The bioavailability of cefpodoxime proxetil tablets relative to an oral solution

Abstract

The bioavailability of cefpodoxime proxetil tablets relative to an oral solution of cefpodoxime proxetil in a sucrose/alcohol/citric acid vehicle was studied in 11 healthy volunteers in a randomized, crossover study. Fasted subjects took one cefpodoxime proxetil 100 mg tablet or 50 mL of a 2 mg mL-1 cefpodoxime proxetil oral solution on two separate occasions. In a third study period, all subjects took a 100 mg dose of the oral solution with a high-fat meal to investigate the effect of food on cefpodoxime proxetil absorption from the oral solution. Serial blood samples were obtained over a 24 h period, and urine was collected for 48 h after dosing. Cefpodoxime concentrations in plasma and in urine were determined using HPLC methods. The bioavailability of cefpodoxime proxetil tablets relative to the oral solution was 82%, as determined from AUC ratios. There was no difference in the rate of cefpodoxime absorption between dosage forms. Food had no effect on the extent of drug absorption from the oral solution but did result in delayed absorption. These results suggest that complete dissolution of cefpodoxime proxetil is critical for optimal bioavailability.

Effect of food on absorption of cefpodoxime proxetil oral suspension in adults

“…This food effect was not associated with meal composition because the increases in cefpodoxime bioavailability were similar in five equicaloric test meals which varied with respect to fat and protein content (8). Administration of a cefpodoxime proxetil oral solution with food had no effect on the extent of drug absorption, suggesting that food may improve drug solubility from the tablet dosage form by facilitating drug dissolution and/or by retaining the tablet in the acidic environment of the stomach, where cefpodoxime proxetil is more soluble and stable (3).…”

“…Blood samples were collected in tubes containing EDTA anticoagulant at zero hour (prior to drug administration) and at 0.25, 0.50, 0.75, 1, 1.5, 2, 2.5, 3,4,6,8,10,12,16,20, and 24 h after dosing. Samples were immediately refrigerated and then were centrifuged at 2,060 ϫ g for 6 min at 4ЊC.…”

Cefpodoxime Proxetil Fast Dissolving Tablets: Comparative Study

“…Cefpodoxime proxetil (CP) is a broad spectrum third-generation cephalosporin, which shows effective antibacterial activity against both gram-positive and gram-negative bacteria. Cefpodoxime proxetil having the low aqueous solubility and also having the low oral bioavailability up to 50% that may have a negative impact on its subtherapeutic plasma drug levels leading to therapeutic failure [8,9]. Consequently, to improve the aqueous solubility and bioavailability of cefpodoxime proxetil, FDTs of cefpodoxime proxetil will be in consideration.…”