Abstract
The goal of our research was to compare the pharmacokinetics and evaluate the bioequivalence of two brands of cephradine 500 mg capsules in 24 normal Korean volunteers. The plasma samples were acquired at 13 time points for 8 h after administration. The concentrations of cephradine in human plasma were measured by a high-performance liquid chromatography (HPLC). Isocratic mobile phase which consisted of acetonitrile, methanol, and 20 mM potassium phosphate (15/5/80, v/v/v, pH 3.48) was used to separate the analytical column cosmosil cholester (250 × 4.6 mm, 3 μm). Analytes were detected in ultraviolet (260 nm). The novel analytical method was described as simple sample preparation, a short retention time (less than 6 min) and making it suitable for use in clinical trials. Pharmacokinetic parameters, such as AUC0-t (20.54 vs 18.42 μg·h/mL), AUC0-infinity (21.22 vs 19.14 μg·h/mL), Cmax (12.69 vs 12.81 μg/mL), Tmax (1.22 vs 0.92 h), half-life (1.02 vs 1.13 h), extrapolation (3.22% vs 3.75%), and Ke (0.73 vs 0.69 h–1) were determined for the reference and test drugs in plasma. Pharmacokinetic parameters with a 90% confidence interval were 87% - 95% for AUC0-t and 91% - 115% for Cmax. They were satisfied within the bioequivalence range 80% - 125% of the KFDA guidelines. Therefore, our HPLC method was well applied in a bioequivalence and pharmacokinetic study of two formulations in normal subjects.
Highlights
IntroductionIt has broad spectrum antibacterial activity against gram-positive and gram-negative microorganisms and acts through inhibiting bacterial cell wall synthesis
The concentrations of cephradine in human plasma were measured by a high-performance liquid chromatography (HPLC)
The following chromatograms were shown in Figure 2: (a) double blank plasma without cephradine and IS, (b) blank plasma with 200 μg/mL of IS, (c) blank plasma spiked with 0.3 μg/mL (LLOQ) of a calibration standard of cephradine and 200 μg/mL of IS, and (d) human plasma taken 1.5 h after a single oral dose of cephradine (500 mg tablet) and spiked with 200.0 μg/mL of IS
Summary
It has broad spectrum antibacterial activity against gram-positive and gram-negative microorganisms and acts through inhibiting bacterial cell wall synthesis. Cephradine is used to treat upper respiratory infections, ear infections, skin infections, and urinary tract infections. It is rapidly absorbed from the gastrointestinal tract and has low plasma protein binding (6% - 20%) [1]. It is excreted approximately 90% of the drug which is unchanged by the kidney within 6 h administration [2]. A daily therapeutic dose of cephradine is 250 - 500 mg, and after oral administration of 500 mg of cephradine the maximal plasma concentration (Cmax) is 15.67 ± 4.21 μg/mL and the time to maximal plasma concentration (Tmax) is about 1 h [3]
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