平衡透析法研究荭草及其制剂的人血浆蛋白结合率  

Determination of plasma protein binding rate both in Polygonum orientale L. extract and compound Hongcao freeze-dried powder for injection by equilibrium dialysis

作　　者：黄勇[1] 陈慧[1] 何峰[1] 张治蓉[1] 王永林[1] 

机构地区：[1]贵阳医学院药学院,贵州贵阳550004

出　　处：《中国医院药学杂志》2012年第21期1708-1713,共6页Chinese Journal of Hospital Pharmacy

基　　金：国家科技重大专项课题(编号:2008ZX09101-021);国家自然科学基金资助项目(编号:30860366);贵州省科技计划重大专项项目(编号:黔科合重大专项字[2007]6010号)

摘　　要：目的:比较荭草提取物及其复方制剂中两类成分的人血浆蛋白结合率。方法:以超高效液相色谱—质谱联用为检测手段,结合平衡透析法考察单味荭草提取物及注射用复方荭草在人血浆中的蛋白结合率并计算相关参数。结果:在所研究浓度范围内,原儿茶酸与血浆蛋白具有中等强度结合,异荭草素与血浆蛋白结合力较强。经统计分析,两者与血浆蛋白的结合能力在考察浓度范围无显著差异;其中异荭草素指标在复方中的血浆蛋白结合率有所升高,复方中其他的血浆蛋白结合动力学参数相对单味荭草也有一定变化。结论:荭草中化学成分的血浆蛋白结合无浓度依赖性,而在组成复方后某些成分的结合率可能发生改变。OBJECTIVE To determine and compare the plasma protein binding rate of two kinds of compounds in the extraction of Polygonum orientale and compound Hongcao freeze-dried powder for injection by equilibrium dialysis method.METHODS Equilibrium dialysis method combined with liquid chromatography-tandem mass spectrometry（UPLC-ESI-MS/MS） was employed to determine the protein binding rate of protocatechuic acid,isoorientin with human plasma protein both in the extraction of Polygonum orientale and compound Hongcao freeze-dried powder and the binding characteristics were also calculated.RESULTS The results showed medium binding power of protocatechuic acid and high binding power of isoorientin to plasma protein,the powers of the two compounds with the plasma protein were independent on the area of the concentration which was determinate.In the compound Hongcao freeze-dried powder,the related binding characteristics of isoorientin had somewhat increase;and compared with the extraction of Polygonum orientale,there was also some difference.CONCLUSION The protein binding rates of the compounds in the Polygonum orientale were independent on the area of the concentration which was determinate,but there was some change when the herb was composed to compound preparation.

关 键 词：荭草提取物 血浆蛋白结合率 平衡透析法 液质联用 

分 类 号：R969.1[医药卫生—药理学]