不同剂量西瑞香素及其代谢产物在大鼠尿中的排泄  

Urinary Excretion of Daphnoretin and its Metabolite at Different Doses in Rats

作　　者：高金薇[1,2] 王小波[1] 王彩芬[1] 崔钰琪 佟立今[1] 孙立新[1] 

机构地区：[1]沈阳药科大学药学院,沈阳110016 [2]沈阳药科大学中药学院,沈阳110016

出　　处：《中国实验方剂学杂志》2014年第3期99-103,共5页Chinese Journal of Experimental Traditional Medical Formulae

基　　金：国家"十一五""重大新药创制"科技重大专项(2009ZX09301-012);辽宁省高校创新团队支持计划项目(LT 2021018)

摘　　要：目的:研究不同剂量西瑞香素及其葡萄糖醛酸化代谢产物在大鼠尿中的排泄动力学。方法:将西瑞香素制成混悬液,按50,100,200 mg·kg-1给大鼠灌胃,于灌胃后不同时间收集尿液,用β-葡糖醛酸苷酶溶液处理尿液。采用高效液相色谱法测定尿液中西瑞香素及其葡萄糖醛酸化代谢产物的浓度。结果:50,100,200 mg·kg-13种给药剂量时,累积经尿液排泄的原形药物量为(23.13±2.36),(41.74±2.02)和(80.01±3.21)μg,累积经尿液排泄的葡萄糖醛酸结合形药物为(37.51±4.51),(61.17±3.90)和(131.25±13.85)μg。结论:西瑞香素在大鼠尿液中葡萄糖醛酸化代谢产物的排泄量大于原形排泄量,原形及其葡萄糖醛酸化代谢产物的排泄呈现明显的剂量依赖性特征。Objective： To study the urinary excretion of daphnoretin and glucuronidated daphnoretin in rats. Method： Suspended in solution, daphnoretin was orally administered to rats at the dose of 50, 100, 200 mg-kg-1. At various time intervals, the urine was collected. The urine was treated with β-glucuronidase. The daphnoretin in urine was extracted by acetic ether. The organic phase was removed into the tubes and then dried in pressure blowing concentrator. The residue was dissolved in 200 μL of mobile phase. The solution of 20 μL was drawn and detected by high-perormance liquid chromatography. Result： The cumulative urine excretion of daphnoretin was （23.13±2.36）, （41.74±2.02） and （80.01±3.21） μg at the dose of 50, 100, 200 mg.kg-1, respectively. The cumulative urine excretion of glueuronidated daphnoretin was （37.51 ± 4.51 ） , （61.17 ± 3.90） and （131.25 ± 13.85） μg at the dose of 50, 100, 200 mg .kg-1, respectively. Conclusion： The cumulative urine excretion of glucuronidated daphnoretin is more than cumulative urine excretion of daphnoretin. The daphnoretin and glueuronidated daphnoretin are excreted in the manner of linear dose-dependent.

关 键 词：西瑞香素 尿排泄 葡萄糖醛酸 高效液相色谱 

分 类 号：R284.1[医药卫生—中药学] R285.5[医药卫生—中医学]