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Research ArticleArticle

HEPATOBILIARY EXCRETION OF BERBERINE

Pi-Lo Tsai and Tung-Hu Tsai
Drug Metabolism and Disposition April 2004, 32 (4) 405-412; DOI: https://doi.org/10.1124/dmd.32.4.405
Pi-Lo Tsai
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Tung-Hu Tsai
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Abstract

Berberine is a bioactive herbal ingredient isolated from the roots and bark of Berberis aristata or Coptis chinensis. To investigate the detailed pharmacokinetics of berberine and its mechanisms of hepatobiliary excretion, an in vivo microdialysis coupled with high-performance liquid chromatography was performed. In the control group, rats received berberine alone; in the drug-treated group, 10 min before berberine administration, the rats were injected with cyclosporin A (CsA), a P-glycoprotein (P-gp) inhibitor; quinidine, both organic cation transport (OCT) and P-gp inhibitors; SKF-525A (proadifen), a cytochrome P450 inhibitor; and probenecid to inhibit the glucuronidation. The results indicate that berberine displays a linear pharmacokinetic phenomenon in the dosage range from 10 to 20 mg kg-1, since a proportional increase in the area under the concentration-time curve (AUC) of berberine was observed in this dosage range. Moreover, berberine was processed through hepatobiliary excretion against a concentration gradient based on the bile-to-blood distribution ratio (AUCbile/AUCblood); the active berberine efflux might be affected by P-gp and OCT since coadministration of berberine and CsA or quinidine at the same dosage of 10 mg kg-1 significantly decreased the berberine amount in bile. In addition, berberine was metabolized in the liver with phase I demethylation and phase II glucuronidation, as identified by liquid chromatography/tandem mass spectrometry. Also, the phase I metabolism of berberine was partially reduced by SKF-525A treatment, but the phase II glucuronidation of berberine was not obviously affected by probenecid under the present study design.

Footnotes

  • ↵1 Abbreviations used are: P-gp, P-glycoprotein; HPLC, high-performance liquid chromatography; SKF-525A, proadifen; CsA, cyclosporin A; LC/MS-MS, liquid chromatography/tandem mass spectrometry; ESI, electrospray ionization; AUC, area under the concentration-time curve; CL, clearance; PSC 833, valspodar; MRP2, multidrug resistance-associated protein 2.

  • This study was supported in part by research grants (NSC92-2113-M-077-005; NSC92-2320-B-077-004) from the National Science Council, Taiwan.

    • Received June 19, 2003.
    • Accepted December 23, 2003.
  • The American Society for Pharmacology and Experimental Therapeutics
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Drug Metabolism and Disposition: 32 (4)
Drug Metabolism and Disposition
Vol. 32, Issue 4
1 Apr 2004
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Research ArticleArticle

HEPATOBILIARY EXCRETION OF BERBERINE

Pi-Lo Tsai and Tung-Hu Tsai
Drug Metabolism and Disposition April 1, 2004, 32 (4) 405-412; DOI: https://doi.org/10.1124/dmd.32.4.405

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Research ArticleArticle

HEPATOBILIARY EXCRETION OF BERBERINE

Pi-Lo Tsai and Tung-Hu Tsai
Drug Metabolism and Disposition April 1, 2004, 32 (4) 405-412; DOI: https://doi.org/10.1124/dmd.32.4.405
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