Enantiospecific high-performance liquid chromatographic assay with fluorescence detection for the monoamine oxidase inhibitor tranylcypromine and its applicability in pharmacokinetic studies.

摘要: In order to be able measure low concentrations of tranylcypromine enantiomers in biological material, chiral fluorescent derivatization and high-performance liquid chromatography (HPLC) were employed. The internal standard S-(+)-amphetamine borate-sodium hydroxide buffer pH 11 added plasma or urine sample aliquots. o-Phthaldialdehyde was used for precolumn combination with the mercaptan N-acetylcysteine. HPLC resolution diastereoisomeric derivatives possible on an octadecylsilane column. mobile phase consisted sodium phosphate solution 6.5, methanol tetrahydrofuran. fluorescence eluate monitored at 344/442 nm. intra-day coefficients variation below 10%, limit determination 0.5 ng/ml. assay found applicable routine analyses a preliminary pharmacokinetic study, which oral dose 20 mg racemic sulfate administered three healthy volunteers. generally low, those S-(-)-tranylcypromine significantly exceeded R-(+)-enantiomer. Average maximum 57.5 6.3 ng/ml S- R-tranylcypromine, respectively. While S-tranylcypromine well detectable within whole study period (8 h), R-tranylcypromine fell detection after 4 h two out studied