Takayama Mariko, Sekiguchi Hiroshi, Hori Yasushi, Fujisawa Manami, Hirose Yasuo
Department of Hospital Pharmacy, Niigata City General Hospital.
Chudoku Kenkyu. 2009 Jun;22(2):113-20.
The symptoms of acute poisoning caused by ingestion of bialaphos (BIAL), an ingredient of herbicide, are supposed to be due to the L-glufosinate (L-GLUF), which is formed by the degradation of bialaphos. To elucidate the pharmacokinetics of BIAL and L-GLUF, we attempted a simultaneous analysis of BIAL and L-GLUF in biological samples by exploiting a reversed phase HPLC method. The derivatization reaction of BIAL and L-GLUF using (+) -1- (9-fluorenyl) ethyl chloroformate was completed in 30 min at 40 degrees C and both derivatives were stable for 48 hr at 25 degrees C. A fluorescence detector were used for HPLC; the exicitation wavelength was set at 265 nm and the emission wavelength at 315 nm. Respective calibration curves prepared by adding BIAL and L-GLUF to serum were linear within ranges of 0.01-10.0 and 0.005-10.0 microg/mL in derivatived liquid samples for introducing into HPLC. The lower limits of detection for BIAL and L-GLUF were 0.005 and 0.001 microg/mL, respectively. An 83-year old male who ingested approximately 350 mL of Herby Liquid, a herbicide containing 18% BIAL and 82% surfactant, in an attempt to commit suicide developed delayed respiratory depression and seizures. L-GLUF was detected in the serum of the patient 2.7 hr after ingestion, but BIAL was not. The change in serum L-GLUF concentration measured over time was consistent with a 2-compartment model, with a distribution half-life of 1.70 hr and an elimination half-life of 6.03 hr.
除草剂成分双丙氨膦（BIAL）引起的急性中毒症状被认为是由双丙氨膦降解形成的L - 草铵膦（L - GLUF）所致。为阐明BIAL和L - GLUF的药代动力学，我们尝试利用反相高效液相色谱法同时分析生物样品中的BIAL和L - GLUF。使用（+）-1 - （9 - 芴基）氯甲酸乙酯对BIAL和L - GLUF进行衍生化反应，在40℃下30分钟内完成，两种衍生物在25℃下48小时内稳定。高效液相色谱使用荧光检测器；激发波长设定为265nm，发射波长设定为315nm。通过向血清中添加BIAL和L - GLUF制备的各自校准曲线在用于引入高效液相色谱的衍生化液体样品中，在0.01 - 10.0和0.005 - 10.0μg/mL范围内呈线性。BIAL和L - GLUF的检测下限分别为0.005和0.001μg/mL。一名83岁男性为自杀企图摄入了约350mL的Herby Liquid除草剂，该除草剂含有18%的BIAL和82%的表面活性剂，出现了延迟性呼吸抑制和癫痫发作。摄入后2.7小时在患者血清中检测到L - GLUF，但未检测到BIAL。随时间测量的血清L - GLUF浓度变化符合二室模型，分布半衰期为1.70小时，消除半衰期为6.03小时。
