Preparation of penta-O-galloyl-β-d-glucose from tannic acid and plasma pharmacokinetic analyses by liquid-liquid extraction and reverse-phase HPLC

Li Li, Ahmad Ali Shaik, Jinhui Zhang, Katai Nhkata, Lei Wang, Yong Zhang, Chengguo Xing, Sung Hoon Kim, Junxuan Lü

Research output: Contribution to journalArticle

35 Scopus citations


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 1μg/mL in mouse plasma was 70.0±1.3% (n=5). The limit of detection (LOD) for PGG was approximately 0.2μg/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 3-4μM at a dose of 0.5mg per mouse (∼20mg/kg) at 2h post-injection (T max).

Original languageEnglish (US)
Pages (from-to)545-550
Number of pages6
JournalJournal of Pharmaceutical and Biomedical Analysis
Issue number3
StatePublished - Feb 20 2011


All Science Journal Classification (ASJC) codes

  • Analytical Chemistry
  • Pharmaceutical Science
  • Drug Discovery
  • Spectroscopy
  • Clinical Biochemistry

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