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伊维菌素商业制剂皮下注射给绵羊后的生物利用度。

Bioavailability of a commercial formulation of ivermectin after subcutaneous administration to sheep.

作者信息

Canga Aranzazu Gonzalez, Sahagun Ana, Diez M Jose, Fernandez Nelida, Sierra Matilde, Garcia Juan J

机构信息

Department of Pharmacology and Toxicology, Veterinary Faculty, University of León, Campus de Vegazana s/n 24071, León, Spain.

出版信息

Am J Vet Res. 2007 Jan;68(1):101-6. doi: 10.2460/ajvr.68.1.101.

Abstract

OBJECTIVE

To evaluate bioavailability and other pharmacokinetic variables of a commercial formulation of ivermectin after IV administration to sheep.

ANIMALS

6 healthy adult sheep.

PROCEDURES

A single dose of a commercial formulation of ivermectin (200 microg/kg) was administered IV to each sheep. After a washout period of 3 weeks, each sheep was administered ivermectin by SC injection. Plasma samples were obtained for up to 36 and up to 42 days after IV and SC administration, respectively. Ivermectin concentrations were quantified by use of high-performance liquid chromatography with fluorescence detection.

RESULTS

Results obtained indicated that after IV administration, ivermectin is cleared slowly from plasma, tends to distribute and accumulate in the peripheral compartment, and is slowly eliminated from the body. After SC administration, noncompartmental analysis revealed that bioavailability of ivermectin is nearly complete (98.20%), has a slow mean absorption time of 0.96 days, and reaches a maximum plasma concentration of 19.55 ng/mL at 3.13 days.

CONCLUSIONS AND CLINICAL RELEVANCE

The commercial formulation of ivermectin used in this study can be administered SC to sheep on the basis of a nearly complete bioavailability. In addition, the maximum plasma concentration and interval from SC injection until maximum plasma concentration is obtained are higher than those reported by other authors who used other routes of administration.

摘要

目的

评估伊维菌素商业制剂静脉注射给绵羊后的生物利用度及其他药代动力学变量。

动物

6只健康成年绵羊。

方法

给每只绵羊静脉注射单剂量伊维菌素商业制剂(200微克/千克)。经过3周的洗脱期后,给每只绵羊皮下注射伊维菌素。分别在静脉注射和皮下注射后长达36天和42天采集血浆样本。使用带荧光检测的高效液相色谱法定量伊维菌素浓度。

结果

所得结果表明,静脉注射后,伊维菌素从血浆中清除缓慢,倾向于在外周室分布和蓄积,且从体内缓慢消除。皮下注射后,非房室分析显示伊维菌素的生物利用度几乎完全(98.20%),平均吸收时间缓慢,为0.96天,在3.13天时达到最大血浆浓度19.55纳克/毫升。

结论及临床意义

本研究中使用的伊维菌素商业制剂基于几乎完全的生物利用度可皮下注射给绵羊。此外,最大血浆浓度以及从皮下注射到获得最大血浆浓度的间隔时间高于其他采用其他给药途径的作者所报告的数值。

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