The effect of coadministration of a cola beverage on the bioavailability of itraconazole in patients with acquired immunodeficiency syndrome

Abstract

This open-label, randomized, two-way crossover study was conducted to determine whether coadministration of an acidic beverage would affect the bioavailability of itraconazole capsules in fasted patients with acquired immunodeficiency syndrome (AIDS). Eighteen men who had been diagnosed with AIDS based on criteria established by the Centers for Disease Control and Prevention and a CD4 cell count <300/μL received single oral doses of itraconazole 200 mg (two 100-mg capsules) with either 8 oz of water (ITR/H 2O) or 8 oz of a cola beverage (ITR/COLA). There was a 2-week washout period between treatments. Gastric pH was monitored continously by pH probe for 6 hours after dosing. Blood samples were taken before itraconazole dosing and for 72 hours postdose; plasma concentrations of itraconazole and its main active metabolite, hydroxyitraconazole, were determined by using high-performance liquid chromatography. In the fasted AIDS patients, the bioavailability of itraconazole was enhanced by the coadministration of a cola beverage compared with coadministration of itraconazole and water; the mean values for peak plasma concentration of the drug and the area under the plasma concentration—time curve from 0 to 24 hours increased 55% and 38%, respectively, while the mean time to peak plasma concentration decreased by 12%. Results were similar for hydroxyitraconazole. This study demonstrated that the bioavailability of itraconazole is increased in fasted AIDS patients when itraconazole is coadministered with a cola beverage.