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Relative bioavailability of three cefixime formulations.
1Department of Pharmacology, University of Regensburg, Fed. Rep. of Germany.
Arzneimittel-Forschung
|March 1, 1990
Summary
Comparing cefixime formulations, dry suspension and tablets showed superior bioavailability compared to syrup. For optimal cefixime absorption, consume dry suspension or tablets with ample liquid.
Area of Science:
- Pharmacology
- Pharmaceutical Sciences
Background:
- Cefixime is a broad-spectrum cephalosporin antibiotic used to treat various bacterial infections.
- Different galenic formulations (tablet, syrup, dry suspension) can influence drug absorption and bioavailability.
- Understanding relative bioavailability is crucial for optimizing cefixime dosage and efficacy.
Purpose of the Study:
- To compare the relative bioavailability of three different cefixime formulations (200 mg each): tablet, syrup, and dry suspension.
- To determine which formulation provides the most reliable and efficient absorption of cefixime in healthy volunteers.
Main Methods:
- A relative bioavailability study was conducted in twelve healthy volunteers.
- Participants received single oral doses of 200 mg of cefixime in tablet, syrup, and dry suspension forms.
- Pharmacokinetic parameters, including peak plasma concentration (Cmax) and area under the curve (AUC0-infinity), were measured and compared.
Main Results:
- All cefixime formulations demonstrated reliable absorption, with peak plasma concentrations reached between 3.3-3.5 hours and terminal half-lives of 2.9-3.1 hours.
- The dry suspension yielded the highest bioavailability (AUC0-infinity = 25.8 ± 7.0 µg/mL·h; Cmax = 3.4 ± 0.9 µg/mL), followed by the tablet (AUC0-infinity = 20.9 ± 8.1 µg/mL·h; Cmax = 3.0 ± 1.0 µg/mL).
- The syrup formulation showed the lowest bioavailability (AUC0-infinity = 17.8 ± 5.9 µg/mL·h; Cmax = 2.4 ± 0.7 µg/mL), with statistical analysis confirming bioinequivalence between the dry suspension and syrup.
Conclusions:
- The dry suspension and tablet formulations offer better cefixime bioavailability compared to the triglyceride-based syrup.
- Optimal oral absorption of cefixime is achieved when administered as a dry suspension or tablet in an aqueous medium with sufficient fluid intake.
- These findings have implications for clinical practice, guiding the selection of cefixime formulations for improved therapeutic outcomes.