title: Quantification of three lidocaine metabolites and their conjugates.
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 beta-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 beta-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%).
authors.affiliation: Faculty of Pharmacy and Pharmaceutical Sciences, University of Alberta, Edmonton, Canada.
authors.forename: Y K
authors.initials: YK
authors.lastname: Tam
authors.forename: J
authors.initials: J
authors.lastname: Ke
authors.forename: R T
authors.initials: RT
authors.lastname: Coutts
authors.forename: D G
authors.initials: DG
authors.lastname: Wyse
authors.forename: M R
authors.initials: MR
authors.lastname: Gray
mesh_terms: D000082:Acetaminophen / Q000031:analogs & derivatives* / Q000378:metabolism; D002623:Chemistry Techniques, Analytical / Q000379:methods; D004355:Drug Stability; D005965:Glucuronates / Q000378:metabolism; D005966:Glucuronidase / Q000378:metabolism; D006801:Humans; D006868:Hydrolysis; D008012:Lidocaine / Q000031:analogs & derivatives* / Q000378:metabolism*; D013431:Sulfates / Q000378:metabolism
chemical_list: D005965:Glucuronates; D013431:Sulfates; D000082:Acetaminophen; C045360:2,6-dimethylacetaminophen; D008012:Lidocaine; C001306:glycinexylidide; C001173:monoethylglycinexylidide; D005966:Glucuronidase