Match!

Effect of doses and dosage forms on the bioavailability of amoxicillin in non-fasted rats

Published on Jan 1, 2012in Journal of Drug Delivery Science and Technology2.606
· DOI :10.1016/S1773-2247(12)50098-5
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 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 plasma concentration at 12 h of the solution was larger than those of the suspension. The difference was considered to be caused by an inadvertent scattering of the data. The AUC 0 -24h , values at 50 mg/kg were 3.17 times larger than those at 15 mg/kg for the solution, and 3.44 times larger for the suspension. A comparison with AUC values in fasted rats reported previously revealed the bioavailability of AMX to decrease due to the effect of food.
  • References (4)
  • Citations (0)
📖 Papers frequently viewed together
6 Citations
2007
4 Authors (Sajid Bashir, ..., Ishrat Bukhari)
78% of Scinapse members use related papers. After signing in, all features are FREE.
References4
Newest
#1T. Tokumura (International University of Health and Welfare)H-Index: 1
#2M. Nagaoka (Hoshi University)H-Index: 1
Last. Yoshiharu Machida (Hoshi University)H-Index: 38
view all 3 authors...
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...
1 CitationsSource
#1Jesús Chesa-Jiménez (University of Valencia)H-Index: 7
#2José-Esteban Peris (University of Valencia)H-Index: 10
Last. Luis Granero (University of Valencia)H-Index: 21
view all 4 authors...
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...
21 CitationsSource
#1Ryouichi Machida (Eisai)H-Index: 3
#2Tadakazu Tokumura (Eisai)H-Index: 10
Last. Kouichi Abe (Eisai)H-Index: 6
view all 5 authors...
A high-performance liquid chromatographic method to determine (Me)Arg-Lys-Pro-Trp-tert-Leu-Leu (NT-2) with neurotensin (NT) activity in rat plasma was developed and a pharmacokinetic study was performed in rats. Quantitative analysis with high reproducibility was achieved for NT-2 over the concentration range of 1.14-500ng/ml.(Me)Arg-Lys-Pro-Trp-tert-Leu-Leu-OEt (NT-1) was rapidly hydrolyzed to NT-2 in rat plasma at 37°C. This degradation of NT-1 was observed as a pseudo first-order reaction, an...
25 CitationsSource
The effect of food on the absorption of amoxicillin and ampicillin was studied in 16 normal subjects in a double-blind crossover study after each subject was given a single oral 500-mg dose. Serum drug levels were analyzed, assuming a one-compartment linear model with first-order absorption and absorption delay, area under the curve, and urinary recovery. Variations in kinetic parameters were examined by using analysis of variance. The results showed little or no effect of fasting versus nonfast...
46 CitationsSource
Cited By0
Newest