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Effect of Quercetin on the Plasma and Intracellular Concentrations of Saquinavir in Healthy Adults
Author(s) -
DiCenzo Robert,
Frerichs Valerie,
Larppanichpoonphol Panupong,
Predko Lisa,
Chen Amy,
Reichman Richard,
Morris Marilyn
Publication year - 2006
Publication title -
pharmacotherapy: the journal of human pharmacology and drug therapy
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 1.227
H-Index - 109
eISSN - 1875-9114
pISSN - 0277-0008
DOI - 10.1592/phco.26.9.1255
Subject(s) - saquinavir , confidence interval , dosing , pharmacokinetics , quercetin , geometric mean , medicine , pharmacology , chemistry , biochemistry , immunology , mathematics , viral load , statistics , human immunodeficiency virus (hiv) , antiretroviral therapy , antioxidant
Study Objectives . To determine if quercetin, a bioflavonoid that inhibits p‐glycoprotein, alters plasma saquinavir concentrations, and to explore the potential influence on intracellular concentrations. Design . Prospective pharmacokinetic analysis. Setting . University‐affiliated general clinical research center. Subjects . Ten healthy adults (four women, six men) with a mean ± SD age of 30.7 ± 9.4 years. Intervention . All subjects received saquinavir 1200 mg 3 times/day with food on days 1–11 and quercetin 500 mg 3 times/day with food on days 4–11. Measurements and Main Results . On days 4 and 11, nine blood samples and four peripheral blood mononuclear cell samples were drawn during a steady‐state dosing interval. Pharmacokinetic parameters were calculated by using standard noncompartmental techniques. Plasma saquinavir concentrations were similar regardless of quercetin administration. Geometric mean ratios for the area under the concentration‐time curve during an 8‐hour dosing interval (AUC 0–8 ), maximum concentration in the dosing interval, and minimum concentration in the dosing interval were 0.99 (95% confidence interval [CI] 0.65–1.50), 0.99 (95% CI 0.64–1.54), and 1.06 (95% CI 0.68–1.67), respectively. Intracellular saquinavir concentrations displayed substantial intra‐ and intersubject variability, which limited the ability to determine the influence of quercetin coadministration (geometric mean ratio for AUC 0–8 = 0.51 [95% CI 0.14–1.95], six patients). Conclusion . Quercetin coadministration did not influence plasma saquinavir concentrations. Because of substantial inter‐ and intrasubject variability, more study is necessary to determine if saquinavir intracellular concentrations are altered by coadministration of quercetin.