荆芥内酯大鼠血浆蛋白结合率的测定  

Determination of plasma protein binding rate of schizonepetin in rats

作　　者：刘东亮[1] 耿婷[1] 孙熠[1] 姚卫峰[1] 丁安伟[1,2] 张丽[1] 

机构地区：[1]南京中医药大学,南京210046 [2]江苏省方剂研究重点实验室,南京210046

出　　处：《中国新药杂志》2012年第1期21-25,共5页Chinese Journal of New Drugs

基　　金：国家"重大新药创制"科技重大专项(2009ZX09103-339)

摘　　要：目的:研究荆芥内酯与大鼠血浆蛋白的结合情况。方法:采用平衡透析法测定体外荆芥内酯对大鼠血浆蛋白的结合率,以HPLC法测定透析袋两侧溶液中荆芥内酯的质量浓度,计算其血浆蛋白结合率。结果:荆芥内酯与内标完全分离,血浆中其他成分无干扰,在0.05～50.3μg.mL-1浓度范围内线性关系良好。日内、日间精密度及提取回收率均符合方法学要求。低、中、高(0.08,0.63,6.30μg.mL-1)质量浓度下,荆芥内酯在大鼠血浆中的蛋白结合率分别为(62.23±1.25)%,(62.71±0.04)%和(63.99±0.79)%。结论:该方法操作简便、快速、准确,灵敏度高,能满足生物样品的分析要求。荆芥内酯具有中等强度的蛋白结合率,蛋白结合率与透析液的药物浓度无关。Objective ： To study the plasma rium dialysis was used to determine the in vitro bin prot ding ein binding rate of schizonepetin in rats. Methods：Equilib- rate of schizonepetin to rat plasma. A HPLC method for the determination of schizonepetin was established and then the plasma protein binding rate in rats was calculated. Results：Schizonepetin and internal standard were separated completely with no interference from other ingredients. The calibration curve of schizonepetin was in good linearity over the range of 0.05 - 50.3 μg·mL ^-1 The intra-day and inter-day precision and recovery of schizonepetin met the requirements of methodology. The plasma protein binding rate of schizonepetin at low,middle and high concentrations （0. 08 ,0. 63 ,6. 30μg. mL^-1） were （62.23± 1.25 ） %, （ 62.71 ± 0.04 ） % and （63.99 ±0.79 ） %, respectively. Conclusion ： The method is simple, rapid, accu- rate, and sensitive, and it can meet the requirement for analysis method of biological samples. Schizonepetin has medium plasma protein binding rate in rats,with no significant relation to drug concentrations in dialyzate.

关 键 词：荆芥内酯 蛋白结合率 平衡透析法 高效液相色谱法 

分 类 号：R969.1[医药卫生—药理学]