Robert A. Blum, PharmD; David T. D'Andrea; Becky M. Florentino, BA; John H. Wilton, PhD; Donald M. Hilligoss, PharmD; Mark J. Gardner, PhD; Eugenia B. Henry, PhD; Harvey Goldstein, MD; Jerome J. Schentag, PharmD
Blum RA, D'Andrea DT, Florentino BM, Wilton JH, Hilligoss DM, Gardner MJ, et al. Increased Gastric pH and the Bioavailability of Fluconazole and Ketoconazole. Ann Intern Med. 1991;114:755-757. doi: 10.7326/0003-4819-114-9-755
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Published: Ann Intern Med. 1991;114(9):755-757.
Two orally active antifungal agents are currently available, ketoconazole and fluconazole. However, the absorption of ketoconazole depends on gastric pH for tablet disintegration and dissolution (1, 2). Reduced serum concentrations of ketoconazole have been reported in patients with achlorhydria and in patients receiving concomitant treatment with antacids or cimetidine (1-3). Our study was done to determine the effects of cimetidine-induced increases in gastric pH on the relative bioavailability of fluconazole and ketoconazole.
Twenty-four healthy male volunteers, 19 to 43 years of age, gave written informed consent to participate in the study. The study protocol was approved by the
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