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Research ArticleArticle

Hydrastine Pharmacokinetics and Metabolism after a Single Oral Dose of Goldenseal (Hydrastis canadensis) to Humans

Prem K. Gupta, Gary Barone, Bill J. Gurley, E. Kim Fifer and Howard P. Hendrickson
Drug Metabolism and Disposition April 2015, 43 (4) 534-552; DOI: https://doi.org/10.1124/dmd.114.059410
Prem K. Gupta
Department of Pharmaceutical Sciences, College of Pharmacy (P.K.G., B.J.G., E.K.F., H.P.H.), and Department of Surgery, College of Medicine (G.B.), University of Arkansas for Medical Sciences, Little Rock, Arkansas
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Gary Barone
Department of Pharmaceutical Sciences, College of Pharmacy (P.K.G., B.J.G., E.K.F., H.P.H.), and Department of Surgery, College of Medicine (G.B.), University of Arkansas for Medical Sciences, Little Rock, Arkansas
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Bill J. Gurley
Department of Pharmaceutical Sciences, College of Pharmacy (P.K.G., B.J.G., E.K.F., H.P.H.), and Department of Surgery, College of Medicine (G.B.), University of Arkansas for Medical Sciences, Little Rock, Arkansas
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E. Kim Fifer
Department of Pharmaceutical Sciences, College of Pharmacy (P.K.G., B.J.G., E.K.F., H.P.H.), and Department of Surgery, College of Medicine (G.B.), University of Arkansas for Medical Sciences, Little Rock, Arkansas
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Howard P. Hendrickson
Department of Pharmaceutical Sciences, College of Pharmacy (P.K.G., B.J.G., E.K.F., H.P.H.), and Department of Surgery, College of Medicine (G.B.), University of Arkansas for Medical Sciences, Little Rock, Arkansas
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Abstract

The disposition and metabolism of hydrastine was investigated in 11 healthy subjects following an oral dose of 2.7 g of goldenseal supplement containing 78 mg of hydrastine. Serial blood samples were collected for 48 hours, and urine was collected for 24 hours. Hydrastine serum and urine concentrations were determined by Liquid Chromatography-tandem mass spectrometry (LC-MS/MS). Pharmacokinetic parameters for hydrastine were calculated using noncompartmental methods. The maximal serum concentration (Cmax) was 225 ± 100 ng/ml, Tmax was 1.5 ± 0.3 hours, and area under the curve was 6.4 ± 4.1 ng⋅h/ml⋅kg. The elimination half-life was 4.8 ± 1.4 hours. Metabolites of hydrastine were identified in serum and urine by using liquid chromatography coupled to high-resolution mass spectrometry. Hydrastine metabolites were identified by various mass spectrometric techniques, such as accurate mass measurement, neutral loss scanning, and product ion scanning using Quadrupole-Time of Flight (Q-ToF) and triple quadrupole instruments. The identity of phase II metabolites was further confirmed by hydrolysis of glucuronide and sulfate conjugates using bovine β-glucuronidase and a Helix pomatia sulfatase/glucuronidase enzyme preparation. Hydrastine was found to undergo rapid and extensive phase I and phase II metabolism. Reduction, O-demethylation, N-demethylation, hydroxylation, aromatization, lactone hydrolysis, and dehydrogenation of the alcohol group formed by lactone hydrolysis to the ketone group were observed during phase I biotransformation of hydrastine. Phase II metabolites were primarily glucuronide and sulfate conjugates. Hydrastine undergoes extensive biotransformation, and some metabolites may have pharmacological activity. Further study is needed in this area.

Footnotes

    • Received July 9, 2014.
    • Accepted January 20, 2015.
  • dx.doi.org/10.1124/dmd.114.059410.

  • Copyright © 2015 by The American Society for Pharmacology and Experimental Therapeutics
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Drug Metabolism and Disposition: 43 (4)
Drug Metabolism and Disposition
Vol. 43, Issue 4
1 Apr 2015
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Research ArticleArticle

Hydrastine ADME in Humans after a Single Dose of Goldenseal

Prem K. Gupta, Gary Barone, Bill J. Gurley, E. Kim Fifer and Howard P. Hendrickson
Drug Metabolism and Disposition April 1, 2015, 43 (4) 534-552; DOI: https://doi.org/10.1124/dmd.114.059410

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Research ArticleArticle

Hydrastine ADME in Humans after a Single Dose of Goldenseal

Prem K. Gupta, Gary Barone, Bill J. Gurley, E. Kim Fifer and Howard P. Hendrickson
Drug Metabolism and Disposition April 1, 2015, 43 (4) 534-552; DOI: https://doi.org/10.1124/dmd.114.059410
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