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

作　　者：杨迪[1] 袁婷婷[2] 干舒蕾 崔亚娇 丁茹[2] 吴玉林[1] 杨劲[2] YANG Di YUAN Tingting GAN Shulei CUI Yajiao DING Ru WU Yulin YANG Jing(School of Basic Medicine and Clinical Pharmacy School of Pharmacy, China Pharmaceutical University, Nanjing 210009, Jiangsu, China)

机构地区：[1]中国药科大学基础医学与临床药学学院 [2]中国药科大学药学院

出　　处：《中国临床药理学与治疗学》2017年第4期394-400,共7页Chinese Journal of Clinical Pharmacology and Therapeutics

基　　金：国家科技重大专项项目(2013ZX09301303001007)

摘　　要：目的:比较研究静脉给药黄芩苷、黄芩素在大鼠体内药代规律。方法:大鼠分别静脉注射等摩尔的黄芩苷、黄芩素,剂量为37μmo L/kg,给药体积为10 m L/kg,于给药后0.08、0.17、0.33、0.5、1、2、4、6、8、10、12和24 h采集血样,用HPLC-MS/MS法同时测定血浆样本中黄芩苷和黄芩素浓度,血药浓度-时间数据及药代参数用BAPP软件进行药代动力学分析。结果:(1)大鼠血浆样本中能同时检测到黄芩苷和黄芩素。黄芩苷组中的原型药物黄芩苷的C_(max)为(24.5±18.3)nmol/m L,AUC_(0-24)为(13.3±11.6)nmol·m L^(-1)·h^(-1),黄芩素组中的原型药物黄芩素C_(max)为(10.5±5.1)nmol/m L,AUC_(0-24)为(18.2±4.9)nmol·m L^(-1)·h^(-1);(2)静脉注射黄芩苷后,代谢转化为黄芩素的转化率为26.5%;静脉注射黄芩素后,代谢转化为黄芩苷的转化率为35%。结论:等摩尔给药情况下黄芩素的C_(max)高于黄芩苷,AUC_(0-24)却相反,这可能是由于黄芩素亲脂性较高,分布较广,清除率较低导致的;提示静脉注射黄芩苷和黄芩素能在体内进行相互转化且黄芩素的转化率高于黄芩苷。AIM： To compare the pharmacoki- netics 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 intrave- nously to rats. In BG group, the Cmax of BG was （24. 5 ± 18. 3） nmol/mL, AUCo.24 was （ 13. 3 ± 11.6） nmol·mL^-1·h^-1 group. In BL group , the Cmas of BL was （ 10.5 ± 5.1 ） nmol/mL, AUC0.24 was（ 18.2 ± 4.9 ） nmol·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 AUG0.24 value was opposite. It might be caused by the higher lipophilicity, the wi- der distribution; the lower clearance rate of baicalein. It is suggested be transformed into that baicalin and baicalein can each other in vivo BL transforming into BG is significantly that of BG transforming into BL. The rate of higher than

关 键 词：黄芩苷 黄芩素 静脉注射 药代动力学 

分 类 号：R965.2[医药卫生—药理学]