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Single intravenous and oral pharmacokinetics of danofloxacin in the goat
Small Ruminant Research ( IF 1.6 ) Pub Date : 2021-04-22 , DOI: 10.1016/j.smallrumres.2021.106393
Irene Sartini , Beata Łebkowska-Wieruszewska , Andrzej Lisowski , Amnart Poapolathep , Victoria Llewelyn , Mario Giorgi

Respiratory diseases including pneumonia are a common concern in goats, with M. Haemolytica the usual causative organism. Owing to danofloxacin’s wide spectrum of activity, it is used to treat such disease in goats. The aim of the present study was to investigate danofloxacin pharmacokinetics in the goat after single intravenous (IV) and oral (PO) administration.

Sixteen healthy goats were randomly divided into two groups. The first group (n = 8) was administered danofloxacin IV (6 mg/kg) and the second group (n = 8) was administered danofloxacin PO (12 mg/kg). Blood was collected from 0 to 36 h after drug administration. Plasma samples were analyzed for danofloxacin content using a validated HPLC-FL method. The pharmacokinetic analysis was performed using a non-compartmental model, and the PK/PD index was used to predict the antimicrobial effect of danofloxacin.

Danofloxacin was quantifiable up to 36 h for both administration routes. After IV administration, danofloxacin demonstrated a long t1/2kel (10.09 h), with a Cl of 0.69 mL/g*h and a Vss of 2.66 mL/g. Unfortunately, an unanticipated long-lasting absorption phase after PO administration only allowed calculation of Cmax (0.13 μg/mL), Tmax (8 h) and AUC(0-t) (2.74 h).

The PK/PD surrogate for the prediction of a fluoroquinolone’s efficacy (AUC(0–24)/MIC), corrected for danofloxacin’s low plasma protein binding, suggested that a single PO danofloxacin dose at 12 mg/kg may be effective against M. haemolytica in the goat.



中文翻译:

达氟沙星在山羊中的单次静脉内和口服药代动力学

山羊中常见的呼吸系统疾病包括肺炎,而溶血支原体是常见的致病菌。由于达氟沙星具有广泛的活性,因此可用于治疗山羊中的此类疾病。本研究的目的是研究单次静脉内(IV)和口服(PO)给药后达氟沙星在山羊中的药代动力学。

将十六只健康的山羊随机分为两组。第一组(n = 8)服用danofloxacin IV(6 mg / kg),第二组(n = 8)服用danofloxacin PO(12 mg / kg)。给药后0至36小时收集血液。使用经过验证的HPLC-FL方法分析血浆样品中的达氟沙星含量。使用非房室模型进行药代动力学分析,PK / PD指数用于预测达氟沙星的抗微生物作用。

两种给药途径中达氟沙星的定量长达36小时。静脉注射后,达氟沙星显示出较长的t 1 / 2kel(10.09 h),Cl为0.69 mL / g * h,V ss为2.66 mL / g。不幸的是,PO给药后出乎意料的持久吸收阶段仅允许计算C max(0.13μg/ mL),T max(8 h)和AUC (0-t)(2.74 h)。

PK / PD替代品可预测氟喹诺酮的药效(AUC (0-24) / MIC),并已校正达氟沙星的血浆蛋白结合率较低,提示单剂量PO达氟沙星剂量为12 mg / kg可能对溶血支原体有效在山羊身上。

更新日期:2021-04-29
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