从鞣酸制备五没食子酰基葡萄糖和液液萃取-反相高效液相色谱法的血浆药代动力学分析。
Preparation of penta-O-galloyl-β-D-glucose from tannic acid and plasma pharmacokinetic analyses by liquid-liquid extraction and reverse-phase HPLC.
机构信息
The Hormel Institute, University of Minnesota, 801 16th Avenue NE, Austin, MN 55912, USA.
出版信息
J Pharm Biomed Anal. 2011 Feb 20;54(3):545-50. doi: 10.1016/j.jpba.2010.09.028. Epub 2010 Sep 29.
Abstract
The gallotannin penta-O-galloyl-beta-D-glucose (PGG) has many biological activities including in vivo anti-cancer efficacy. We present in this paper a scaled-up protocol for its preparation in high purity from tannic acid by acidic methanolysis with typical yield of 15%. We also describe a method for the analysis of PGG in mouse plasma by HPLC and its application in preliminary pharmacokinetic studies. A liquid-liquid extraction (LLE) protocol was optimized for the extraction of PGG from mouse plasma. The extraction efficiency for PGG at 1 μg/mL in mouse plasma was 70.0±1.3% (n=5). The limit of detection (LOD) for PGG was approximately 0.2 μg/mL. Preliminary pharmacokinetic parameters of PGG following a single i.p. injection with 5% ethanol/saline vehicle in mice were established. The peak plasma PGG concentrations (C(max)) were approximately 3-4 μM at a dose of 0.5 mg per mouse (∼20 mg/kg) at 2 h post-injection (T(max)).
摘要
没食子单宁五-O-没食子酰基-β-D-葡萄糖（PGG）具有多种生物活性，包括体内抗癌功效。我们在本文中提出了一种从鞣酸经酸性甲醇解制备高纯度 PGG 的放大方案，典型收率为 15%。我们还描述了一种用于 HPLC 分析小鼠血浆中 PGG 及其在初步药代动力学研究中的应用的方法。优化了一种液-液萃取（LLE）方案，用于从小鼠血浆中提取 PGG。在小鼠血浆中，PGG 在 1μg/mL 时的提取效率为 70.0±1.3%（n=5）。PGG 的检测限（LOD）约为 0.2μg/mL。建立了单次腹腔注射 5%乙醇/盐水载体后 PGG 的初步药代动力学参数。在注射后 2 小时（T(max)），每只小鼠剂量为 0.5 毫克（约 20 毫克/千克）时，血浆 PGG 浓度（C(max)）约为 3-4μM。
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