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单次口服驱虫药阿苯达唑后其及其主要代谢产物在羊奶及奶制品中的分布情况。

Distribution of the anthelmintic drug albendazole and its major metabolites in ovine milk and milk products after a single oral dose.

作者信息

De Liguoro M, Longo F, Brambilla G, Cinquina A, Bocca A, Lucisano A

机构信息

Dipartimento di Patologia, Profilassi e di Ispezione degli Alimenti, Napoli, Italia.

出版信息

J Dairy Res. 1996 Nov;63(4):533-42. doi: 10.1017/s0022029900032076.

Abstract

The distribution of albendazole (ABZ) and its main metabolites albendazole sulphoxide (ABZSO), albendazole sulphone (ABZSO2) and albendazole 2-aminosulphone (NH2ABZSO2) were investigated in bulk milk and milk products after administration of a single oral dose of the drug (12.5 mg/kg) to 80 Laticauda sheep. An analytical method was developed for this investigation from an existing procedure used for the determination of these compounds in plasma and digesta samples. No traces of the parent compound or NH2ABZSO2 were found in milk or milk products, with the exception of the milk collected 36 h after treatment in which 89 micrograms NH2ABZSO2/kg was detected. Results indicated that ABZ was rapidly oxidized to ABZSO and then to ABZSO2. These metabolites were found at high levels (1-4 mg/kg) in milk collected within 24 h after treatment. Products derived from such milk also contained high concentrations of the two oxidized metabolites, including up to 5 mg ABZSO/kg in Pecorino cheese. Only small quantities of these two metabolites were found in milk collected during the second day after treatment (range 50-500 micrograms/kg). They were no longer detectable in milk collected during the third day after dosing, nor were they found in products made from such milk. These findings confirm that the two polar metabolites ABZSO and ABZSO2 were efficiently excreted from the body. Considering that the established maximum residue limit for ovine milk is 100 micrograms/kg for ABZ plus its metabolites, our results confirmed the appropriateness of the currently prescribed withdrawal time (3 d) after the use of ABZ in lactating sheep. However, considerable levels of ABZSO were detected in milk collected within 24 h after treatment as well as in products and by-products derived from such milk. Owing to the known toxicity of the ABZSO, we stress the need for careful control to ensure adherence to the prescribed withdrawal time.

摘要

给80只蓝灰扁尾海蛇单次口服阿苯达唑(ABZ)(12.5毫克/千克)后,研究了阿苯达唑及其主要代谢产物阿苯达唑亚砜(ABZSO)、阿苯达唑砜(ABZSO2)和阿苯达唑2-氨基砜(NH2ABZSO2)在散装牛奶和奶制品中的分布情况。基于现有的用于测定血浆和消化物样品中这些化合物的方法,开发了一种用于本研究的分析方法。除了治疗后36小时采集的牛奶中检测到89微克NH2ABZSO2/千克外,在牛奶或奶制品中未发现母体化合物或NH2ABZSO2的痕迹。结果表明,ABZ迅速氧化为ABZSO,然后再氧化为ABZSO2。在治疗后24小时内采集的牛奶中发现这些代谢产物的含量很高(1-4毫克/千克)。源自此类牛奶的产品中也含有高浓度的这两种氧化代谢产物,包括佩科里诺奶酪中高达5毫克ABZSO/千克。在治疗后第二天采集的牛奶中仅发现少量的这两种代谢产物(范围为50-500微克/千克)。在给药后第三天采集的牛奶中不再检测到它们,在用此类牛奶制成的产品中也未发现。这些发现证实了两种极性代谢产物ABZSO和ABZSO2能有效地从体内排出。考虑到羊乳中阿苯达唑及其代谢产物的既定最大残留限量为100微克/千克,我们的结果证实了目前规定的泌乳期绵羊使用阿苯达唑后的停药时间(3天)是合适的。然而,在治疗后24小时内采集的牛奶以及源自此类牛奶的产品和副产品中检测到了相当高含量的ABZSO。由于已知ABZSO具有毒性,我们强调需要严格控制,以确保遵守规定的停药时间。

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