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柚皮苷(一种潜在的镇咳药)在大鼠重复口服 184 天后的毒代动力学。

Toxicokinetics of naringin, a putative antitussive, after 184-day repeated oral administration in rats.

机构信息

Guangzhou Quality R&D Center of Traditional Chinese Medicine, School of Life Sciences, Sun Yat-sen University, Guangzhou 510275, China.

出版信息

Environ Toxicol Pharmacol. 2011 May;31(3):485-9. doi: 10.1016/j.etap.2011.01.006. Epub 2011 Feb 4.

Abstract

The toxicokinetic characteristics of naringin were investigated in rats that had been orally administered naringin extract, a candidate for oral treatment of cough, prepared from Citrus grandis "Tomentosa", at 50, 250, or 1250 mg/kg/day in a repeated-dose study for 1, 32, 93, or 184 days. Increased values of the mean systemic exposure were approximately proportional to increases in dose levels during all collection intervals; no saturation was observed. No significant differences in mean systemic exposure were observed between male and female rats. Results provide a reference for interpretation of toxicology findings and relevance to clinical safety issues.

摘要

在一项重复剂量研究中,大鼠经口给予柚皮苷提取物(一种治疗咳嗽的口服候选药物,源自‘Tomentosa’柚子),剂量分别为 50、250 或 1250mg/kg/天,连续给药 1、32、93 或 184 天,考察柚皮苷的毒代动力学特征。在所有采集时间间隔内,平均系统暴露的增加值与剂量水平的增加大致成正比;未观察到饱和现象。雌雄大鼠之间的平均系统暴露无显著差异。研究结果为毒理学发现的解释和与临床安全性问题的相关性提供了参考。

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