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哺乳期雌性单峰骆驼(骆驼属单峰驼)血浆和乳汁中培氟沙星的浓度-时间过程。

Concentration-time courses of pefloxacin in plasma and milk of lactating she-camels (Camelus dromedarius).

作者信息

Goudah Ayman, Shah Syed Sher, Shin Ho-Chul, Chang Byung-Joon, Shim Jae-Han, Abd El-Aty A M

机构信息

Department of Pharmacology, Faculty of Veterinary Medicine, Cairo University, Giza, Egypt.

出版信息

Berl Munch Tierarztl Wochenschr. 2008 Nov-Dec;121(11-12):432-9.

Abstract

Using the microbial inhibition test, the single-dose pharmacokinetics of pefloxacin mesylate dehydrate were studied in six clinically normal lactating she-camels (Camelus dromedarius) after intravenous (IV) and intramuscular (IM) administration of 10 mg/kg body weight (bwt). Blood and milk samples were collected intermittently for a 48 h period, and the pharmacokinetic variables were calculated using compartmental and non-compartmental analytical methods.The plasma course of pefloxacin was best resolved to a two-compartment open model after IV administration and a two-compartment open model with first-order absorption after IM administration. Pefloxacin exhibits a long elimination-phase disposition half-life (t1/2beta) of 4.89 +/- 1.12 h after IV injection and 5.73 +/- 1.42 h after IM administration. The mean volume of distribution at steady state (Vdss) and total body clearance (Cl(tot)) values after IV dosing were 1.18 +/- 0.45 I/kg and 0.21 +/- 0.10 I/kg/h, respectively. The observed peak plasma level (Cmax) of 3.6 +/- 0.1 microg/ml was rapidly attained at 0.75 h (the time of maximum concentration Tmax) after IM administration. The areas under the concentration versus time curves (AUCs) were 44.18 +/- 9.68 microg x h/ml and 29.42 +/-6.49 microg x h/ml after IV and IM administration, respectively. The absolute bioavailability (F%) obtained after IM administration was 71.59 +/- 12.45%. Milk was penetrated quickly, with a mean peak level of 3.24 +/- 0.17 microg/ml occurring at 1.0 h. The elimination half-life was significantly shorter after IV versus IM administration (4.21 +/- 0.84 h versus 5.32 +/- 0.67 h, respectively). Ultimately, pefloxacin could be useful for treatment of udder infections in she-camels after specific assessment of susceptible microorganisms.

摘要

采用微生物抑制试验,对6头临床健康的泌乳雌性单峰骆驼( Camelus dromedarius )静脉注射(IV)和肌肉注射(IM)10mg/kg体重的甲磺酸培氟沙星脱水物后的单剂量药代动力学进行了研究。在48小时内间歇性采集血液和乳汁样本,并使用房室和非房室分析方法计算药代动力学变量。静脉注射后,培氟沙星的血浆过程最佳解析为二室开放模型,肌肉注射后为具有一级吸收的二室开放模型。培氟沙星静脉注射后的消除相处置半衰期(t1/2β)较长,为4.89±1.12小时,肌肉注射后为5.73±1.42小时。静脉给药后的稳态分布容积(Vdss)和总体清除率(Cl(tot))平均值分别为1.18±0.45L/kg和0.21±0.10L/kg/h。肌肉注射后0.75小时(达峰时间Tmax)迅速达到3.6±0.1μg/ml的观察到的血浆峰浓度(Cmax)。静脉注射和肌肉注射后的浓度-时间曲线下面积(AUCs)分别为44.18±9.68μg·h/ml和29.42±6.49μg·h/ml。肌肉注射后的绝对生物利用度(F%)为71.59±12.45%。乳汁很快被渗透,1.0小时时平均峰浓度为3.24±0.17μg/ml。静脉注射后的消除半衰期明显短于肌肉注射(分别为4.21±0.84小时和5.32±0.67小时)。最终,在对敏感微生物进行特定评估后,培氟沙星可能对治疗雌性单峰骆驼的乳房感染有用。

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