J Korean Soc Clin Pharmacol Ther.  2013 Dec;21(2):104-112. 10.12793/jkscpt.2013.21.2.104.

Pharmacokinetic Characteristics of Cefcapene Pivoxil Hydrochloride after Single Oral Administration in Healthy Korean Subjects

• Rhee SJ
• Shin KH
• Cha YJ
• Kim JR
• Oh DS
• Cho JY
• Yu KS
• Jang IJ
• Chung JY
• Lim KS

• KMID: 2203223
• DOI: http://doi.org/10.12793/jkscpt.2013.21.2.104

Abstract

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.

Keyword

Cefcapene pivoxil hydrochloride; Pharmacokinetics; Tolerability; Korean; Healthy subjects

MeSH Terms

Administration, Oral*
Humans
Male
Pharmacokinetics
Physical Examination
Plasma

Figure

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  Figure 1. Mean plasma concentration time profiles of cefcapene after single oral administration of 100, 150 and 200 mg (left: linear scale, right: log-linear scale). Error bars mean standard error. * 100 mg. †150 and 200 mg. Mean concentrations on 12 hours after dose include only plasma concentrations above lower limit of quantification.

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  Figure 2. Comparison of dose-normalized pharmacokinetic parameters among the dosing groups (100, 150 and 200 mg). The boxes represent 50 % of the values, and the horizontal lines correspond to the median(—) and the mean(—) (left: dose normalized Cmax, right: dose normalized AUCinf).

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