Stereoselective degradation kinetics of tebuconazole in rabbits.
Stereoselective degradation kinetics of tebuconazole in rabbits.
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DOI：
10.1002/chir.20340
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发表时间：
2007-02
期刊：
影响因子：
2
通讯作者：
Wentao Zhu;J. Qiu;Ziheng Dang;Chunguang Lv;Guifang Jia;Li Li-Li;Zhiqiang Zhou
中科院分区：
文献类型：
--
作者：
Wentao Zhu;J. Qiu;Ziheng Dang;Chunguang Lv;Guifang Jia;Li Li-Li;Zhiqiang Zhou
戊唑醇[（RS）-1-p-氯苯基-4，4-二甲基-3-（1H-1，2，4-三唑-1-基甲基）戊-3-醇]是一种有效的三唑类杀菌剂，由一对对对映体组成。研究了戊唑醇在家兔体内的对映体选择性降解动力学。采用纤维素-三（3，5-二甲基苯基氨基甲酸酯）为手性固定相的高效液相色谱法测定血浆和组织中（-）-（R）-戊唑醇和（+）-（S）-戊唑醇的浓度。开发并验证了血浆和组织中该杀真菌剂的对映选择性分析方法。两种对映体在0.25-25 mg/l浓度范围内线性良好。外消旋戊唑醇在大鼠体内的降解符合准一级动力学，外消旋戊唑醇给药后，（+）-（S）-戊唑醇的降解速度远快于（-）-（R）-戊唑醇。本研究还表明，可能需要对戊唑醇的对映体降解进行环境评估，以充分评估戊唑醇的使用风险。
Tebuconazole[(RS)-1-p-chlorophenyl-4,4-dimethyl-3-(1H-1,2,4-triazol-1-ylmethyl)pentan-3-ol] is a potent triazole fungicide and consists of a pair of enantiomers. The enantioselective degradation kinetics of tebuconazole was investigated in rabbits by intravenous (iv) injection. The concentrations of (-)-(R)-tebuconazole and (+)-(S)-tebuconazole in plasma and tissues were determined by HPLC with a cellulose tris(3,5-dimethylphenylcarbamate)-based chiral stationary phase. Enantioselective analysis methods for this fungicide in plasma and tissues were developed and validated. Good linearities were obtained over the concentration range of 0.25-25 mg/l for both enantiomers. The degradation followed pseudo-first-order kinetics and the degradation of the (+)-(S)-tebuconazole was much faster than that of the (-)-(R)-tebuconazole in plasma after administration of racemic tebuconazole. This study also indicated that environmental assessment of enantiomeric degradation may be needed to fully evaluate risks of tebuconazole use.