大鼠体内泻心汤蒽醌类成分尿排泄动力学研究

Urinary pharmacokinetics of five anthraquinones after oral administration of Xiexin Decoction in rats

目的:研究泻心汤(大黄、黄连、黄芩)中蒽醌类成分在大鼠体内尿排泄动力学规律。方法:建立大鼠尿中芦荟大黄素、大黄酸、大黄素、大黄酚、大黄素甲醚高效液相色谱(HPLC-FLD)测定方法。大鼠灌胃给予泻心汤12 g/kg,药前及药后不同时间采集尿样,用HPLC-FLD法分析尿中蒽醌类成分,测定5种蒽醌类成分经时变化,根据尿排泄量-时间数据计算排泄动力学参数。结果:大鼠灌胃给予泻心汤后,芦荟大黄素、大黄酸、大黄素、大黄酚、大黄素甲醚均从肾脏经尿液排泄;排泄T1/2分别为: (3. 46±1. 18)h, (3. 24±0. 60)h, (4. 69±1. 99)h, (4. 49±1. 63)h, (5. 65±1. 74)h; 48 h累积排泄量分别为: (11. 28±4. 30)μg, (116. 73±17. 46)μg, (5. 48±2. 92)μg, (9. 53±2. 67)μg, (0. 41±0. 20)μg。结论:泻心汤中5种蒽醌类成分均可从尿中排泄,尿中排泄量占给药量均<10%。

AIM ： To study the urinary pharmacokinetics of five anthraquinones after oral administration of Xiexin Decoction （Radix et Rhizoma rhei, Rhizoma coptidis and Radix scutellariae） in rats. METHODS： A high-performance liquid chromatographic method with fluorescence detection （HPLC-FLD） was established and validated the quantification for five anthraquinones （aloe-emodin, rhein, emodin, chrysophanol and physcion） in rat urine. SD rats were given 12 g/kg of Xiexin Decoction. Urine was collected before and after perfusion. Anthraquinones components in urine were measured by HPLC-FLD. Urinary pharmacokinetic parameters were determined according to urinary output-time data. RESULTS： After oral administration of Xiexin Decoction all the five anthraquinones were excreted from the urine. The excretion T1/2 of aloe-emodin, rhein, emodin, ehrysophanol and physcion were 3.46 ± 1.18, 3.24 ±0.60, 4.69 ± 1.99, 4.49 ± 1.63, 5.65 ± 1.74 h, respectively. The amounts of aloe-emodin, rhein, emodin, ehrysophanol and physcion excreted from urine during 0 - 48 h were （ 11.28 ± 4.30） μg, （ 116.73 ± 17.46） μg, （5.48 ± 2.92） μg, （9.53 ± 2.67 ） μg, （0- 41 ± 0.20） μg, respectively. CONCLUSION： After oral administration of Xiexin Decoction five anthraquinones were excreted from urine and a small quantity of five anthraquinones excreted from urine in rats is less than 10% of oral dose.