维刚

机构：[1]甘肃中医药大学药学院,甘肃兰州730000;[2]联勤保障部队第九四〇医院临床药学科,甘肃兰州730050;[3]甘肃省药学行业技术中心,甘肃兰州730050;[4]西宁联勤保障中心药品仪器监督检验站,甘肃兰州730050;[5]西北民族大学化工学院,甘肃兰州730124

第一机构：甘肃中医药大学药学院（西北中藏药协同创新中心办公室）

年份：2021

卷号：32

期号：12

起止页码：1839

中文期刊名：中药新药与临床药理

外文期刊名：Traditional Chinese Drug Research and Clinical Pharmacology

收录：CSTPCD;;北大核心:【北大核心2020】；CSCD:【CSCD2021_2022】；

基金：甘肃省重点研发计划项目(20YF3FA035);甘肃省卫生行业科研计划项目(GSWSKY2020-41);九四○医院青年培育项目(2021yxky060);中央高校基本科研业务费专项资金项目(31920200010);九四○医院“新冠肺炎(COVID-19)”应急医学科研项目(20yjky018)。

语种：中文

中文关键词：毛蕊花糖苷;高效液相色谱-超滤法;常氧;缺氧;血浆蛋白结合率;大鼠

外文关键词：Verbascoside;HPLC-ultrafitration;normoxia;hypoxia;plasma protein binding;rates

摘要：目的建立毛蕊花糖苷血浆蛋白结合率的测定方法,比较常氧及缺氧大鼠血浆中毛蕊花糖苷蛋白结合率的异同。方法将大鼠置于低压低氧动物实验舱中,于海拨7 500 m下缺氧暴露3 d制备缺氧大鼠模型。采用超滤法处理样品,结合高效液相色谱(HPLC)法测定常氧及缺氧大鼠血浆中毛蕊花糖苷游离型药物浓度(Cf)和总药物浓度(Ct),并考察超滤膜非特异性结合率(NSB),对Cf进行矫正后,计算血浆蛋白结合率。结果大鼠血浆中毛蕊花糖苷浓度为3、6、12μg·mL^(-1)时,毛蕊花糖苷与常氧大鼠血浆的蛋白结合率分别为(62.02±8.51)%、(60.17±5.59)%和(62.60±3.77)%;与缺氧大鼠血浆的蛋白结合率分别为(32.79±4.20)%、(33.16±1.74)%和(32.72±2.20)%,两者比较差异有统计学意义(P<0.05)。结论毛蕊花糖苷与常氧大鼠血浆蛋白属于中强度结合,且在研究的浓度范围内,不具浓度依赖性,而毛蕊花糖苷与缺氧大鼠血浆蛋白结合强度明显低于常氧大鼠血浆。
Objective To establish a method for determination of plasma protein binding rate of verbascoside,and compare the difference of plasma protein binding rate in normoxic and hypoxic rats.Methods The rats were placed in a low-pressure and hypoxic animal experiment chamber,and hypoxic rat models were prepared by exposure to hypoxia at altitude of 7 500 m for 3 days.The samples were processed by ultrafiltration and the HPLC method was used to determine verbascosides in the plasma of normoxic and hypoxic rats,to obtain free drug concentration(Cf)and total drug concentration(Ct);the ultrafiltration membrane non-specific binding rate(NSB)was also investigated.After correctiion for Cf,the plasma protein binding rate was calculated according to the traditional formula of ultrafiltration.Results When the concentrations of verbascoside in rat plasma was 3,6 and 12 μg·mL^(-1),the plasma protein binding rates of verbascoside with normoxic rats were(62.02 ± 8.51)%,(60.17 ± 5.59)%,and(62.60 ±3.77)%;and the plasma protein binding rates with hypoxic rats were(32.79±4.20)%,(33.16±1.74)%,and(32.72±2.20)%.The difference of the plasma protein binding rate was significant between the normoxic and hypoxic rats(P<0.05).Conclusion The plasma protein binding of verbascoside in normoxic rats is moderate,and there is no concentration-dependence within the concentration range of the study.The binding intensity of verbascoside to plasma protein in hypoxic rats is obivious lower than that in normoxia rats.