9-O-小檗碱葡萄糖苷在大鼠体内的药动学研究  

Pharmacokinetic Study of 9-O-glucosyl-berberine in Rats

作　　者：陈竹[1] 曾雪[1] 张保顺[2] 曲中堂[1] 刘应杰[1] 易骏[2] 

机构地区：[1]重庆医药高等专科学校药学系,重庆400030 [2]西南大学药学院,重庆400716

出　　处：《中国药房》2012年第27期2501-2503,共3页China Pharmacy

基　　金：重庆市医学科研计划项目(2011-1-114)

摘　　要：目的:研究9-O-小檗碱葡萄糖苷(BOG)在大鼠体内的药动学参数。方法:采用高效液相色谱法测定大鼠血浆中小檗碱(BBR)、小檗红碱(BRB)、9-O-辛基小檗碱(BOO)、BOG的血药浓度,色谱柱为PREP-ODSC18(250mm×4.6mm,5μm),流动相为乙腈-醋酸缓冲液(醋酸铵7.7g,冰醋酸12mL,以蒸馏水定容至500mL)=40∶60(V/V),流速为1mL·min-1,柱温为室温,检测波长为345nm,进样量为20μL。用PKSolver软件计算药动学参数。结果:各组分分离效果良好,无杂质峰干扰。BBR检测浓度在1.0～75.0μg·L-1范围内与峰面积积分值呈良好线性关系。BOG的口服生物利用度与BBR、BRB、BOO比较有显著提高,BOG的Cmax与AUC0～t分别为BBR的9.3和11.1倍,达到63.438μg·L-1、267.994μg·h·L-1。结论:亲水性糖苷化修饰有助于提高BBR生物利用度。OBJECTIVE： To study the pharmacokinetic parameters of 9-O-glucosyl-berberine （BOG）synthesized by our laborato- ry. METHODS： Berberine, berberrubine, 9-O-octyl-berberine, BOG in rat＇s plasma was determinted by HPLC. The determination was performed on PREP-ODS C18（250 mm×4.6 mm, 5μm） column with mobile phase consisted of acetonitrile-acetic acid buffer so- lution （7.7 gammonium acetate, 12 mL glacial acetic acid, dissolved in 500 mL distilled water）=40：60（V/V） at the flow rate of 1 mL. min^-1, the column temperature was the room temperature. The detection wavelength was set at 345 nm and injection volume was 20 μL. The pharmacokinetic parameters were calculated by PKSolver software. RESULTS： The components were well-separat- ed from other interference components without interference of impurity. The linear range of berberine was 1.0-75.0 pg. L^-1. The bioavailability of 9-O-glucosyl-berberine was increased dramatically, compared with berberine berberrubine and 9-O-octyl-berberine. The Cmax and AUC0-1 of 9-O-glucosyl-berberine were 63.438μg-L^-1 and 267.994 μg·h·L^-1 respectively, 9.3 and 11.1 times higher than those of berberine. CONCLUSION： The trial indicates that hydrophilic glycosylated modification could increase the bioavail- ability of berberine.

关 键 词：小檗碱 9-O-小檗碱葡萄糖苷 药动学 高效液相色谱法 

分 类 号：R284.3[医药卫生—中药学] R969.1[医药卫生—中医学]