Determination of β-carboline derivatives in biological samples by high-performance liquid chromatography with fluorescence detection

✍ Scribed by W. Krause; H. Mengel; L. Nordholm

• Publisher: John Wiley and Sons
• Year: 1989
• Tongue: English
• Weight: 524 KB
• Volume: 78
• Category: Article
• ISSN: 0022-3549
• DOI: 10.1002/jps.2600780804

✦ Synopsis

E l An assay procedure for measuring plasma, urine, and feces levels of seven p-carbolines and possible metabolites is described. The drugs are extracted with diethylether or, alternatively, with a commercially available automated extraction device after adding an appropriate internal standard. Separation from matrix constituents is performed by reversed-phase high-performance liquid chromatography (HPLC) followed by fluorescence detection. The carboxylic acid metabolites of the p-carbolines have to be esterified before HPLC measurement. The detection limits are 0.2 ngimL for p-carbolines and 2 ng/mL for their metabolites. Plasma levels and pharmacokinetic parameters of six different p-carbolines in healthy male volunteers following iv or PO treatment are described. Total clearance ranged from 17 to 52 mliminlkg and the terminal half-life ranged from 1 to 4 h. The absolute bioavailability exhibited a range from <1 to 61%.

R3

R4 R5 R6