Simultaneous quantification of cycloserine and its prodrug acetylacetonylcycloserine in plasma and urine by high-performance liquid chromatography using ultraviolet absorbance and fluorescence after post-column derivatization.

D-Cycloserine is a broad-spectrum antibiotic used with other antibiotics to treat various forms of tuberculosis. Its prodrug sodium (R)-4-[(1-methyl-3-oxo-1-butenyl)amino]-3-isoxazolidinone hemihydrate, developed for better aqueous stability and solubility, is combined with another broad-spectrum antibiotic, fludalanine. An ion-pair, reversed-phase high-performance liquid chromatographic assay has been developed to simultaneously detect cycloserine and its prodrug in plasma and urine. The prodrug is detected directly by ultraviolet absorbance and cycloserine by fluorescence following post-column derivatization.