Pharmacokinetic Characteristics of Cefcapene Pivoxil Hydrochloride after Single Oral Administration in Healthy Korean Subjects
Background: Cefcapene pivoxil hydrochloride (CFPN-PI) is an oral ester cephalosporin antibiotic with a
broad spectrum. In this study, we investigated the pharmacokinetics (PK) and tolerability of CFPN-PI
following single oral administration in healthy Korean subjects.
Methods: An open?label, dose?escalation, parallel group study was conducted in 18 healthy male
volunteers. A single dose of CFPN-PI was administered to 6 subjects in each treatment group of 100,
150 and 200 mg. Serial blood and urine samples were collected up to 12 h and 24 h after dosing,
respectively. Plasma and urine concentrations of cefcapene were measured by HPLC-UV. PK parameters
were estimated using non-compartmental analysis. For the safety evaluation, adverse event monitoring,
clinical laboratory tests and physical examination were performed throughout the study.
Results: Median values of time to peak plasma concentration were observed around 1.5 to 2.0 h.
Maximum plasma concentrations (Cmax) were 1.04 ± 0.22, 1.24 ± 0.46 and 1.56 ± 0.43 mg/L (mean ± SD),
and area under the plasma concentration?time curve (AUCinf) were 2.94 ± 0.46, 3.97 ± 1.28 and 4.70 ±
1.19 h*mg/L in 100, 150 and 200 mg dose groups, respectively. The differences of dose?normalized Cmax
and AUCinf among three groups were not statistically significant. The fractions of drug excreted in urine
unchanged were 31.5 % - 42.9 %. There were no serious adverse events or clinically significant
abnormalities related to CFPN-PI.
Conclusion: CFPN-PI was well tolerated with single oral administration and showed a linear PK
property within 100 - 200 mg in healthy Korean male subjects.
Cefcapene pivoxil hydrochloride, Pharmacokinetics, Tolerability, Korean, Healthy subjects