Pharmacokinetics of Florfenicol and its Metabolite, Florfenicol Amine, in Broiler Chickens

육계에서의 플로르페니콜 및 그의 대사체인 플로르페니콜 아민의 약물동태학적 연구

  • Published : 2006.06.01

Abstract

A study on bioavailability and pharmacokinetics of florfenicol was conducted in broilers following a single intravenous (i.v.) and oral (p.o.) doses of 20 mg/kg body weight (b.w.). Florfenicol concentrations in plasma were determined by a high-performance liquid chromatography/mass spectrometry. Plasma concentration-time data after i.v. administration were analyzed by a non-compartmental analysis. Following i.v. injection, the total body clearance was $0.74{\pm}0.25L/kg/h$ and the volume of distribution at steady-state was $1.16{\pm}0.19L/kg$. Florfenicol was rapidly distributed and eliminated following i.v. injection with $1.15{\pm}1.06h$ of elimination half-life. After oral administration, the calculated $C_{max}$ values ($8.18{\pm}0.97{\mu}g/mL$) were reached at $1.33{\pm}0.29h$ in broilers. The elimination half-life of florfenicol was $1.31{\pm}0.27h$ and the absolute bioavailability (F) was 75.46% after oral administration of florfenicol. Florfenicol amine, a major metabolite of florfenicol, was detected in all broilers after i.v. and p.o. administration of florfenicol. The observed $C_{max}$ values of florfenicol amine ($3.96{\pm}2.60\;and\;2.22{\pm}1.71{\mu}g/mL$) were reached at $0.16{\pm}0.19\;and\;1.61{\pm}1.02h$ after i.v. and p.o. administration of florfenicol, respectively. Florfenicol amine was eliminated with $1.88{\pm}0.39\;and\;2.64{\pm}1.39h$ of the elimination half-life after i.v. and p.o. administration of florfenicol, respectively.

본 연구는 플로르페니콜을 체중당 20mg 용량으로 경구 및 정맥내로 투여한 후 플로르페니콜 및 그 대사체인 플로르페니콜 아민의 생체이용율 및 약물동태학적 분석을 육계에서 실시하였다. 혈청내의 플로르페니콜 및 플로르페니콜 아민의 정량은 액체크로마토그래프/질량분석기를 사용하였으며, 경구 및 정맥내 투여후 혈청 농도-시간 자료는 non-compartmental analysis를 이용하여 분석하였다. 플로르페니콜의 정맥주사 후 청소율 및 소실반감기는 각각 $0.74{\pm}0.25L/kg/h$$1.15{\pm}1.06h$로 나타났으며, 정상상태 분포용적은 $1.16{\pm}0.19L/kg$으로 정맥주사후 빠른 체내 분포와 소실을 나타냈다. 플로르페니콜의 경구투여 후 혈중최고농도 ($8.18{\pm}0.97{\mu}g/mL$)는 $1.33{\pm}0.29h$에 나타났다. 소실반감기는 $1.24{\pm}0.64h$이었으며, 경구생체이용율은 약 75.46%로 나타났다. 플로르페니콜의 주요 대사체인 플로르페니콜 아민은 정맥 및 경구투여한 모든 육계에서 검출되었다. 플로르페니콜 아민의 혈중최고농도는 정맥 및 경구투여 후 각각 $1.88{\pm}0.39{\mu}g/mL$$2.64{\pm}1.39{\mu}g/mL$$0.16{\pm}0.19h$$1.61{\pm}1.02h$에 관찰되었다. 플로르페니콜 아민은 정맥 및 경구 투여후 각각 $1.88{\pm}0.39$ and $2.64{\pm}1.39h$로 그 모약인 플로프페니콜보다 다소 느리게 소실되었다.

Keywords

References

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