건강한 한국인 피험자에서 염산세프카펜 피복실 단회 경구투여 시 약동학적 특성에 관한 연구 (Pharmacokinetic Characteristics of Cefcapene Pivoxil Hydrochloride after Single Oral Administration in Healthy Korean Subjects)

서지정보

· 발행기관 : 대한임상약리학회
· 수록지 정보 : Translational and Clinical Pharmacology / 21권 / 2호 / 104 ~ 112페이지
· 저자명 : 이수진, 신광희, 차유정, 김정렬, 오달석, 조주연, 유경상, 장인진, 정재용, 임경수

초록

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.

영어초록

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.

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