Determination of a New 5-Lipoxygenase Inhibitor, Zileuton, and its Inactive N-Dehydroxylated Metabolite in Plasma by High Performance Liquid Chromatography
| Autor: | R A Braeckman, K A Erdman, G R Granneman |
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| Rok vydání: | 1995 |
| Předmět: |
Metabolite
Hydroxylation Sensitivity and Specificity High-performance liquid chromatography chemistry.chemical_compound Drug Stability Spectrophotometry Blood plasma medicine Animals Humans Hydroxyurea Urea Pharmacology (medical) Lipoxygenase Inhibitors Chromatography High Pressure Liquid Pharmacology Chromatography biology medicine.diagnostic_test Extraction (chemistry) Reproducibility of Results Stereoisomerism Haplorhini Zileuton Reference Standards Rats chemistry Enzyme inhibitor Calibration biology.protein Spectrophotometry Ultraviolet Quantitative analysis (chemistry) medicine.drug |
| Zdroj: | Clinical Pharmacokinetics. 29:1-8 |
| ISSN: | 0312-5963 |
| DOI: | 10.2165/00003088-199500292-00003 |
| Popis: | A rapid and sensitive assay was developed for the measurement of plasma concentrations of zileuton racemate, a potent inhibitor of 5-lipoxygenase. Zileuton and its inactive N-dehydroxylated metabolite were extracted from human, monkey, and rat plasma by use of a solid-phase extraction column (Analytichem Bond Elut). The compounds were then separated by reverse-phase high performance liquid chromatography (HPLC) on a Supelcosil LC-18 column and quantified on the basis of ultraviolet absorption at 260nm relative to an internal standard. The extraction recovery of zileuton, as determined by HPLC assay, was 77.9 +/- 1.7%. Recovery of the metabolite was 85.8 +/- 0.7%. Calibration curves for both compounds were linear over the zileuton concentration range 0.01 to 10.0 mg/L (correlation coefficients0.987), while the intra- and interassay coefficients of variation were15.6%. In practice,97% of blinded daily spiked control samples for zileuton and90% of those for the metabolite were within 10% of their target concentrations. |
| Databáze: | OpenAIRE |
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