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Pharmacokinetics of Oleandomycin in Dogs After Intravenous or Oral Administration Alone and After Pretreatment With Metamizole or Dexamethasone

机译:单独或静脉内给药以及用间苯二甲胺或地塞米松预处理后狗中奥利霉素的药代动力学

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摘要

The pharmacokinetics of oleandomycin OLD) after intravenous and oral administration, both alone and after intramuscular pretreatment with metamizole or dexamethasone, were studied in healthy dogs. After intravenous injection of OLD alone 10 mg/kg as bolus), the elimination half-life t 1/2β, volume of distribution V d, area), body clearance CLB) and area under the concentration-time curve AUC) were 1.60 h, 1.11 L/kg, 7.36 ml/kg)/min and 21.66 µg h/ml, respectively. There were no statistically significant differences following pretreatment with metamizole or dexamethasone. After oral administration of OLD alone, the t frac12;β, maximum plasma concentrations C max), time of C max t max), mean absorption time MAT) and absolute bioavailability F abs) were 1.68 h, 5.34 µg/ml, 1.5 h, 1.34 h and 84.29%, respectively. Pretreatment with metamizole caused a significantly decreased value for C max 2.93 µg/ml) but the MAT value 2.23 h) was significantly increased. Statistically significant changes in the pharmacokinetic parameters of OLD following oral administration were also observed as a result of pretreatment with dexamethasone. The C max was increased 8.24 µg/ml) and the t max 0.5 h) and MAT 0.45 h) were lower.
机译:在健康犬中研究了单独和静脉内和口服咪达唑或地塞米松预处理后,oleandomycin OLD)的药代动力学。单独静脉注射OLD 10 mg / kg推注后),消除半衰期t 1 /2β,分布体积d,面积),身体清除率CLB )和在浓度-时间曲线AUC下的面积分别为1.60h,1.11L / kg,7.36ml / kg)/ min和21.66μgh/ ml。用间咪唑或地塞米松预处理后无统计学差异。单独口服OLD后,t frac12;β,最大血浆浓度C max ),C max t max 的时间,平均吸收时间MAT)和绝对生物利用度(abs)分别为1.68 h,5.34 µg / ml,1.5 h,1.34 h和84.29%。 meta咪唑预处理导致C max值显着降低,为2.93 µg / ml,但MAT值显着提高了2.23 h。口服地塞米松也可观察到口服给药后OLD的药代动力学参数有统计学上的显着变化。 C max升高8.24 µg / ml,t max 0.5 h和MAT 0.45 h降低。

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