Identification of major degradation products of ketoconazole

Abstract

Analytical methods were developed for the identification of major degradation products of Ketoconazole, an antifungal agent. The stressed degradation of Ketoconazole drug substance was performed under acid, base, thermal, photo and oxidative stress conditions. The major degradation was observed under acid, base and oxidative stress conditions. The degradation study was performed on Inertsil ODS-3V, length 100 X diameter 4.6 mm, particle size 3 μm column using gradient method. These degradants were identified by LC-MS technique.

Keywords: Hydrolysis degradent; Ketoconazole; LC-MS; Oxidative degradent; Stress degradation.

Fig. 1

HPLC Chromatograms for Stressed conditions

Fig. 1

HPLC Chromatograms for Stressed conditions

Fig. 1

HPLC Chromatograms for Stressed conditions

Fig. 1

HPLC Chromatograms for Stressed conditions

Fig. 2

HPLC Chromatograms for preparation Oxidative degradent

Fig. 3

LC-Mass spectrum for Ketoconazole and degradent products

Fig. 3

LC-Mass spectrum for Ketoconazole and degradent products

Fig. 3

LC-Mass spectrum for Ketoconazole and degradent products

Fig. 4

Mass fragmentation behavior of Ketoconazole and N-Oxide

Fig. 5

NMR Spectrum of Ketoconazole and N-Oxide

Fig. 6

Elemental analysis for Ketoconazole and degradent products

Sch. 1

Structure of elucidated compounds