HPLC-荧光法测定大鼠血浆中4种蒽醌类成分及其药代动力学研究  

Simultaneous determination of four anthraquinones in rat plasma by HPLC-FLD method and its pharmacokinetic study

作　　者：黄金秋[1] 严雪梅[1] 冯芳[1,2] 

机构地区：[1]中国药科大学药物分析教研室,江苏南京210009 [2]中国药科大学药物质量与安全预警教育部重点实验室,江苏南京210009

出　　处：《中国中药杂志》2014年第19期3850-3854,共5页China Journal of Chinese Materia Medica

基　　金：国家自然科学基金项目(81274063)

摘　　要：建立大鼠灌服栀子大黄汤后血浆中芦荟大黄素、大黄酸、大黄酚、大黄素甲醚的测定方法并考察4种蒽醌类成分在大鼠体内的药动学行为。采用HPLC-荧光法测定大鼠血浆中4种蒽醌的血药浓度,血浆样品通过液液萃取法进行处理。Phecda C18色谱柱(4.6 mm×150 mm,5μm),流动相0.2%乙酸-甲醇,梯度洗脱,流速1.0 m L·min-1。激发和发射波长分别为430,525 nm,采用DAS 2.0软件对所得的血药浓度进行拟合,求算相应的药动学参数。结果显示4种蒽醌类成分均可被吸收进入体内。大鼠血浆中芦荟大黄素,大黄酸,大黄酚,大黄素甲醚的Cmax分别为(0.085±0.058),(3.772±1.152),(0.464±0.267),(0.028±0.008)mg·L-1;tmax分别为(1.042±0.510),(0.805±0.307),(1.167±0.283),(0.616±0.162)h;t1/2分别为(3.557±1.250),(6.879±1.126),(5.196±2.032),(4.337±1.816)h;AUC0-t分别为(0.504±0.130),(9.558±1.106),(2.545±1.554),(0.052±0.018)mg·h·L-1。该研究建立了一种专属性强,准确度高,灵敏度好的HPLC-荧光法,可适用于4种蒽醌成分的体内浓度测定。This paper aims to develop a method for the determination of aloe-emodin, rhein, chrysophanol and physcion and study the pharmacokinetic properties of four anthraquinones in rat plasma after oral administration of gardenia and rhubarb decoction. The plasma concentrations at different time points of four anthraquinones were determined by HPLC-FLD method. Plasma samples were extracted with liquid-liquid extraction procedure. Plasma samples were separated on a Cls column （4. 6 mm × 150 mm, 5 μm）, using 0. 2% acetic acid and methanol as mobile phase at a flow rate of 1.0 mL min^-1 with gradient elution. The excitation and emission wavelengths were set at 430, 525 nm, respectively. DAS 2.0 software was applied to calculate the pharmacokinetic parameters. The results showed four anthraquinones can be absorbed. The main parameters of aloe-emodin, rhein, chrysophanol and physcion were as follows： Cmax for aloe-emodin was （0. 085 ±0. 058）, （3. 772 ±1. 152）, （0. 464 ±0. 267）, （0. 028 ±0. 008） mg · L-1 respectively; tmax for rhein was （1. 042 ±0. 510）, （0. 805 ±0. 307）, （1. 167 ±0. 283）, （0. 616 ±0. 162） h respectively; t1/2 for chrysophanol was （3. 557 ± 1. 250）, （6. 879 ±1. 126）, （5. 196 ±2. 032）, （4. 337 ±1. 816） h; AUC0-t for physcion was （0. 504 ±0. 130）, （9. 558 ±1. 106）, （2. 545 ±1. 554）, （0. 052 ±0. 018） mg · h · L^-1. This paper developed a selective, accurate and sensitive HPLC-FLD method for the simultaneous determination of four anthraquiones in rat plasma.

关 键 词：栀子大黄汤 蒽醌 HPLC-荧光法 药代动力学 

分 类 号：R285.5[医药卫生—中药学]