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大鼠血浆和组织中高圣草酚-7-O-β-D-吡喃葡萄糖苷的高效液相色谱测定及药代动力学研究

HPLC determination and pharmacokinetic study of homoeriodictyol-7-O-beta-D-glucopyranoside in rat plasma and tissues.

作者信息

Zhao Yunli, Wang Xiaoying, Zhao Yingchun, Gao Xiaoxia, Bi Kaishun, Yu Zhiguo

机构信息

School of Pharmacy, Shenyang Pharmaceutical University, P.R. China.

出版信息

Biol Pharm Bull. 2007 Apr;30(4):617-20. doi: 10.1248/bpb.30.617.

Abstract

Homoeriodictyol-7-O-beta-D-glucopyranoside (HEDT-Glu) was isolated from Viscum coloratum and identified by MS, 1H- and 13C-NMR. A HPLC method was developed for determination of HEDT-Glu in rat plasma and tissues. All biological samples were pretreated by protein precipitation with acetone. Vanillin was selected as internal standard. The mobile phase consisted of methanol-water-glacial acetic acid (45 : 55 : 0.5, v/v/v). Good linearity were observed over the concentration ranges of 0.1-200.0 microg.ml(-1) in rat plasma and 0.05-5.0 microg.ml(-1) in tissues. Both intra- and inter-day precisions of HEDT-Glu, expressed as the relative standard deviation, were less than 13.1%. Accuracy, expressed as the relative error, ranged from -0.8 to 5.4% in plasma and from -5.6 to 9.4% in tissues. The mean extraction recovery of HEDT-Glu was above 73.17% in biological samples. The described assay method was successfully applied to the pre-clinical pharmacokinetic study of HEDT-Glu. After intravenous administration of HEDT-Glu to rat, AUC and CL(tot) were 16.04+/-3.19 microg.h.ml(-1) and 0.85+/-0.17 l.kg(-1).h(-1), respectively. T(1/2,alpha) and t(1/2,beta) were 0.06+/-0.01 h and 1.27+/-0.31 h, respectively. HEDT-Glu was cleared from the blood and mainly distributed to the liver and small intestine.

摘要

从槲寄生中分离得到高圣草素-7-O-β-D-吡喃葡萄糖苷(HEDT-Glu),并通过质谱、1H-和13C-核磁共振进行鉴定。建立了一种高效液相色谱法用于测定大鼠血浆和组织中的HEDT-Glu。所有生物样品均采用丙酮沉淀蛋白进行预处理。选择香草醛作为内标。流动相由甲醇-水-冰醋酸(45 : 55 : 0.5,v/v/v)组成。在大鼠血浆浓度范围为0.1 - 200.0 μg·ml-1和组织浓度范围为0.05 - 5.0 μg·ml-1内观察到良好的线性关系。HEDT-Glu的日内和日间精密度以相对标准偏差表示,均小于13.1%。准确度以相对误差表示,在血浆中为-0.8%至5.4%,在组织中为-5.6%至9.4%。生物样品中HEDT-Glu的平均提取回收率高于73.17%。所描述的分析方法成功应用于HEDT-Glu的临床前药代动力学研究。大鼠静脉注射HEDT-Glu后,AUC和CL(tot)分别为16.04±3.19 μg·h·ml-1和0.85±0.17 l·kg-1·h-1。T(1/2,α)和t(1/2,β)分别为0.06±0.01 h和1.27±0.31 h。HEDT-Glu从血液中清除,主要分布到肝脏和小肠。

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