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左旋咪唑经皮下和口服途径给药在兔体内的生物利用度。

Bioavailability of levamisole administered by subcutaneous and oral routes in rabbits.

作者信息

García J J, Diez M J, Sierra M, Terán M T

机构信息

Department of Physiology, Pharmacology and Toxicology, Veterinary Faculty, University of León, Spain.

出版信息

J Vet Pharmacol Ther. 1994 Apr;17(2):135-40. doi: 10.1111/j.1365-2885.1994.tb00223.x.

Abstract

The bioavailability of levamisole in rabbits was determined after subcutaneous and oral administration at three dose levels of 12.5, 16.0 and 20.0 mg/kg. After non-compartmental analysis the mean values obtained were: Cmax = 3.54, 4.51 and 5.39 micrograms/ml; tmax = 12.0, 22.0 and 20.0 min; F = 134.8, 105.4 and 124.1% after subcutaneous administration for each dose, respectively, and Cmax = 0.71, 1.32 and 1.77 micrograms/ml; tmax = 46.0, 96.0 and 84.0 min; F = 53.0, 62.0 and 80.7% after oral administration. The extent and rate of absorption from the two routes differed significantly, except for tmax at the 12.5 mg/kg dose. After compartmental analysis the pharmacokinetics of levamisole was characteristic of a two-compartment open model in 13 rabbits and of a one-compartment open model in two rabbits after subcutaneous administration, while it was two compartmental in nine and one compartmental in six rabbits after oral administration. The ka values were 0.321, 0.145 and 0.145 min-1 after subcutaneous administration and 0.054, 0.023 and 0.027 min-1 after oral administration. There were no significant differences between the values of Cmax, tmax and AUC calculated by compartmental and non-compartmental analysis.

摘要

在兔皮下和口服给予12.5、16.0和20.0mg/kg三个剂量水平的左旋咪唑后,测定其生物利用度。经过非房室分析,得到的平均值为:皮下给药各剂量时,Cmax分别为3.54、4.51和5.39微克/毫升;tmax分别为12.0、22.0和20.0分钟;F分别为134.8%、105.4%和124.1%;口服给药时,Cmax分别为0.71、1.32和1.77微克/毫升;tmax分别为46.0、96.0和84.0分钟;F分别为53.0%、62.0%和80.7%。除12.5mg/kg剂量的tmax外,两种给药途径的吸收程度和速率有显著差异。经过房室分析,皮下给药后,13只兔的左旋咪唑药代动力学符合二室开放模型,2只兔符合一室开放模型;口服给药后,9只兔符合二室模型,6只兔符合一室模型。皮下给药后的ka值分别为0.321、0.145和0.145分钟-1,口服给药后的ka值分别为0.054、0.023和0.027分钟-1。房室分析和非房室分析计算得到的Cmax、tmax和AUC值之间无显著差异。

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