摘要：药物小分子和血浆蛋白结合的试验，不仅对药物和蛋白结合的定性定量方面都提供了重要的资料，并且对新药开发都具有非常重要的意义。本次实验运用了高效液相色谱法和超滤法来分析研究中药中橙皮苷与血浆蛋白的结合作用。为了研究橙皮苷和血浆蛋白的结合，实验分别建立了用高效液相色谱测定方法来测定大白鼠血浆中橙皮苷的游离浓度。橙皮苷在0.232μg/mL—11.6μg/mL范畴内线性关系良好，此外日内精密度都小于2%，可用来分析与研究橙皮苷与血浆蛋白的结合。橙皮苷与大白鼠的血浆蛋白的结合率是用超滤法测得，其结合率为73.98%—35.09%，结果表明随着橙皮苷浓度的增加，橙皮苷与血浆蛋白的结合作用逐渐降低，说明橙皮苷与血浆蛋白结合呈现浓度依赖性。以上结果为阐明橙皮苷的药物代谢动力学处置过程和其药效效果分析研究提供依据。68788

毕业论文关键词： 橙皮苷；药物血浆蛋白结合；超滤法

The study of the binding of plasma protein to effective ingredients of traditional Chinese medicine

Abstract:The in vitro experiment of the plasma protein binding to drug molecules provides important information on qualitative and quantitative aspects,furthermore it has important significance to drug development.This experiment use high performance liquid chromatography (HPLC) and ultrafiltration method to analyze the binding effect of hesperidin in traditional Chinese medicine to plasma protein.In order to study the binding effect of hesperidin and plasma protein, we established HPLC to analyze the free concentration of hesperidin in rat plasma.The linearity of hesperidin in the range of 0.232μg / ml-11.6μg / ml is good, and the within-day precision is less than 2%.Both linearity and within-day precision can be used to analyze the binding of hesperidin to plasma proteins.The binding ratio of hesperidin to rat plasma protein is measured by ultrafiltration method, the binding rate is 73.98% -35.09%.The results shows that the combination of hesperidin and plasma protein decreased gradually with the increasing of hesperidin concentration, which indicated that the binding of plasma protein and hesperidin is concentration-dependent.These result provide the basis to hesperidin’s drug metabolism kinetics of disposal process and their pesticide effect research.

KeyWords: hesperidin；drug-plasma protein binding；Chinese medicine；ultrafiltration

目录

1 引言 5

1.1 论文的目的和意义 5

1.2海内外研究近况、水平和发展趋向 6

1.2.1 药物血浆蛋白结合与药效相关性 6

1.2.2 药物血浆蛋白结合与药代动力学的关系 7

1.2.3 药物与血浆蛋白的结合 7

1.2.4 药物与血浆蛋白结合作用研究方法 8

1.2.5 橙皮苷的研究概况 13

1.3 本论文拟解决的问题 14

2 橙皮苷-血浆蛋白结合率测定 15

2.1 概述 15

2.2 仪器和试剂 16

2.2.1  仪器 16

2.2.2  试剂 16

2.3 实验方法 17

2.3.1  色谱条件 17

2.3.2  Sorenson缓冲溶液的配制 17

2.3.3  橙皮苷标准品储备液的配制