ノスカピンの生体内運命に関する研究(第1報)家兎尿中代謝物の検索

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After oral administration of noscapine (80-150 mg/kg) to male rabbits, detection of its urinary metabolites was carried out. The first 24-hr urine was extracted with CHCl_3 at pH 8-9 (F-I) and the remaining urine was re-extracted with CHCl_8 after acid hydrolysis (F-II). By means of thin-layer chromatography (TLC) coupled with methane chemical ionization mass spectrometry, the Dragendorffpositive spots in CHCl_3 extracts were easily recognized as the metabolites. These spots were separated by two successive preparative TLC using the solvent systems of CHCl_3-acetone (4 : 1) and cyclohexaneethyl acetate (2 : 3). The quasi-molecular ions of the separated metabolites suggested that these metabolites should be demethylation products. Thus, unchanged noscapine (M-1) and two O-monodemethylated metabolites (M-2 and M-3) were detected as free metabolites, and M-2,M-3,and M-4 (O-didemethylated metabolite) as conjugated metabolites. The main urinary metabolite was M-2,but it was excreted only in a small amount, same as unchanged noscapine.
公益社団法人日本薬学会の論文
1976-10-31