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2012 (v.20 no.2)

The Journal of Korean Society for Clinical Pharmacology and Therapeutics

Korean Society for Clinical Pharmacology and Therapeutics
ISSN: 1225-5467

  • Targeted Plasma Metabolite Profiling of Metformin in Healthy Korean Volunteers

    Ho-Seob Lihm, Jaemin Cha, Jeong Ju Seo, Jeonghyeon Park, Joomi Lee, Hae Won Lee, Kyun Seop Bae, Woomi Kim, Young-Ran Yoon

    J Korean Soc Clin Pharmacol Ther | v.20, no.2, pp.175-181, Dec, 2012


    Background: Metformin is an effective oral antihyperglycaemic agent for type 2 diabetes mellitus, with
    a variety of metabolic effects. In addition to controlling blood glucose level, it has been appeared to
    decrease the long-period complications of diabetes, including macrovascular disease. Few reports have
    addressed the metabolite profiling of metformin. The study was to evaluate if targeted metabolic profiling
    approach is sensitive enough to predict the therapeutic effects of metformin after a single oral dose.
    Methods: A randomized, open-label, single-dose study was conducted in twenty eight healthy Korean
    male volunteers. To determine the concentrations of endogenous metabolites in their pre-dose and
    post-dose plasma samples, blood samples were collected before and at 2 and 6 h after a single oral dose
    of 500 mg metformin. Both Modular P/Modular D analyzer and ultra-performance liquid chromatography
    tandem mass spectrometry (UPLC-MS/MS)-based metabolic profiling was performed.
    Results: We quantified pre-dose and post-dose creatinine, blood urea nitrogen (BUN), lactic acid, 7
    amino acids (lysine, glutamic acid, alanine, valine, leucine, phenylalanine, tryptophan), and 5
    lysophosphatidylcholines (14:0, 16:0, 17:0, 18:0, and 18:1) using autoanalyser and UPLC-MS/MS. The
    postdose levels of alanine, lactic acid, glutamic acid, lysine, valine, leucine, phenylalanine, tryptophan, and
    lysoPC (18:1) were slightly decreased with statistical significance, but there is no clinical significance.
    Conclusion: In order to explore the potential endogenous metabolites associated with the therapeutic
    effects of metformin, further study including non-targeted (global) metabolite profiling is nee.


    Metformin, Targeted metabolite profiling, UPLC-MS/MS