比较注射用妥曲珠利-格列齐特和口服妥曲珠利+注射用格列齐特在仔猪中的应用:血液活性和药代动力学。

IF 1.5 4区 农林科学 Q3 PHARMACOLOGY & PHARMACY
Hamadi Karembe, Anne Geneteau, Sandrine Lacoste, Nathalie Varinot, Reynald Magnier, Evelyne Coussanes, Santiago Lopez, Daniel Sperling, Mathieu Peyrou
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引用次数: 0

摘要

缺铁性贫血(IDA)和囊虫病是快速生长仔猪最常见的临床症状。迄今为止,IDA 和囊虫病一直是通过肌肉注射铁复合物(如右旋糖酐或格列铁酮)和口服妥曲珠利来治疗的。最近,一种含有托曲唑脲和格列铁酮的新型肌肉注射复合制剂(Forceris®)获得了注册。本研究旨在比较哺乳仔猪口服(Baycox®)或肌肉注射(Forceris®,一种妥曲珠利-铁复方产品)20 毫克/千克妥曲珠利及其主要代谢物妥曲珠利砜后的药代动力学特征。经口服处理的仔猪还补充了铁(Gleptosil®),并对其血液活性进行了比较。两组仔猪的剂量相当。肌肉注射后的妥曲珠利峰值浓度(Cmax)比口服低 11%(p = .376)。然而,肌肉注射妥曲珠利时,妥曲珠利的暴露量(AUC)显著增加(高出40%)(p = .036)。肌肉注射后,活性代谢物妥曲珠利砜的 Cmax 值和 AUC 值分别高出 39% 和 34% (p = .007 和 0.008)。两组的仔猪都能得到适当的保护,避免感染 IDA。总之,肌肉注射妥曲珠利可提高妥曲珠利的相对生物利用率。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
Comparison of an injectable toltrazuril-gleptoferron and an oral toltrazuril + injectable gleptoferron in piglets: Hematinic activities and pharmacokinetics.

Iron deficiency anemia (IDA) and cystoisosporosis are the most common clinical conditions of fast-growing piglets. Until now, IDA and cystoisosporosis have been managed by intramuscular injection of iron complexes (such as dextran or gleptoferron) and oral administration of toltrazuril. Recently, a new combination product containing toltrazuril and gleptoferron for intramuscular application (Forceris®) has been registered. The objective of this study was to compare the pharmacokinetic profiles of toltrazuril and its main metabolite, toltrazuril sulfone, following a single oral (Baycox®) or intramuscular (Forceris®, a toltrazuril-iron combination product) administration at 20 mg/kg to young suckling piglets. The orally treated piglets were also supplemented with iron (Gleptosil®), and the hematinic activities were compared. Piglets in both groups received comparable doses. The peak concentration (Cmax) of toltrazuril after intramuscular administration was 11% lower than that after oral administration (p = .376). However, the exposure to toltrazuril (AUC) was significantly increased (40% higher) when toltrazuril was administered intramuscularly (p = .036). The Cmax and AUC values of the active metabolite, toltrazuril sulfone were 39% and 34% higher, respectively, after intramuscular administration (p = .007 and 0.008, respectively). Piglets in both groups were properly protected against IDA. In conclusion, a higher relative bioavailability of toltrazuril is observed when toltrazuril is administered intramuscularly.

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来源期刊
CiteScore
3.10
自引率
15.40%
发文量
69
审稿时长
8-16 weeks
期刊介绍: The Journal of Veterinary Pharmacology and Therapeutics (JVPT) is an international journal devoted to the publication of scientific papers in the basic and clinical aspects of veterinary pharmacology and toxicology, whether the study is in vitro, in vivo, ex vivo or in silico. The Journal is a forum for recent scientific information and developments in the discipline of veterinary pharmacology, including toxicology and therapeutics. Studies that are entirely in vitro will not be considered within the scope of JVPT unless the study has direct relevance to the use of the drug (including toxicants and feed additives) in veterinary species, or that it can be clearly demonstrated that a similar outcome would be expected in vivo. These studies should consider approved or widely used veterinary drugs and/or drugs with broad applicability to veterinary species.
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