Determination of Girisopam (2,3-Benzodiazepine Compound) and Its Four Metabolites in Human and Rat Plasma by Gradient RP-HPLC Method

Autor: Imre Klebovich, I. Ürmös, Katalin Balogh Nemes
Rok vydání: 1998
Předmět:
Zdroj: Journal of Liquid Chromatography & Related Technologies. 21:803-818
ISSN: 1520-572X
1082-6076
DOI: 10.1080/10826079808000510
Popis: A gradient RP-HPLC bioanalytical method has been developed for the human pharmacokinetic studies of girisopam, the new 2,3-benzodiazepine compound with anxiolytic effect that has no myorelaxant and anticonvulsive side effects. The compound is an analogue of tofizopam (Grandaxin®, EGIS Pharmaceuticals Ltd., Budapest, Hungary). The method was found to be appropriate for the purposes of human pharmacokinetic studies performed at 25, 50, 100, 200, 325, and 525 mg dose levels. The method allowed the simultaneous determination of girisopam (G) and its four metabolites (4′-hydroxy-G, 7-demethyl-G, 4-hydroxymethyl-G and 4-demethyl-4-oxo-G) identified in previous studies in human plasma. The solutes were separated on Hypersil BDS C18 column and quantified by UV detection at 238 nm. A solid phase extraction (SPE) method using reversed-phase cartridges was developed for sample processing, whereby girisopam and the much more polar metabolites, as well as the internal standard could be extracted in a single s...
Databáze: OpenAIRE