Chen Jin Hui, Wang Hui Li, Guo Bao Yuan, Xu Peng, Li Jian Zhong
Research Center for Eco-Environmental Sciences, Chinese Academy of Sciences, Beijing, P.R. China.
Chirality. 2013 Dec;25(12):910-6. doi: 10.1002/chir.22233. Epub 2013 Sep 6.
The pharmacokinetics of diniconazole enantiomers in quail (Coturnix coturnix japonica) were investigated by liquid chromatography-tandem mass spectrometry (LC-MS/MS). Quails were exposed to racemic diniconazole in capsule by oral at dose of 10 mg/kg (body weight). The maximal concentrations observed in blood, heart, liver, and kidney were 3.18, 11.35, 12.32, 15.03 µg/g for S-diniconazole, and 1.13, 3.70, 6.00, 2.60 µg/g for R-diniconazole. The elimination of enantiomers all met the one-compartment model in blood, heart, liver, and kidney well. The elimination half-lives (T1/2) of S-diniconazole were 2.87, 3.85, 5.29, and 4.42 h in blood, heart, liver, and kidney, respectively; the T1/2 of R-diniconazole were 2.44, 3.42, 146.23, and 74.02 h in blood, heart, liver, and kidney, respectively. The enantiomer fractions (EFs) steadily increased from 0.50 to 0.92 in blood samples and 0.91 in heart samples. Meanwhile, the values increased to 0.70 and 0.80 in liver and kidney initially, and then decreased to 0.33 and 0.44 at the end of the experiment. Metabolism was examined as well and it was found that diniconazole was metabolized to 1, 2, 4-triazole, (E)-3-(1H-1, 2, 4-triazol-1-yl) acrylaldehyde, (E, S)-(R, S)-4-(2, 4-dichlorophenyl)-2, 2-dimethyl-5-(1H-1, 2, 4-triazol-1-yl) pent-4-ene-1, 3-diol, (E)-4-(2, 4-dichlorophenyl)-3-hydroxy-2, 2-dimethyl-5-(1H-1, 2, 4-triazol-1-yl) pent-4-enoic acid, and 1, 3-dichlorobenzen in all samples of quail.
采用液相色谱 - 串联质谱法（LC-MS/MS）研究了喹禾灵对映体在鹌鹑（日本鹌鹑）体内的药代动力学。鹌鹑经口给予剂量为10 mg/kg（体重）的消旋喹禾灵胶囊。在血液、心脏、肝脏和肾脏中观察到的S-喹禾灵的最大浓度分别为3.18、11.35、12.32、15.03 μg/g，R-喹禾灵的最大浓度分别为1.13、3.70、6.00、2.60 μg/g。对映体在血液、心脏、肝脏和肾脏中的消除均很好地符合一室模型。S-喹禾灵在血液、心脏、肝脏和肾脏中的消除半衰期（T1/2）分别为2.87、3.85、5.29和4.42小时；R-喹禾灵在血液、心脏、肝脏和肾脏中的T1/2分别为2.44、3.42、146.23和74.02小时。对映体分数（EFs）在血液样本中从0.50稳定增加到0.92，在心脏样本中为0.91。同时，在肝脏和肾脏中，该值最初增加到0.70和0.80，然后在实验结束时降至0.33和0.44。还对代谢进行了检测，发现喹禾灵在鹌鹑的所有样本中均代谢为1,2,4-三唑、（E）-3-（1H-1,2,4-三唑-1-基）丙烯醛、（E,S）-（R,S）-4-（2,4-二氯苯基）-2,2-二甲基-5-（1H-1,2,4-三唑-1-基）戊-4-烯-1,3-二醇、（E）-4-（2,4-二氯苯基）-3-羟基-2,2-二甲基-5-（1H-1,2,4-三唑-1-基）戊-4-烯酸和1,3-二氯苯。
