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Relative bioavailability and comparative clinical efficacy of different ivermectin oral formulations in lambs

机译:伊维菌素口服制剂在羔羊中的相对生物利用度和临床疗效比较

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摘要

BackgroundSeveral oral ivermectin (IVM) formulations for use in sheep are available in the pharmaceutical veterinary market in different countries. All of them are indicated at the same dose rate to treat the gastrointestinal nematodes. However, there is a lack of information on the relative systemic exposure (plasma bioavailability) and clinical efficacy among oral formulations routinely used in sheep. The main goal of the work reported here was to perform a pharmaco-parasitological assessment of three different IVM oral formulations in lambs infected with multiple resistant gastrointestinal nematodes. The comparative drug systemic exposure (IVM plasma concentrations) and nematodicidal efficacies (clinical efficacy) in lambs were determined for a reference (RF) and two different test (T1, T2) IVM oral formulations. One hundred and fifty six (n= 156) healthy Corriedale lambs, naturally infected with multiple resistant gastrointestinal nematodes were allocated into four experimental groups (n=39). Animals in each group received treatment (200 μg/kg) with either the RF, one of the test IVM formulations or were kept as untreated control. Blood samples were collected over 15 days post-treatment (n=8). The IVM plasma concentrations were measured by high performance liquid chromatography with fluorescence detection. The faecal nematode egg count reduction test (FECRT) (n=39) and evaluation of the clinical efficacy were performed at day 14 post-treatment (n=6), where a predominance of IVM highly resistant nematodes was observed.
机译:背景技术用于绵羊的几种口服伊维菌素(IVM)制剂可在不同国家的兽药市场上买到。所有这些都以相同的剂量使用,以治疗胃肠道线虫。然而,在绵羊常规使用的口服制剂中,缺乏相对的全身暴露(血浆生物利用度)和临床功效方面的信息。此处报道的工作的主要目的是对感染了多种耐药胃肠道线虫的羔羊进行三种不同的IVM口服制剂的药理寄生虫学评估。针对参考(RF)和两种不同的测试(T1,T2)IVM口服制剂,确定了羔羊的比较药物全身暴露(IVM血浆浓度)和杀线虫功效(临床功效)。将一百五十六只(n = 156)健康的Corriedale羔羊自然感染了多种抗性胃肠道线虫,将其分为四个实验组(n = 39)。每组中的动物接受RF,一种测试IVM制剂的治疗(200μg/ kg),或作为未经治疗的对照。在治疗后的15天内收集血液样本(n = 8)。通过具有荧光检测的高效液相色谱法测量IVM血浆浓度。粪便线虫卵数减少试验(FECRT)(n = 39)和临床疗效评估是在治疗后第14天(n = 6)进行的,其中观察到了IVM高抗性线虫的优势。

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