Effects of Sucralfate, Magnesium Oxide and Sodium Ferrous Citrate on Sparfloxacin Pharmacokinetics.

Abstract

The effects of sucralfate, magnesium oxide and sodium ferrous citrate on the pharmacokinetics of sparfloxacin were studied in 6 healthy subjects. According to a four-way crossover design, each subject received the following drug combinations in a random order : (A) a single 200 mg dose of sparfloxacin alone ; (B) a single 200 mg dose of sparfloxacin with a 900 mg dose of sucralfate ; (C) a single 200 mg dose of sparfloxacin with a 1 g dose of magnesium oxide ; (D) a single 200 mg dose of sparfloxacin with a 100 mg dose of sodium ferrous citrate. The four regimens were given to subjects in the fasting state. Blood samples were collected over a 24- hour period, and plasma concentrations of sparfloxacin were determined by high-performance liquid chromatography. The area under the curve from 0 to 24 hours (AUC0-24) for sparfloxacin for regimen B was significantly lower (52.9% less, p<0.005) than that for regimen A. However, for regimens C and D, the reductions in AUC0-24 as compared with regimen A were not significant (19.4% and 28.2%, respectively). Also, the peak plasma concentrations (Cmax) of sparfloxacin for regimens B and D were significantly lower (54.7 % less, p< 0.001 and 31.4% less, p<0.05, respectively) than that for regimen A. However, the Cmax for regimen C was not significantly lower than that for regimen A (22.1% less). These results suggest that aluminum containing drugs should not be given in combination with sparfloxacin.