Abstract
A method has been developed to quantify three lidocaine metabolites, N-ethylglycyl-2,6-xylidide (MEGX), glycyl-2,6-xylidide (GX), and 4-hydroxy-2,6-xylidine (4-OH-XY), and their conjugates in pooled human urine using enzymic hydrolysis. The commonly used enzymes, pure β-glucuronidase, sulfatase, and a mixture of the two, were tested for their efficiencies in hydrolyzing the conjugates. Initially, it was found that 4-OH-XY was highly unstable after it was released from conjugates by β-glucuronidase and the enzyme mixture. This problem was corrected by purging the sample with nitrogen prior to incubation. It has been determined that 4-OH-XY is present in human urine exclusively as its glucuronide. The percentage of MEGX in free and in conjugated forms (glucuronide, sulfate, and others) are 44.9 ± 6.8,16.6 ± 4.5, 6.6 ± 1.8, and 31.9 ± 4.4, respectively. GX was present mostly in the free form (90.6 ± 10.5%).
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Tam, Y.K., Ke, J., Coutts, R.T. et al. Quantification of Three Lidocaine Metabolites and Their Conjugates. Pharm Res 7, 504–507 (1990). https://doi.org/10.1023/A:1015868800614
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DOI: https://doi.org/10.1023/A:1015868800614