Document Detail

High-performance liquid chromatographic analysis of the new antitumour drug N-benzoylstaurosporine (CGP 41 251) and four potential metabolites in micro-volumes of plasma.
MedLine Citation:
PMID:  8833979     Owner:  NLM     Status:  MEDLINE    
A high-performance liquid chromatographic (HPLC) assay is described for the determination of the new antitumour drug N-benzoylstaurosporine (CGP 41 251; I) and four of its potential metabolites in micro-volumes (100 microliters) of plasma. After addition of an internal standard, the compounds were isolated from plasma by liquid-liquid extraction with diisopropyl ether. Chromatography was carried out using a 5 microns LiChrospher C-18 end-capped column (125 x 4.0 mm i.d.) and binary gradient elution with acetonitrile and a triethylamine-containing phosphate buffer (pH 3.6) as solvents. Fluorimetric detection was performed with excitation and emission wavelengths set at 286 and 386 nm, respectively. The absolute recovery was more than 98% for all of the investigated compounds. The limit of detection (LOD) for I and three metabolites was 0.1 ng ml-1 and the lower limit of quantitation (LLQ) was 0.2 ng ml-1 in 100 microliters of plasma. The LOD and LLQ for the fourth metabolite was 0.25 and 0.5 ng ml-1, respectively. The between-day and within-day precisions were always < 15% for all the analytes. A limited pharmacokinetic study in mice treated and with I demonstrated that the method is appropriate for this purpose.
R van Gijn; E Havik; E Boven; J B Vermorken; W W ten Bokkel Huinink; O van Tellingen; J H Beijnen
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Publication Detail:
Type:  Journal Article    
Journal Detail:
Title:  Journal of pharmaceutical and biomedical analysis     Volume:  14     ISSN:  0731-7085     ISO Abbreviation:  J Pharm Biomed Anal     Publication Date:  1995 Dec 
Date Detail:
Created Date:  1997-01-02     Completed Date:  1997-01-02     Revised Date:  2003-11-14    
Medline Journal Info:
Nlm Unique ID:  8309336     Medline TA:  J Pharm Biomed Anal     Country:  ENGLAND    
Other Details:
Languages:  eng     Pagination:  165-74     Citation Subset:  IM    
Department of Pharmacy, Slotervaart Hospital/Netherlands Cancer Institute, Amsterdam.
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MeSH Terms
Antineoplastic Agents / blood*,  pharmacokinetics
Chromatography, High Pressure Liquid
Mice, Inbred Strains
Quality Control
Reference Standards
Staurosporine / analogs & derivatives*,  blood,  pharmacokinetics
Reg. No./Substance:
0/Antineoplastic Agents; 0/Solutions; 120685-11-2/4'-N-benzoylstaurosporine; 62996-74-1/Staurosporine

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