Pharmacokinetic analysis of the effects of different foods on absorption of cefaclor

Abstract

Cefaclor is an oral cephalosporin antibiotic which has a broad antibacterial spectrum. The purpose of this study was to investigate the effect of food on the absorption of cefaclor and to analyze kinetically the absorption process of this drug. Cefaclor was given to eight volunteers at five test times: after overnight fasting, after two rice meals (350 and 700 cal [1 cal = 4.184 JI), and after two bread meals (500 and 1,000 cal). Urinary recoveries of cefaclor and concentrations of the drug in plasma were determined for each administration. Areas under the concentration-time curves and urinary recoveries were not affected by food intake, but the maximum concentration of drug in serum was reduced and the time to maximum concentration of drug in serum was prolonged depending on the type and the quantity of the meal. The larger the quantity of the meal, the more the maximum concentration of drug in serum and the time to maximum concentration of drug in serum were affected. The rice meals affected the absorption process of cefaclor more than the bread meals. The concentrations of cefaclor in plasma following administration after overnight fasting were well fitted to a conventional one-compartment model with a first-order absorption process, but those after the other administrations were not fitted to the model. For the pharmacokinetic analysis of those data, it was necessary to introduce a transfer process from administration site to absorption site to the conventional model. The concentrations in plasma after rice and bread meals were best fitted to the model with a zero-order transfer process than to that with a first-order process. The velocity of the transfer process depended on the type and volume of the meal.

The effect of four different types of food on the bioavailability of cefaclor

“…All diets studied showed an insignificant decrease in the AUC O _ t except high fat non-vegetarian diet as compared to fasting state. There, however, was no significantdecrease in AUC o _ oo in all treatments, which is in agreement with published reports in the literature (6,11). Only high fat non-vegetarian diet significantly decreased the extent of absorption.…”

“…is hindered by food intake (7,8) or cases in whichabsorption is accelerated by food intake (9,10) The bioavailability of cefaclor has been reported to be reduced by food intake (11). However, in a recent study with the modified release formulation of cefaclor the bioavailability of cefaclor was found to be increased with the co-administration of cefaclor with food (12).There is a wide variation in dietary practices and beliefs among populations throughout the world.…”

Comparative effect of different types of food on the bioavailability of cefaclor extended release tablet

“…There was a 50% increase in C max when rice diet was compared with fasting (P<O.OOI) this was followed by 33% increase with low-fat vegetarian diet (wheat based) (P<O.OOI) and 29% with high-fat non-vegetarian diet (P<O.OI).The increase in C max by rice diet, followed by low-fat non-vegetarian diet is in agreement with reported food effect by Oguma et al (19). Oguma et al have reported that rice diet decreased the rate of absorption more than the bread diet with cefador immediate release formulation.…”

“…This is in agreement with the results reported by other workers. (9,19).The increase was inversely related to the fat content of the diet. Both high-fat vegetarian and non-vegetarian diets produced a smaller increase in tmax (37.5%) as compared to the respective low-fat vegetarian and nonvegetarian diets (100%).…”

Combined effects of a high-fat diet and chronic valproic acid treatment on hepatic steatosis and hepatotoxicity in rats

“…Food preferences contribute to the physiological diversity among individuals, especially in patients, because food may influence metabolic patterns and the efficacy of drugs [12,13] . It is well known that a high-fat diet (HFD) is a major contributing factor in the prevalence of NAFLD, which is defined as the significant accumulation of fat in the liver (>5%-10% of the weight of the liver), which can be as high as 76% in obese subjects [14][15][16] .…”