摘要
目的研究奥克梯隆型人参皂苷ocotillol,RT5和F11的大鼠血浆蛋白结合率。方法采用平衡透析法分别模拟ocotillol,RT5和F11在体内与血浆蛋白结合的过程,建立液相色谱串联质谱(LC-MS/MS)测定3个不同质量浓度的ocotillol,RT5和F11在透析袋内血浆和透析袋外缓冲液中的浓度,并分别计算3种化合物的血浆蛋白结合率。结果 LC-MS/MS测定ocotillol,RT5和F11的线性关系良好(r≥0.996 2),准确度、精密度、提取回收率、基质效应以及稳定性均符合生物样品分析要求。Ocotillol,RT5和F11低、中、高3个质量浓度间的血浆蛋白结合率数据均无显著性差异(P>0.05),3种化合物与大鼠的平均血浆蛋白结合率分别为(84.55±1.69)%,(83.08±1.27)%和(62.23±2.97)%。结论 Ocotillol和RT5与大鼠血浆蛋白有较强的结合作用,F11与大鼠血浆蛋白属于中等强度结合。
OBJECTIVE To study the rat plasma protein binding rates of ocotillol, RT5 and F11, the main active ingredients of ocotillol type ginsenosides. METHODS The equilibrium dialysis method was used to imitate the in vivo plasma protein binding process of ocotillol, RT5 and F11. The liquid chromatography-tandem mass spectrometry(LC-MS/MS) method was established for determination of the concentrations of three ginsenosides in and out of the dialysis membrane at different concentrations, and the plasma protein binding rates of three ginsenosides were calculated. RESULTS The LC-MS/MS method showed good linearity(r≥0.996 2) in the established concentration ranges. The accuracy, precision, extraction recovery, matrix effect and stability of the analytes all met the methodology requirements. The average plasma protein binding rates of ocotillol, RT5 and F11 in rats were(84.55±1.69)%,(83.08±1.27)% and(62.23±2.97)%, respectively. There were no significant differences among three concentrations. CONCLUSION Ocotillol and RT5 are highly bounded to plasma protein in rats, while F11 belongs to moderate protein binding rate.
作者
燕晓晶
李振国
姜杰
英子越
耿聪
YAN Xiao-jing;LI Zhen-guo;JIANG Jie;YING Zi-yue;GENG Cong(The Second Affiliated Hospital of Dalian Medical University,Dalian 116023,China)
出处
《中国药学杂志》
CAS
CSCD
北大核心
2020年第24期2029-2035,共7页
Chinese Pharmaceutical Journal
基金
国家自然科学基金项目资助(31700293)
大连医科大学附属第二医院-中国科学院大连化学物理研究所“个体化诊疗协同创新中心”联合基金项目资助
大连医科大学附属第二医院博士科研启动基金项目资助
大连医科大学附属第二医院青年后备人才培养计划项目资助。
