ガスクロマトグラフ法による新規抗血小板薬KBT-3022の主代謝物(Desethyl KBT-3022)の血漿中微量定量

概要

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A highly sensitive, accurate and reproducible gas chromatographic method for the determination of a main metabolite, 2-[4,5-bis (4-methoxy-phenyl) thiazol-2-yl] pyrrol-ylacetic acid (desethyl KBT-3022) of a new antiplatelet agent, ethyl 2-[4,5-bis (4-methoxyphenyl) thiazol-2-yl] pyrrol-1-ylacetate (KBT-3022), in the human or dog plasma has been developed. Desethyl KBT-3022 in the plasma was extracted with a mixture of n-hexane and dichloromethane (1 : 1), and was derivatized using pentafluorobenzyl bromide. The obtained pentafluo robenzyl derivative of desethyl KBT-3022 in the plasma was separated by high-performance liquid chromatography. After the separation, the pentafluorobenzyl derivative of desethyl KBT-3022 was detected by gas chromatography. Gas chromatography was performed with a Ultra 1 column (12 m×0.22 mm i. d., film thickness 0.33μm), using an electron capture detector. 2-[2-{4,5-Bis (4-methoxyphenyl) thiazol-2-yl} pyrrol-1-yl] propionic acid was used as an internal standard. The detection limit of desethyl KBT-3022 in the plasma was 0.2 ng/ml. The coefficients of variation were below 5.3%. This method was applied to the determination of the plasma concentration of desethyl KBT-3022 after oral administration of KBT-3022 to dogs.
公益社団法人日本薬学会の論文
1992-06-25