水荭花提取物的药动学特性及绝对生物利用度研究  

Pharmacokinetics and absolute bioavailability of Polygonum orientale L. flower extract

作　　者：谢玉敏[1,2,3] 梅朝叶 陈浩[1,2] 李月婷[1,2] 兰燕宇[1,4] 郑林[1,2] 

机构地区：[1]贵州医科大学药学院,贵阳550004 [2]贵州医科大学贵州省药物制剂重点实验室,贵阳550004 [3]国家苗药工程技术研究中心,贵阳550004 [4]贵州医科大学,民族药与中药开发应用教育部工程研究中心,贵阳550004

出　　处：《中国抗生素杂志》2017年第7期611-615,共5页Chinese Journal of Antibiotics

基　　金：国家自然科学基金(No.81360664和No.81560630);贵州省研究生卓越人才计划项目(黔教研合ZYRC字[2014]012);贵州省科学技术厅人才团队项目(黔科合平台人才[2016]5613\5677);贵州省科技计划项目(黔科合平台人才[2017]5601)

摘　　要：目的为建立血浆中原儿茶酸,山柰素-鼠李糖苷的UPLC-MS/MS分析方法,研究两个指标成分的药动学特征及其绝对生物利用度。方法采用UPLC-MS/MS检测大鼠口服及静注给予水荭花提取物后的血药浓度,利用DAS 2.0软件计算药动学参数及绝对生物利用度。结果口服水荭花提取物后,原儿茶酸、山柰素-鼠李糖苷在大鼠体内半衰期分别为(8.3±2.9)和(15.9±6.9)h,达峰浓度分别为(386.3±56.7)和(98.0±13.7)ng/m L;静注水荭花提取物后,原儿茶酸、山柰素-鼠李糖苷在大鼠体内半衰期分别为(41.9±12.3)和(108.2±96.5)min,达峰浓度分别为(1.7±0.7)和(9.5±3.6)μg/m L;原儿茶酸、山柰素-鼠李糖苷在大鼠体内的绝对生物利用度分别为2.5%和0.30%。结论所建立的UPLC-MS/MS检测方法能特异、快速、准确且灵敏地同时测定生物样品中原儿茶酸,山柰素-鼠李糖苷的血药浓度;两个成分不同给药途径下药动学参数存在一定差异且生物利用度低。Objective To establish a UPLC-MS/MS method for the determination of protocatechuie acid and kaempferol-3-O-α-L-rhamnosid, and to study their pharmacokinetics and absolute bioavailability in rats. Methods Based on the UPLC-MS/MS method, the absolute bioavailability was calculated by DAS 2.0 after intravenous injection or oral administration of Polygonum orientale L. flower extract in rats. Results The results showed that the t1/2 ofprotocatechuie acid and kaempferol-3-O-α-L-rhamnosid after oral administration and intravenous injection were （8.3±2.9）h, （15.9±6.9）h and （41.9±12.3）min, （108.2±96.5）min, respectively. The Cmax were （386.3±56.7）ng/mL, （98.0±13.7）ng/mL and （1.7±0.7）μg/mL, （9.5±3.6）μg/mL. The absolute bioavailability were 2.5% and 0.30%, respectively. Conclusion The developed method is simple, rapid, sensitive enough and has been successfully applied to the pharmacokinetic study. There exist some differences in the pharmacokinetie parameters after oral administration and intravenous injection, and the absolute bioavailability of the compounds is low.

关 键 词：大鼠 药动学 水荭花 UPLC-MS/MS 绝对生物利用度 

分 类 号：R9[医药卫生—药学]