摘要
目的:建立黄芩素在血浆中的高效液相色谱法检测方法,并研究大鼠灌胃黄芩素后的体内药动学。方法:采用Agi-lent1200高效液相色谱系统,Zorbax SB-C18色谱柱(250mm×4.6mm,5μm),流动相0.1%pH2.0甲酸-乙腈溶液(60:40),流速1.0mL·min-1,进样量20μL,检测波长276nm,室温检测。大鼠按黄芩素75mg.kg-1灌胃给药后,测定给药后不同时间的原型药物和酶解后药物在血浆中的浓度,并用Win Nolin软件计算药动学参数。结果:大鼠灌胃给药后,血浆中酶解后黄芩素总量的AUC0-24和Cmax均显著高于黄芩素原型,前者分别是后者的2.67倍和2.59倍,且黄芩素总量的达峰时间tmax明显迟于黄芩素原型。结果说明,大鼠灌胃给药黄芩素后首过效应严重,大部分在体内被代谢成葡萄糖醛酸、硫酸结合物。无论原型还是Ⅱ相代谢结合物在体内的消除过程都比较缓慢。结论:此方法简便、稳定、准确,可用于黄芩素的体内药动学研究。
OBJECTIVE To establish a HPLC-UV method for the determination of baicalein in blood samples, and to studyits pharmacokinetics after intragastric administration in rats. METHODS Agilent 1200 series HPLC system equipped with 250 minx4. 6 mm Agilent 5 μm Zorbax SB-C18 column and photodiode array detector was used for sample analysis, with mobile phase （buffer solution （Formic acid 0. 1%, pH 2.0）/acetonitrile at 60：40 ratio） running at 1.0 mL·min^-1 at room temperature. The detection wavelength was 276 nm with the injection volume of 20 μL. A dose of 75 mg·kg^-1 baicalein was administrated intragastrically in rats. The blood concentrations of baicalein in free form and after enzymolysis were analyzed by HPLCUV method. The pharmacokinetic parameters of baicalein were calculated by WinNolin software. RESULTS After intragastric administration in rats, the AUC0 24 and Cmax of total baicalein after enzymolysis were 2. 67 times and 2. 59 times than those of the baicalein free form, respectively. Meanwhile, the tmaxof the total baicalein after enzymolysis was obviously longer than that of the baicalein free form, suggesting a relatively slow elimination process. The baicalein glucuronides or sulfates accounted the majority of the total baicalein in the circulation, which maybe attributed to the extensive first-pass metabolism at gut and liver. CONCLUSION The method was convenient, accurate and specific. It was suitable for the study on pharmacokinetics of baiealein in vivo.
出处
《中国医院药学杂志》
CAS
CSCD
北大核心
2010年第22期1901-1905,共5页
Chinese Journal of Hospital Pharmacy
基金
澳门科学技术发展基金(编号:008/2007/A1)
澳门大学科研基金(编号:UL016/09-YZ/MS/WYT01/ICMS)
关键词
黄芩素
药动学
高效液相色谱
首过效应
baicalein
pharmacokinetics
HPLC- UV
first-pass metabolism
