中国临床药理学与治疗学2017，Vol.22Issue(4)：394-400,7.
静脉注射黄芩苷、黄芩素在大鼠体内的药代规律比较研究
Comparative study on the pharmacokinetics of baicalin and baicalein in rats after intravenous administration
摘要
Abstract
AIM:To compare the pharmacokinetics of baicalin (BG) and baicalein (BL) in rats by intravenous administration.METHODS:Two groups of rats (5 per group) received an intravenous administration of BG or BL at equimolar dose of 37 μmol/kg and dosing volume of 10 mL/kg.After administration,blood samples were collected in 1.5 mL heparinized polythene tubes,at 0 (pre-dose),0.08,0.17,0.33,0.5,1,2,4,6,8,12,24 h after dosing,simultaneous determination of baicalin and baicalein in plasma by HPLC-MS / MS.RESULTS:BG and BL could be detected in all plasma after baicalein/baicalin was administrated intravenously to rats.In BG group,the Cmax of BG was (24.5 ± 18.3) nmol/mL,AUC0-24 was (13.3 ±11.6)nmol · mL-1 · h1 group.In BL group,the Cmax of BL was (10.5 ± 5.1) nmol/mL,AUC0-24 was (18.2±4.9)nmol · mL1 · h-1.The rate of BG transformed into BL was 26.5％ in the BG group.The rate of BL transformed into BG was 35％.CONCLUSION:The Cmax of BL in BL group was significantly higher than that of BG in BG group after intravenous administration of equimolar dose of BG/BL;however,the AUC0-24 value was opposite.It might be caused by the higher lipophilicity,the wider distribution;the lower clearance rate of baicalein.It is suggested that baicalin and baicalein can be transformed into each other in vivo.The rate of BL transforming into BG is significantly higher than that of BG transforming into BL.关键词
黄芩苷/黄芩素/静脉注射/药代动力学Key words
baicalein/baicalin/intravenous administration/pharmacokinetic分类
医药卫生引用本文复制引用
杨迪,袁婷婷,干舒蕾,崔亚娇,丁茹,吴玉林,杨劲..静脉注射黄芩苷、黄芩素在大鼠体内的药代规律比较研究[J].中国临床药理学与治疗学,2017,22(4):394-400,7.基金项目
国家科技重大专项项目(2013ZX09301303001007) （2013ZX09301303001007）
