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Plasma concentrations of itraconazole following a single oral dose in juvenile California sea lions (Zalophus californianus).
Journal of Veterinary Pharmacology and Therapeutics ( IF 1.5 ) Pub Date : 2020-04-14 , DOI: 10.1111/jvp.12865
Gregory Scott 1, 2 , Cara L Field 3 , Mark G Papich 4 , Craig A Harms 1, 2
Affiliation  

The objective of this study was to establish a single‐dose pharmacokinetic profile for orally administered itraconazole in California sea lions (Zalophus californianus ). Twenty healthy rehabilitated juvenile California sea lions were included in this study. Itraconazole capsules were administered orally with food at a target dose of 5–10 mg/kg. Blood samples were collected from each animal at 0 hr and at two of the following timepoints: 0.5, 1, 2, 4, 6, 8, 12, 24, 48, and 72 hr. Quantitative analysis of itraconazole in plasma samples was performed by high‐performance liquid chromatography. An average maximum concentration of 0.22 µg/ml ± 0.11 was detected 4 hr after administration. The average concentration fell to 0.12 µg/ml ± 0.11 by 6 hr and 0.02 µg/ml ± 0.02 at 12 hr. At no point did concentrations reach 0.5 µg/ml, the concentration commonly accepted for therapeutic efficacy. While this formulation was well tolerated by the sea lions, oral absorption was poor and highly variable among individuals. These data indicate that a single oral dose of itraconazole given as a capsule at 5–10 mg/kg, under the conditions used in this study, does not achieve therapeutic plasma concentrations in California sea lions.

中文翻译:

加利福尼亚加利福尼亚海狮(Zalophus californianus)的单次口服剂量后伊曲康唑的血浆浓度。

这项研究的目的是为加利福尼亚海狮(Zalophus californianus)口服伊曲康唑建立单剂量药代动力学特征)。这项研究包括了二十只健康的加州少年海狮。伊曲康唑胶囊与食物一起口服,目标剂量为5-10 mg / kg。在0小时和以下两个时间点从每只动物采集血样:0.5、1、2、4、6、8、12、24、48和72小时。通过高效液相色谱法对血浆样品中伊曲康唑进行定量分析。给药4小时后,平均最大浓度为0.22 µg / ml±0.11。到6小时时,平均浓度降至0.12 µg / ml±0.11;到12小时时,平均浓度降至0.02 µg / ml±0.02。浓度没有达到0.5 µg / ml,该浓度通常被认为是治疗功效。虽然这种配方对海狮有很好的耐受性,但口服吸收差,个体之间差异很大。
更新日期:2020-04-14
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