M. Ahmadi et al., METABOLISM OF BECLAMIDE AFTER A SINGLE ORAL DOSE IN MAN - QUANTITATIVE STUDIES, Journal of Pharmacy and Pharmacology, 47(10), 1995, pp. 876-878
A simple reverse phase HPLC assay is described for the determination o
f the anticonvulsant compound, beclamide and its 3- and 4-hydroxypheny
l metabolites in urine. Following oral administration of 1 g beclamide
to a panel of healthy volunteers, less than 0.4% of the dose was excr
eted unchanged in the 24-h urine and unconjugated 3- and 4-hydroxyphen
yl metabolites were not detected. Based on examination of the urine af
ter incubation with beta-glucuronidase and aryl sulphatase, it was fou
nd that these hydroxyl metabolites were excreted as both glucuronide a
nd sulphate conjugates. For each metabolite the glucuronide was the ma
jor excretory product (approximately 10:1). The 24-h excretion of the
combined conjugated metabolites was 7% (for the 3-hydroxy metabolite)
and 24% (for the 4-hydroxy metabolite) of the dose. Approximately 22%
of the administered dose of beclamide was excreted as hippuric acid. I
n view of the simplicity of assay, beclamide may be a useful tool subs
tance with which to examine factors influencing the xenobiotic metabol
ic pathways of benzene ring hydroxylation and glucuronide and sulphate
conjugation in man.