Comparison of the effects of food on the pharmacokinetics of cefprozil and cefaclor.
The objective of this study was to assess the effects of food on the pharmacokinetics of cefprozil and cefaclor. A group of 12 healthy male volunteers received a single 250-mg dose of cefprozil or cefaclor under fasting conditions as well as after the intake of food. There was a 1-week washout period between each treatment. Serial blood samples were collected and assayed for cefprozil or cefaclor by specific high-pressure liquid chromatographic methods. The mean +/- standard deviation peak concentration (Cmax) of cefprozil in plasma was 6.13 +/- 1.22 micrograms/ml under the fasting condition and 5.27 +/- 1.06 micrograms/ml after breakfast, and these values were not significantly different from each other. The corresponding median time to reach Cmax was prolonged after food intake, but this difference was not significant. The mean Cmax values of cefaclor decreased significantly from 8.70 +/- 2.72 micrograms/ml under the fasting condition to 4.29 +/- 1.52 micrograms/ml after breakfast, and the corresponding median times to reach Cmax were significantly prolonged. The mean half-lives of cefprozil and cefaclor were nearly identical for the two treatments, suggesting that the elimination kinetics of these cephalosporins remained unaltered when the drugs were administered with food. The area under the plasma-concentration-versus-time curves for fasted and fed conditions were not significantly different for both drugs. The results of this study indicate that the extent of absorption and rate of elimination of both cephalosporins remain unaltered in the presence of food. However, the absorption rate of cefaclor is significantly reduced in the presence of food, while that of cefprozil remains unaltered. As a result, the Cmax of cefaclor is significantly reduced in the presence of food, whereas that of cefprozil is not significantly affected. Cefprozil can be administered with a meal without markedly affecting levels in blood.
Barbhaiya
R H
RH
Department of Metabolism and Pharmacokinetics, Bristol-Myers Squibb Company, Syracuse, New York 13221-4755.
Shukla
U A
UA
Gleason
C R
CR
Shyu
W C
WC
Pittman
K A
KA
D000328:Adult; D002433:Cefaclor / Q000493:pharmacokinetics*; D002506:Cephalexin / Q000031:analogs & derivatives*; D002511:Cephalosporins / Q000493:pharmacokinetics*; D005502:Food / Q000009:adverse effects*; D006801:Humans; D007408:Intestinal Absorption; D008297:Male; D000097670:Cefprozil
D002433:Cefaclor; D002506:Cephalexin; D002511:Cephalosporins; D000097670:Cefprozil