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单端孢霉烯族霉菌毒素T-2毒素的尿液代谢物T-2四醇在犬体内的药代动力学

Pharmacokinetics of T-2 tetraol, a urinary metabolite of the trichothecene mycotoxin, T-2 toxin, in dog.

作者信息

Sintov A, Bialer M, Yagen B

机构信息

Department of Pharmacy, School of Pharmacy, Hebrew University, Jerusalem, Israel.

出版信息

Xenobiotica. 1987 Aug;17(8):941-50. doi: 10.3109/00498258709044192.

Abstract
  1. The urinary metabolites of T-2 toxin were identified and analysed quantitatively after i.v. administration to dogs. 2. A new routine assay for T-2 tetraol was developed and a pharmacokinetic study was carried out on this final hydrolytic metabolite of T-2 toxin. T-2 tetraol was excreted in urine for 2-3 days. Its 'sigma minus' plot demonstrated a significantly longer apparent half-life than its precursors (T-2 toxin and HT-2 toxin). This fact was explained by extraplasma binding causing prolongation of the metabolism and excretion of T-2 toxin metabolites. 3. The urinary metabolites of T-2 toxin were: HT-2 toxin, T-2 triol and T-2 tetraol. The metabolites were excreted in free and conjugated forms. In two dogs T-2 toxin was found in the urine in an amount which accounts for 3.2 and 16% of the administered dose respectively. The cumulative amount of the identified metabolites and toxins formed in the urine ranged from 9.7 to 17.3% in four dogs and 44.7% in one dog.
摘要
  1. 给犬静脉注射T-2毒素后,对其尿液代谢产物进行了鉴定和定量分析。2. 开发了一种新的T-2四醇常规检测方法,并对T-2毒素的这种最终水解代谢产物进行了药代动力学研究。T-2四醇在尿液中排泄2至3天。其“sigma减”图显示其表观半衰期明显长于其前体(T-2毒素和HT-2毒素)。这一事实可通过血浆外结合导致T-2毒素代谢产物的代谢和排泄延长来解释。3. T-2毒素的尿液代谢产物为:HT-2毒素、T-2三醇和T-2四醇。这些代谢产物以游离和结合形式排泄。在两只犬的尿液中发现了T-2毒素,其含量分别占给药剂量的3.2%和16%。在四只犬中,尿液中鉴定出的代谢产物和毒素的累积量在9.7%至17.3%之间,在一只犬中为44.7%。

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