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单次静脉给药后头孢曲松在四氯化碳诱导的肝病山羊和硝酸铀酰诱导的肾病山羊体内的药代动力学。

Pharmacokinetics of ceftriaxone in carbontetrachloride-induced hepatopathic and uranyl nitrate-induced nephropathic goats following single dose intravenous administration.

作者信息

Sar Tapas Kumar, Mandal Tapan Kumar, Das Shymal Kumar, Chakraborty Animesh Kumar

机构信息

Department of Pharmacology & Toxicology, West Bengal University of Animal and Fishery Sciences, 37&68, Kshudiram Bose Sarani, Kolkata-37, West Bengal, India.

出版信息

Drug Metab Lett. 2008 Jan;2(1):23-8. doi: 10.2174/187231208783478515.

Abstract

The pharmacokinetic profile of ceftriaxone was studied in female healthy goats, induced hepatopathic and nephropathic goats after a single intravenous dose at 50 mg kg(-1). Ceftriaxone persisted for 2 h in plasma of hepatopathic goats compared to 1 h of healthy goats, but the kinetic behaviour followed 'one-compartment open model' in both healthy and hepatopathic goats. Mean value of t((1/2))beta (0.32 +/- 0.008 h) was significantly higher in hepatopathic goats compared to healthy goats (0.19 +/- 0.002 h). Ceftriaxone was recovered at 24 h in urine of hepatopathic goats but it could not be detected in urine of healthy goats. However, its metabolite ceftizoxime was present in urine of healthy goats but not in urine of hepatopathic goats. On the other hand ceftriaxone persisted for 2 h in plasma of kidney damaged goats with significant higher concentration compared to healthy goats but kinetic behaviour followed 'one Compartment open model'. Ceftizoxime was identified with an adequate plasma concentration from 8 h to 12 h post dosing in nephropathic goats. Elimination halflife (t(1/2)beta) of Elimination ceftriaxone (0.38 +/- 0.01 h) in nephropathic goats increased significantly compared to healthy goats (0.19 +/- 0.002 h). Ceftriaxone, not the metabolite ceftizoxime was recovered at 24 h and 48 h post dosing in urine of nephropathic goats, while only ceftizoxime not ceftriaxone was detected in urine of healthy goats.

摘要

在雌性健康山羊、诱导性肝病山羊和肾病山羊中,以50mg/kg的剂量单次静脉注射后,研究了头孢曲松的药代动力学特征。与健康山羊血浆中头孢曲松持续1小时相比,肝病山羊血浆中头孢曲松持续2小时,但在健康山羊和肝病山羊中,其动力学行为均遵循“一室开放模型”。与健康山羊(0.19±0.002小时)相比,肝病山羊的t((1/2))β平均值(0.32±0.008小时)显著更高。在肝病山羊的尿液中,24小时时可检测到头孢曲松,但在健康山羊的尿液中未检测到。然而,其代谢产物头孢唑肟存在于健康山羊的尿液中,而不存在于肝病山羊的尿液中。另一方面,与健康山羊相比,肾损伤山羊血浆中头孢曲松持续2小时,浓度显著更高,但其动力学行为遵循“一室开放模型”。在肾病山羊给药后8小时至12小时,可检测到血浆中头孢唑肟浓度适宜。与健康山羊(0.19±0.002小时)相比,肾病山羊中头孢曲松的消除半衰期(t(1/2)β)(0.38±0.01小时)显著延长。在肾病山羊给药后24小时和48小时的尿液中可检测到头孢曲松,而非其代谢产物头孢唑肟,而在健康山羊的尿液中仅检测到头孢唑肟,未检测到头孢曲松。

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