Comparative pharmacokinetics of two tablet formulations of amoxicillin: bioequivalence assessment.
The aim of the present study was to compare the bioavailability of amoxicillin (CAS 26787-78-0) from two different amoxicillin tablets (Demoksil 1 g tablet as test preparation and 1 g tablet of the originator product as reference preparation). The study was conducted according to an open-label, randomised two-period cross-over design with a wash-out phase of 4-7 days. Blood samples for pharmacokinetic profiling were taken up to 10 h post-dose, and amoxicillin plasma concentrations were determined with a validated LC-MS/ MS method. Maximum plasma concentrations (C(max)) of 13,296.4 ng/ml (test) and 12,797.7 ng/ml (reference) were achieved. Areas under the plasma concentration-time curve (AUC(0-infinity)) of 39,556.7 ng x h/ml (test) and 38,599.1 ng x h/ml (reference) were calculated. The median t(max) was 1.62 h (test) and 1.54 h (reference). Plasma elimination half-lives (t(1/2)) of 1.64 h (test) and 1.65 h (reference) were determined. Both primary target parameters, AUC(0-infinity) and C(max) were tested parametrically by analysis of variance (ANOVA) and the 90% confidence intervals were between 96.76%-108.46% (AUC(0-infinity)) and 97.80%-111.98% (C(max)). Bioequivalence between test and reference preparation was demonstrated since for both parameters, AUC and C(max) the 90% confidence intervals of the T/R-ratios of logarithmically transformed data were in the generally accepted range of 80%-125%.
Sailer
Reinhard
R
Pharmakin GmbH, Gesellschaft für Pharmakokinetik, Ulm, Germany. reinhard.sailer@pharmakin.de
Arnold
Peter
P
Erenmemişoğlu
Aydin
A
Martin
Wolfgang
W
Tamur
Uygur
U
Kanzik
Ilker
I
Hincal
A Atilla
AA
D000293:Adolescent; D000328:Adult; D000658:Amoxicillin / Q000008:administration & dosage / Q000493:pharmacokinetics*; D000900:Anti-Bacterial Agents / Q000008:administration & dosage / Q000493:pharmacokinetics*; D019540:Area Under Curve; D002138:Calibration; D002626:Chemistry, Pharmaceutical; D018592:Cross-Over Studies; D004311:Double-Blind Method; D005260:Female; D006207:Half-Life; D006801:Humans; D008297:Male; D011786:Quality Control; D021241:Spectrometry, Mass, Electrospray Ionization; D013810:Therapeutic Equivalency
D000900:Anti-Bacterial Agents; D000658:Amoxicillin