340 BIOAVAILABILITY OF ORAL CHLORAMPHENICOL PALMITATE COMPARED TO INTRAVENOUS CHLORAMPHENICOL SUCCINATE

Abstract

The relative bioavailability of intravenous (I.V.) chloramphenicol succinate (CAP-S) and oral chloramphenicol palmitate (CAP-P) was compared in 14 children ages 2 months to 8 years. Chloramphenicol and CAP-S were measured in serum and urine by HPLC. The area under the serum concentration vs time curve (AUC) of chloramphenicol and urinary excretion of CAP-S were determined in each child under steady-state conditions while receiving CAP-S and again while receiving CAP-P. In 12 of the 14 children AUC was greater during oral CAP-P therapy, in 1 patient AUC was unchanged, and in 1 patient AUC was slightly decreased during oral compared to I.V. therapy. The mean AUC was significantly greater during oral therapy compared to I.V. therapy (116.3±6.8 mg.hrs/L vs 77.7±9.1 mg.hrs/L, p<.005). The relative bioavailability of I.V. CAP-S was 67% compared to oral CAP-P. This was explained by a loss of 39% of the I.V. dose in the urine as unhydrolyzed CAP-S. The dose of I.V. CAP-S did not correlate with AUC (r=.247). However, there was a significant correlation between dose of oral CAP-P and AUC (r=.733, p<.005). The bioavailability of oral CAP-P is superior to I.V. CAP-S. Furthermore, there is a greater correlation between dose and amount of active drug in the body when the oral preparation is used. Oral CAP-P appears to offer significant therapeutic advantages in patients who can tolerate oral medication.

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