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用一种简单的高效液相色谱 - 紫外检测法测定大鼠血浆中的紫檀芪及其在临床前药代动力学研究中的应用。

Determination of pterostilbene in rat plasma by a simple HPLC-UV method and its application in pre-clinical pharmacokinetic study.

作者信息

Lin Hai-Shu, Yue Bing-De, Ho Paul C

机构信息

Department of Pharmacy, National University of Singapore, Singapore.

出版信息

Biomed Chromatogr. 2009 Dec;23(12):1308-15. doi: 10.1002/bmc.1254.

Abstract

A simple HPLC-UV method was developed and validated for the quantification of pterostilbene (3,5-dimethoxy-4'-hydroxy-trans-stilbene), a pharmacologically active phytoalexin in rat plasma. The assay was carried out by measuring the UV absorbance at 320 nm. Pterostilbene and the internal standard, 3,5,4'-trimethoxy-trans-stilbene eluted at 5.7 and 9.2 min, respectively. The calibration curve (20-2000 ng/mL) was linear (R(2)> 0.997). The lower limits of detection and of quantification were 6.7 and 20 ng/mL, respectively. The intra- and inter-day precisions in terms of RSD were all lower than 6%. The analytical recovery ranged from 95.5 +/- 3.7 to 103.2 +/- 0.7% while the absolute recovery ranged from 101.9 +/- 1.1 to 104.9 +/- 4.4%. This simple HPLC method was subsequently applied in a pharmacokinetic study carried out in Sprague-Dawley rats. The terminal elimination half-life and clearance of pterostilbene were 96.6 +/- 23.7 min and 37.0 +/- 2.5 mL/min/kg, respectively, while its absolute oral bioavailability was 12.5 +/- 4.7%. Pterostilbene appeared to have better pharmacokinetic characteristics than its natural occurring analog, resveratrol.

摘要

开发并验证了一种简单的高效液相色谱 - 紫外(HPLC - UV)方法,用于定量测定大鼠血浆中具有药理活性的植物抗毒素紫檀芪(3,5 - 二甲氧基 - 4'- 羟基 - 反式芪)。该测定通过测量320 nm处的紫外吸光度进行。紫檀芪和内标3,5,4'- 三甲氧基 - 反式芪分别在5.7分钟和9.2分钟洗脱。校准曲线(20 - 2000 ng/mL)呈线性(R(2)> 0.997)。检测限和定量下限分别为6.7 ng/mL和20 ng/mL。日内和日间精密度的相对标准偏差(RSD)均低于6%。分析回收率在95.5 +/- 3.7%至103.2 +/- 0.7%之间,而绝对回收率在101.9 +/- 1.1%至104.9 +/- 4.4%之间。这种简单的HPLC方法随后应用于在Sprague - Dawley大鼠中进行的药代动力学研究。紫檀芪的末端消除半衰期和清除率分别为96.6 +/- 23.7分钟和37.0 +/- 2.5 mL/min/kg,而其绝对口服生物利用度为12.5 +/- 4.7%。紫檀芪似乎比其天然类似物白藜芦醇具有更好的药代动力学特征。

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