Effect of antacid on the bioavailability of cefprozil

Abstract

The effect of antacid on the bioavailability of cefprozil was investigated in a two-way crossover study. Eight healthy male subjects received a single 500-mg oral dose of cefprozil with and without coadministration of 30 ml of an antacid suspension containing magnesium hydroxide and aluminum hydroxide (Maalox). Cefprozil consists of cis and trans isomers in an approximate 90:10 ratio. When cefprozil was administered alone (treatment A), the mean maximum concentrations (C..,) of the cis and trans isomers were 9.2 and 1.2 ag/ml, respectively. When cefprozil was coadministered with Maalox (treatment B), the Cm.x values of the cis and trans isomers were 8.7 and 1.3 ,g/ml, respectively. The mean values of the area under the curve from time zero to infinity (AUC>.C) were 27.7 and 3.5 ag-h/ml for treatment A and 27.5 and 3.5 pg h/ml for treatment B for the cis and trans isomers, respectively.

Magnesium Hydroxide/Aluminium Hydroxide‐Containing Antacid Does Not Affect the Pharmacokinetics of the Targeted Phosphodiesterase 4 Inhibitor Roflumilast

“…Balanced mixtures of magnesium hydroxide and aluminium hydroxide are widely used as nonprescription antacids for the symptomatic treatment of hyperacidity‐associated gastric symptoms and complications 9 . Antacids are known for their potential to interfere with the absorption of many drugs, including chloroquine, itraconazole, and fluoroquinolone antibiotics 10–17 …”

Lack of Pharmacokinetic Interaction between Linezolid and Antacid in Healthy Volunteers

“…However, the pharmacokinetics of gemifloxacin were only slightly affected and were not significantly affected clinically by the concomitant use of antacids and the proton pump inhibitor omeprazole (1, 2). Antacids also had no effect on the cephalosporins cefopril, cefixime, and cephalexin (16,23), as well as amoxicillin or amoxicillin-clavulanic acid (9,27). A significant reduction of bioavailability was, however, observed for cefpodoxime proxetil after coadministration with antacids or famotidine, an H 2 antagonist (22,26), which was thought to be due to the pH-dependent reduction of tablet disintegration and drug solubility in the gut lumen.…”