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In vivo exposure of Albendazole sulphoxide by Haemonchus contortus and correlation between plasma and target tissue or gastrointestinal content dispositions in goats
Journal of Veterinary Pharmacology and Therapeutics ( IF 1.5 ) Pub Date : 2021-04-24 , DOI: 10.1111/jvp.12974
Cengiz Gokbulut 1 , Veli Y Cirak 2 , Suleyman Aypak 3 , Hamdi Avci 4 , Selim Sekkin 5 , Hande S Yalinkilinc 5 , Buket Boga 3 , Erol Ayaz 6
Affiliation  

Sheep and goats are sharing different helminth parasites including Haemonchus contortus. Control of these helminths is based mainly on the use of anthelmintics. However, in goats, the application of anthelmintics is often carried out mainly at dosages determined for sheep without knowing the real effects and metabolism features. One of the several anthelmintic classes used against these parasites is (pro) benzimidazoles which are still widely in use in small ruminants in many countries. The objective of this study was to determine (i) the correlation between plasma and tissue or gastrointestinal content dispositions of ricobendazole (RBZ) in goats and (ii) the in vivo exposure of ricobendazole by Hcontortus. Ten goats were experimentally infected with 10,000 larvae of Hcontortus. Four weeks of post-infection, the animals received RBZ subcutaneously at 5 mg/kg body weight. Two goats were sacrificed per time at 1, 2, 4, 6 and 12 h after drug administration and, blood, bile, urine, liver, lung, muscle and kidney gastrointestinal tissues/fluids were collected. Adult Hcontortus were collected from abomasum, and all samples were analysed by HPLC system. Ricobendazole (RBZ) and its sulphone metabolite were extensively excreted by urine and distributed to all tissues and digestive tract, mainly into the abomasum fluid. RBZ concentration in the lung and ABZSO2 in the kidney were relatively higher than those of other tissues, respectively. The parent drug and its metabolite were recovered in both male and female Hcontortus. This study indicates that in goats the plasma concentration profiles of RBZ are strongly correlated with those achieved in different target tissues or fluids, which in turn, reflect the amount of drug taken up by parasites.

中文翻译:

阿苯达唑亚砜在山羊体内暴露以及血浆与靶组织或胃肠道内容物分布之间的相关性

绵羊和山羊共享不同的蠕虫寄生虫,包括Haemonchus contortus。控制这些蠕虫主要基于使用驱虫药。然而,在山羊中,驱虫药的应用通常主要是在为绵羊确定的剂量下进行,而不知道真正的效果和代谢特征。用于对抗这些寄生虫的几种驱虫剂之一是(亲)苯并咪唑,它在许多国家仍广泛用于小型反刍动物。本研究的目的是确定 (i) 山羊体内 ricobendazole (RBZ) 的血浆与组织或胃肠道内容物分布之间的相关性,以及 (ii) H体内 ricobendazole 的暴露。 扭曲. 10 只山羊实验感染了 10,000 只H幼虫。 扭曲。感染后 4 周,动物皮下接受 5mg/kg 体重的 RBZ。在给药后1、2、4、6和12小时,每次处死两只山羊,并收集血液、胆汁、尿液、肝、肺、肌肉和肾胃肠组织/液体。成人H线虫从皱胃收集,并且所有样品通过HPLC系统进行分析。利康苯达唑(RBZ)及其砜代谢物通过尿液广泛排泄,分布于各组织和消化道,主要进入真胃液。肺中的 RBZ 浓度和 ABZSO 2在肾脏中分别相对高于其他组织。在雄性和雌性H 中均回收到母体药物及其代谢物。 扭曲。该研究表明,山羊的 RBZ 血浆浓度曲线与不同靶组织或体液中达到的浓度密切相关,这反过来又反映了寄生虫吸收的药物量。
更新日期:2021-04-24
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