Lai Olimpia, Belloli Chiara, Crescenzo Giuseppe, Carofiglio Vito, Ormas Paolo, Marangi Oronzo, Cagnardi Petra
Department of Animal Health and Welfare, Faculty of Veterinary Medicine, University of Bari, Valenzano, Italy.
Vet Hum Toxicol. 2002 Apr;44(2):79-83.
The residual depletion of a commercial product containing imidocarb dipropionate in sheep and goat tissues was investigated. Additionally, the oral bioavailability of residues was determined in rats to evaluate the extent to which tissue imidocarb residues could be reabsorbed by consumers. Ten ewes and 5 goats were administered im with a commercial formulation containing imidocarb dipropionate (Carbesia cavalli, Shering-Ploug 121.15 mg/ml) at the single dose of 3 mg/kg bw corresponding to 2.1 mg/kg bw imidocarb base. Two sheep and 1 goat were slaughtered 15, 30, 60, 90 or 120 d after dosing and samples of muscle, injection site muscle, liver, omental and subcutaneous fat, and kidneys were collected. Samples of cerebral hemisphere, cerebellum, olfactory bulb, pineal and pituitaryglands were dissected. For the residue bioavailability study 7 groups of3 Wistar rats each, were dosed by gavage with imidocarb dipropionate standard in water (group 2, 3 and 4) or with imidocarb as a liver residue collected from prior dosed animals (group 5, 6 and 7) at 8.4. 16.8 or 33.6 microg/kg of imidocarb base respectively, for 5 d. Group I was control. All animals were sacrificed the day after the last drug administration and livers were collected. The highest drug levels in sheep and goats occurred in liver and kidney, suggesting that these tissues are targets for residues; muscle had negligible importance as storage tissue. Goats had a lower storage capability than sheep. The residue profile in sheep liver and omental fat showed a 30-d storage period to reach maximum concentrations, and suggested that imidocarb is redistributed. The high and long-lasting concentrations in brain showed its capacity to cross the blood-brain barrier and caused concern for potential neurotoxic effects. Detectable concentrations of imidocarb were not found in rat liver.
对含有双丙酸咪唑苯脲的商业产品在绵羊和山羊组织中的残留消除情况进行了研究。此外，在大鼠中测定了残留物的口服生物利用度，以评估组织中的咪唑苯脲残留物被消费者重新吸收的程度。给10只母羊和5只山羊肌肉注射含有双丙酸咪唑苯脲的商业制剂（Carbesia cavalli，先灵葆雅，121.15毫克/毫升），单剂量为3毫克/千克体重，相当于2.1毫克/千克体重的咪唑苯脲碱。给药后15、30、60、90或120天宰杀2只绵羊和1只山羊，采集肌肉、注射部位肌肉、肝脏、网膜和皮下脂肪以及肾脏样本。解剖采集大脑半球、小脑、嗅球、松果体和垂体样本。在残留生物利用度研究中，7组Wistar大鼠，每组3只，分别以8.4、16.8或33.6微克/千克体重的咪唑苯脲碱经口灌胃给予水中的双丙酸咪唑苯脲标准品（第2、3和4组）或从先前给药动物收集的肝脏残留物中的咪唑苯脲（第5、6和7组），持续5天。第1组为对照组。在最后一次给药后次日处死所有动物并采集肝脏。绵羊和山羊体内药物水平最高的是肝脏和肾脏，表明这些组织是残留物的靶器官；肌肉作为储存组织的重要性可忽略不计。山羊的储存能力低于绵羊。绵羊肝脏和网膜脂肪中的残留分布显示，达到最大浓度的储存期为30天，表明咪唑苯脲会重新分布。大脑中高浓度且持久的药物表明其能够穿过血脑屏障，并引发了对潜在神经毒性作用的担忧。在大鼠肝脏中未检测到可检测浓度的咪唑苯脲。
