THE EFFECT OF COADMINISTRATION OF A COLA BEVERAGE ON THE BIOAVAILABILITY OF ITRACONAZOLE IN PATIENTS WITH ACQUIRED-IMMUNODEFICIENCY-SYNDROME

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 a cquired immunodeficiency syndrome (AIDS). Eighteen men who had been di agnosed with AIDS based on criteria established by the Centers for Dis ease Control and Prevention and a CD4 cell count <300/mu L received si ngle oral doses of itraconazole 200 mg (two 100-mg capsules) with eith er 8 oz of water (ITR/H2O) or 8 oz of a cola beverage (ITR/COLA), Ther e was a 2-week washout period between treatments, Gastric pH was monit ored continuously by pH probe for 6 hours after dosing, Blood samples were taken before itraconazole dosing and for 72 hours postdose; plasm a concentrations of itraconazole and its main active metabolite, hydro xyitraconazole, were determined by using high-performance liquid chrom atography. In the fasted AIDS patients, the bioavailability of itracon azole 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 co ncentration-time curve from 0 to 24 hours increased 55% and 38%, respe ctively, while the mean time to peak plasma concentration decreased by 12%. Results were similar for hydroxyitraconazole. This study demonst rated that the bioavailability of itraconazole is increased in fasted APDS patients when itraconazole is coadministered with a cola beverage .