건강한 한국인 피험자에서 Entecavir 1 mg 제제의 약동학적 특성 평가
Pharmacokinetic Propertiese of Entecavir 1 mg in Korean Healthy Volunteers
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초록
Entecavir is a potent and selective guanosine analogue that has demonstrated a significant antiviral efficacy against hepatitis B virus (HBV). The aim of this study was to evaluate the safety and pharmacokinetic profile after a single dose of entecavir 1 mg administration in Korean healthy male subjects. Eight volunteers were enrolled. After a single dose of 1 mg entecavir was orally administered, blood samples were collected at specific time intervals from 0-168 hours. The plasma concentrations of entecavir were determined by LC-MS/MS. The pharmacokinetic parameters were determined from the plasma concentration-time profiles. The mean values for AUC_(last) and AUC_(inf) were 14.84±7.81 ng·hr/mL and 20.71±8.80 ng·hr/mL, respectively. The mean value for C_(max) was 9.19±4.91 ng/mL and median value for t_(max) was 0.58 hr. No adverse events were reported by subjects or found on analysis of vital signs or laboratory tests. The results are suggested to be useful in clinical trials of entecavir in Korean subject including bioequivalence study.
Abstract
Entecavir is a potent and selective guanosine analogue that has demonstrated a significant antiviral efficacy against hepatitis B virus (HBV). The aim of this study was to evaluate the safety and pharmacokinetic profile after a single dose of entecavir 1 mg administration in Korean healthy male subjects. Eight volunteers were enrolled. After a single dose of 1 mg entecavir was orally administered, blood samples were collected at specific time intervals from 0-168 hours. The plasma concentrations of entecavir were determined by LC-MS/MS. The pharmacokinetic parameters were determined from the plasma concentration-time profiles. The mean values for AUC_(last) and AUC_(inf) were 14.84±7.81 ng·hr/mL and 20.71±8.80 ng·hr/mL, respectively. The mean value for C_(max) was 9.19±4.91 ng/mL and median value for t_(max) was 0.58 hr. No adverse events were reported by subjects or found on analysis of vital signs or laboratory tests. The results are suggested to be useful in clinical trials of entecavir in Korean subject including bioequivalence study.
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