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Effect of doses and dosage forms on the gastro-intestinal absorption of amoxicillin in rats

Published on Jan 1, 2011in Journal of Drug Delivery Science and Technology2.606
· DOI :10.1016/S1773-2247(11)50032-2
T. Tokumura1
Estimated H-index: 1
(International University of Health and Welfare),
M. Nagaoka1
Estimated H-index: 1
(Hoshi University),
Yoshiharu Machida38
Estimated H-index: 38
(Hoshi University)
Abstract
The absorption of amoxicillin (AMX) administered orally was studied in rats. Male Sprague-Dawley rats received 7, 15, 25 and 50 mg/kg of AMX in two dosage forms, a suspension and a solution. Plasma concentrations of AMX were determined by HPLC. When AMX was administered at 7 mg/kg, there was no significant difference in C max , T max , AUC and MRT values between the dosage forms. At 50 mg/kg, there was no significant difference in the plasma concentrations of AMX, but the C max and AUC values of the suspension were significantly higher than those of the solution. The relationship between dose, and C max and AUC values for the suspension had a good linear relationship, y = 0.113642x - 0.05082, r = 0.995, and y = 0.727784x - 0.56625, r = 0.997, respectively. Thus AMX had a linear pharmacokinetic profile at doses from 7 to 50 mg/kg after its oral administration as a suspension, and the dosage form affected the bioavailability of AMX.
  • References (7)
  • Citations (1)
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Abstract An intragastric buoyant sustained-release tablet (IGB-T) containing 100 mg of amoxicillin (AMX) was prepared to eradicate gastric Helicobacter pylori . A tablet prepared by compressing the mixture of hydroxypropylcellulose-H (HPC-H), citric acid (17.2 mg), sodium hydrogen carbonate (22.8 mg) and AMX was employed as the basic system for preparing IGB-T. The weight and diameter of the tablets were designed to be about 300 mg and 10 mm, respectively. IGB-T containing 5 mg of AMX and HPC-H ...
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Several studies have been carried out to elucidate the causes of the low oral bioavailability of amoxicillin in rats. The hepatic first-pass effect of the antibiotic was estimated by comparing the area under the plasma drug concentration-versus-time curve from time zero to infinity (AUC0-infinity) obtained after injecting the drug into a mesenteric vein with the AUC0-infinity value obtained after injecting the drug into the jugular vein of conscious rats. No hepatic first-pass effect was detecte...
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Most factors influencing amoxycillin oral absorption are, even today, unknown. Since many dosage schedules have been shown to lead to incomplete absorption, it would be desirable to find a suitable animal model where these factors could be studied in depth. In this paper, it is shown that, in the rat, plasma level curves obtained after oral doses of 7 and 28 mg kg-1 are poorly fitted using first-order absorption kinetics and that the best fit is obtained through the use of an input equation comb...
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#1T. Tokumura (International University of Health and Welfare)H-Index: 1
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The absorption of amoxicillin (AMX) administered orally was studied in non-fasted rats. The rats received 15 and 50 mg/kg of AMX in two dosage forms, a suspension and a solution. Plasma concentrations of AMX were determined by HPLC. When AMX was administered at 15 mg/kg, there was no significant difference in C max , T max , AUC and MRT values between the dosage forms. No significant difference in C max , T max , AUC 0 -24h , and MRT 0 -24h was observed at 50 mg/kg either. However, the mean plas...
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