Davi H, Guyonnet J, Necciari J, Cautreels W
J Chromatogr. 1985 Jul 12;342(1):159-65. doi: 10.1016/s0378-4347(00)84498-9.
Circulating ethyl loflazepate metabolites in the baboon were determined, following a single oral administration of the 14C-labelled drug, by radio-high-performance liquid chromatography with injection of crude plasma samples and by selective extraction with thin-layer chromatographic analysis of the radioactive components. Metabolites identified by comparing their chromatographic behaviour with synthetic standards were loflazepate, descarboxyloflazepate and 3-hydroxydescarboxyloflazepate. Loflazepate represented about 70% of the circulating radioactivity; the two other metabolites were present in amounts too small to allow accurate quantification. The parent drug was not present in the blood. Comparison of high-performance liquid chromatography with solvent extraction demonstrated the inaccuracy of the latter to be caused by the conversion of loflazepate to descarboxyloflazepate.
在对狒狒单次口服14C标记的洛氟西泮后，通过对粗血浆样品进行放射性高效液相色谱法以及对放射性成分进行薄层色谱分析的选择性萃取，测定了狒狒体内循环的洛氟西泮乙酯代谢物。通过将其色谱行为与合成标准品进行比较鉴定出的代谢物有洛氟西泮、去羧基洛氟西泮和3-羟基去羧基洛氟西泮。洛氟西泮约占循环放射性的70%；另外两种代谢物的含量过少，无法进行准确定量。血液中不存在母体药物。高效液相色谱法与溶剂萃取法的比较表明，后者的不准确性是由洛氟西泮转化为去羧基洛氟西泮所致。
