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.
出处
《中国抗生素杂志》
CAS
CSCD
北大核心
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)
