Okamoto M, Ide M, Suzuki H, Ishii T, Tamura K, Numata H, Katsumata T, Fujita T
Biology and Zoology Research Center Inc., Shizuoka, Japan.
J Toxicol Sci. 1998 Jul;23 Suppl 3:483-501. doi: 10.2131/jts.23.supplementiii_483.
A 6-month repeated dose toxicity study with 1-month recovery test of sodium N-[2-[4-(2,2-dimethylpropionyloxy) phenylsulfonylamino] benzoyl] aminoacetate tetrahydrate (ONO-5046.Na), a novel neutrophil elastase inhibitor, was conducted in beagle dogs. The dogs of both sexes were administered ONO-5046.Na intravenously at a daily dose of 0 (vehicle control), 7.5, 15 or 30 mg/kg. In the 15 mg/kg and above groups, transient ataxic gait was observed. It is considered that this symptom could be attributed to the pharmacological effect of ONO-5046.Na. Macro- and microscopic hemorrhage at the injection site was observed in the ONO-5046.Na treated groups. However, it is considered that these findings could be attributed to the long-term repeated dosing procedure, and were not toxic changes. There were no treatment-related changes in body weight, food consumption, ophthalmology, urinalysis, hematology, blood chemistry, electrocardiography and organ weights. These results indicate that the NOAEL of ONO-5046.Na in dogs is 30 mg/kg/day for both sexes in this study.
采用新型中性粒细胞弹性蛋白酶抑制剂N-[2-[4-(2,2-二甲基丙酰氧基)苯磺酰氨基]苯甲酰]氨基乙酸钠四水合物(ONO-5046.Na)对比格犬进行了为期6个月的重复给药毒性研究及为期1个月的恢复试验。雌雄犬均静脉注射ONO-5046.Na,日剂量分别为0(溶媒对照)、7.5、15或30mg/kg。在15mg/kg及以上剂量组中,观察到短暂性共济失调步态。认为该症状可能归因于ONO-5046.Na的药理作用。在ONO-5046.Na治疗组中,观察到注射部位出现肉眼可见及显微镜下可见的出血。然而,认为这些发现可能归因于长期重复给药过程,并非毒性变化。在体重、食物消耗、眼科检查、尿液分析、血液学、血液化学、心电图及器官重量方面,未发现与治疗相关的变化。这些结果表明,在本研究中,ONO-5046.Na对犬的无观察到有害作用水平(NOAEL)为雌雄均30mg/kg/天。