平衡透析法结合HPLC测定去氢骆驼蓬碱衍生物(DH-004)在大鼠血浆的蛋白结合率  

Protein binding rate of harmine derivative(DH-004)in the rats plasma determined by equilibrium dialysis combined with HPLC

作　　者：徐楠 高惠静[2] 冉鑫 李玉玲 滕亮[2] XU Nan;GAO Hui-jing;RAN Xin;LI Yu-ling;TENG Liang(Pharmacy College of Xinjiang Medical University,Urmuqi 830011,Xinjiang Uygur Autonomous Region,China;Department of Pharmacy,The First Affiliated Hospital of Xinjiang Medical University,Urumqi 830054,Xinjiang Uygur Autonomous Region,China)

机构地区：[1]新疆医科大学药学院,新疆乌鲁木齐830011 [2]新疆医科大学第一附属医院药学部,新疆乌鲁木齐830054

出　　处：《中国临床药理学杂志》2021年第22期3144-3147,共4页The Chinese Journal of Clinical Pharmacology

基　　金：中华医学会临床药学分会吴阶平医学基金会科研专项基金资助项目(320.6750.19090-9);新疆维吾尔自治区自然科学基金资助项目(2020D01C245)。

摘　　要：目的研究去氢骆驼蓬碱衍生物(DH-004)在大鼠血浆的蛋白结合率。方法Wistar大鼠腹主动脉采血,肝素抗凝,4℃下以3.5×10^(3) r·min^(-1)离心15 min后分离血浆。以替硝唑为内标,用平衡透析法处理样品,用高效液相色谱(HPLC)法测定透析袋内外溶液中DH-004的浓度,计算蛋白结合率。结果DH-004于大鼠血浆中在1.05,2.10,5.26μg·mL^(-1)下的血浆蛋白结合率分别为(89.96±0.89)%,(90.79±0.85)%和(91.39±1.00)%。结论DH-004与大鼠血浆蛋白有较强的结合作用,属于高蛋白结合型药物。Objective To determine the plasma protein binding rate of harmine derivative(DH-004).Methods The abdominal aorta of blood was collected from Wistar rats,and heparin sodium was used as anticoagulant.The plasma was separated at 4℃by centrifugation at 3.5×10^(3) r·min^(-1) for 15 min.Tinidazole was regarded as internal standard substance,and equilibrium dialysis method was applied to pretreat plasma sample.The concentrations of DH-004 inside and outside of dialysis bag were measured by high performance liquid chromatography(HPLC).Protein binding rate was calculated.Results The plamsa protein binding rates of DH-004 in rat plasma at 1.05,2.10,5.26μg·mL^(-1) were(89.96±0.89)%,(90.79±0.85)%and(91.39±1.00)%,respectively.Conclusion DH-004 have strong binding effect on rat plasma protein,and belong to high protein binding drugs.

关 键 词：去氢骆驼蓬碱衍生物 高效液相色谱法 平衡透析法 血浆蛋白结合率 

分 类 号：R28[医药卫生—中药学]