ISSN:
1573-904X
Keywords:
amoxicillin
;
absorption
;
human
;
dose-dependent
;
nonlinear
;
saturable
;
model
;
compartmental
;
time-constrained
Source:
Springer Online Journal Archives 1860-2000
Topics:
Chemistry and Pharmacology
Notes:
Abstract Amoxicillin pharmacokinetics was modeled using a two-compartment disposition model and a saturable time-constrained absorption model with a storage compartment. The absorption model parameters estimated by the nonlinear regression are: a rate constant of the systemic input, ksys, (median: 1.31 h−1, range: 0.79–7.01 h−1), a maximal absorption rate, Vma, (median: 1407 mg/h, range: 703–4181 mg/h), an account corresponding to the half-maximal rate, Kma, (median: 1077 mg, range: 235–4376 mg), time of the absorption cessation, Tabs, (median: 1.72 h, range: 0.82–4.53 h) and absorption lag time, Tlag, (median: 0.085 h, range: 0–0.123 h). It was shown, that the first-order absorption parallel to the saturable process is negligible in the dose range studied. The model described well the dependence of areas under concentration-time curves on the dose determined in several earlier studies. It was used also to predict the fraction of the amoxicillin dose absorbed for different doses. Simulations performed over a wide dose range (50–10000 mg) demonstrated that the fraction absorbed decreases nonlinearly from 90% at 50 mg to 22% at 10000 mg and strongly depends on the duration of the absorption period.
Type of Medium:
Electronic Resource
URL:
http://dx.doi.org/10.1023/A:1018911032009
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