Reappraisal of amoxycillin absorption kinetics

Westphal, Jean‐Frédéric; Deslandes, Antoine; Jm, Brogard; Carbon, C

doi:10.1093/jac/27.5.647

Cited by 27 publications

(31 citation statements)

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“…Cumulative a amount and b fraction of amoxicillin absorbed with time in 6 healthy subjects after the intake of 500 mg (--) and 3 g ( ..... ), calculated by a deconvolution method sistent with theirs, as there was a more irregular profile of absorption here after both doses, and no saturation of the input rate after 3 g. The discrepancy may be due to the different drug formulations used; Westphal et al gave amoxicillin as capsules and, as they pointed out, with a relatively small amount of water (100 ml) [27]. This may have led to disintegration or dissolution-limited absorption.…”

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confidence: 71%

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Nonlinearity of amoxicillin absorption kinetics in human

Paintaud

Alván

Dahl

et al. 1992

Eur J Clin Pharmacol

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Specialised gastrointestinal absorption of amoxicillin has been suggested in man and has been demonstrated in animals. In order to study the rate and extent of amoxicillin absorption, six healthy subjects were given 500 mg IV and two oral doses (500 mg and 3 g as a suspension). Absorption kinetics was analysed by compartmental modelling, noncompartmental methods and by calculation of absorption rates using deconvolution. Dose-dependency of the extent of amoxicillin absorption was observed, with a lower than expected mean maximum plasma concentration (49%), and fraction of the dose absorbed (39%) after the 3 g dose calculated from the 500 mg dose, assuming kinetic linearity. Zero-order kinetics of absorption was apparent in some subjects after the 500 mg dose, both from model fitting and absorption rate profile. However, no pattern consistent with pure first-order or zero-order absorption was observed after both oral doses in any individual. The dose-dependency of amoxicillin absorption was confirmed by a trend to an increased time of absorption for the high dose. The results show the variable nature and nonlinearity of the gastrointestinal absorption of amoxicillin and indicate the involvement of a number of factors, in addition to simple diffusion.

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confidence: 71%

“…[27] have observed a zero-order rate of absorption after i g amoxicillin, using the Loo-Riegelman method of analysis. The present results are not fully con-…”

Section: Discussionmentioning

confidence: 99%

Nonlinearity of amoxicillin absorption kinetics in human

Paintaud

Alván

Dahl

et al. 1992

Eur J Clin Pharmacol

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“…Figure 2 represents the predicted serum concentrations during multiple dosing (3 times a day) derived Bodey and Nance (10) and Duval et al (11), but lower levels than Croydon and Sutherland (12,13), although a similar assay method was used. Various bioavailability values have been obtained using different fonnulations (partially due to their dissolution behaviour) and C max has been shown to be proportional to the amount of water in which the tablet is dissolved (16,17). This can also reflect the wide interindividual variability encountered with this type of antibiotic, due to an irregular absorption process.…”

Section: Resultsmentioning

confidence: 99%

Pharmacokinetics of a new oral formulation of amoxicillin

Jehl²,

Rouveix

1997

European Journal of Drug Metabolism and Pharmacokinetics

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The bioavailability of the recently developed 1 g dispersible tablet form of amoxicillin (B) and the 1 g dispersible tablet in suspension form (C) were compared to that of the 1 g standard reference formulation (A). Twelve healthy volunteers were involved in this single-dose, open, randomized, three-way cross-over study. The mean peak serum levels were 14.1 +/- 4.1 micrograms/ml after A, 15.1 +/- 3.1 micrograms/ml after B and 15.1 +/- 5.4 micrograms/ml after C. The area under the drug concentration versus time curves were 47.6 +/- 12.0 micrograms.h/ml after A, 52.8 +/- 10.2 micrograms.h/ml after B and 51.1 +/- 13.8 micrograms.h/ml after C. On the basis of these two pharmacokinetic parameters, the three formulations were found to be bioequivalent. In addition, the predicted serum concentrations during multiple dosing (3 times a day), derived from the corresponding mean concentrations after a single 1 g dose of C showed that 8 hourly administration would yield therapeutic serum concentrations for infections such as uncomplicated community-acquired pneumonia due to susceptible or less susceptible strains in otherwise healthy subjects.

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“…Thus the formulations was uniform distributed in gastric site and maintain long time minimum inhibitory concentration (MIC) of the drug around microbial cell line [11]. Amoxicillin is semi-synthetic amino penicillin with a broad-spectrum bactericidal activity [12,13]. Pectin is colloidal polygalacturonic acid in which some of the carboxylic group is esterified with methyl group [14,15].…”

Section: Introductionmentioning

confidence: 99%

Formulation and In Vitro evaluation of pH sensitive oil entrapped buoyant beads of amoxicillin.

Tripathi¹,

Singh²

2011

Int J Drug Del

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A gastro retentive pH sensitive system has been a frontier approach to release the drug in controlled manner in stomach and duodenum. The aim of the study is to develop reliable formulation of amoxicillin which will release the drug in controlled way at specific site with acidic pH stimulus present in the gastric region. In the present investigation pectin based oil entrapped micro gel beads were prepared by ionic gelation technique using castor oil and mineral oil. The developed beads were evaluated in term of diameter, surface morphology, floating lag time, encapsulation efficiency, in vitro drug release. Prepared microbeads were regular and spherical in shape. The formulation exhibited sustained release profile and was best fitted in the Peppas model with n < 0.45. Subsequent coating of microbeads exhibited zero-order sustained pattern of amoxicillin release up to 8 hrs.The Results provides evidence that optimized gel bead may be used to incorporate antibiotics like amoxicillin and may be effective when administered locally in the stomach to cure microbial infection.

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Reappraisal of amoxycillin absorption kinetics

Cited by 27 publications

References 0 publications

Nonlinearity of amoxicillin absorption kinetics in human

Nonlinearity of amoxicillin absorption kinetics in human

Pharmacokinetics of a new oral formulation of amoxicillin

Formulation and In Vitro evaluation of pH sensitive oil entrapped buoyant beads of amoxicillin.

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