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伊维菌素新型制剂给山羊给药后的药代动力学

Pharmacokinetics of a novel formulation of ivermectin after administration to goats.

作者信息

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

机构信息

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

出版信息

Am J Vet Res. 2006 Feb;67(2):323-8. doi: 10.2460/ajvr.67.2.323.

Abstract

OBJECTIVE

To evaluate the pharmacokinetics of a novel commercial formulation of ivermectin after administration to goats.

ANIMALS

6 healthy adult goats.

PROCEDURE

Ivermectin (200 microg/kg) was initially administered IV to each goat, and plasma samples were obtained for 36 days. After a washout period of 3 weeks, each goat received a novel commercial formulation of ivermectin (200 microg/kg) by SC injection. Plasma samples were then obtained for 42 days. Drug concentrations were quantified by use of high-performance liquid chromatography with fluorescence detection.

RESULTS

Pharmacokinetics of ivermectin after IV administration were best described by a 2-compartment open model; values for main compartmental variables included volume of distribution at a steady state (9.94 L/kg), clearance (1.54 L/kg/d), and area under the plasma concentration-time curve (AUC; 143 [ng x d]/mL). Values for the noncompartmental variables included mean residence time (7.37 days), AUC (153 [ng x d]/mL), and clearance (1.43 L/kg/d). After SC administration, noncompartmental pharmacokinetic analysis was conducted. Values of the variables calculated by use of this method included maximum plasma concentration (Cmax; 21.8 ng/mL), time to reach Cmax (3 days), and bioavailability (F; 91.8%).

CONCLUSIONS AND CLINICAL RELEVANCE

The commercial formulation used in this study is a good option to consider when administering ivermectin to goats because of the high absorption, which is characterized by high values of F. In addition, the values of Cmax and time to reach Cmax are higher than those reported by other investigators who used other routes of administration.

摘要

目的

评估一种新型伊维菌素商业制剂在山羊给药后的药代动力学。

动物

6只健康成年山羊。

程序

首先给每只山羊静脉注射伊维菌素(200微克/千克),并采集血浆样本36天。经过3周的洗脱期后,每只山羊通过皮下注射接受一种新型伊维菌素商业制剂(200微克/千克)。然后采集血浆样本42天。使用带荧光检测的高效液相色谱法定量药物浓度。

结果

静脉给药后伊维菌素的药代动力学最好用二室开放模型描述;主要房室变量的值包括稳态分布容积(9.94升/千克)、清除率(1.54升/千克/天)和血浆浓度-时间曲线下面积(AUC;143[纳克×天]/毫升)。非房室变量的值包括平均驻留时间(7.37天)、AUC(153[纳克×天]/毫升)和清除率(1.43升/千克/天)。皮下给药后,进行非房室药代动力学分析。使用该方法计算的变量值包括最大血浆浓度(Cmax;21.8纳克/毫升)、达到Cmax的时间(3天)和生物利用度(F;91.8%)。

结论及临床意义

本研究中使用的商业制剂是给山羊使用伊维菌素时可考虑的一个好选择,因为其吸收良好,表现为F值较高。此外,Cmax和达到Cmax的时间值高于其他采用其他给药途径的研究者所报告的值。

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