ABSTRACT
An accidental contamination of metronidazole [MDZ] infusions was detected. The contaminant was identified as Penicillium spp.. The fungus grew rapidly on Czapek- Dox solution containing MDZ [0.5%] as a sole carbon and energy sources. HPLC analysis of the biodegradation products of MDZ by the isolated Penicillium spp. suggested that biodegradation pathway of MDZ involved at least two intermediates; the less active hydroxy and the inactive acelyl derivatives of MDZ. The two intermediates were also detected as inactivation products in the urine of humans after oral administration of MDZ. These results indicate that detoxification mechanism of MDZ in eukaryotics might be similar. Biodegradation of MDZ by Penicillium spp. was affected by temperature, pH and the length of incubation period. Maximum biodegradation was observed after 7 days incubation at a temperature of 25°C and pH 5.5. The biodegradation system of MDZ is inducible and seems to be located in the peirplasmic space of the fungus
Subject(s)
Humans , Metronidazole/metabolismABSTRACT
Se investigó la biodosponibilidad relativa de tres formulaciones de tabletas de metronidazol, al compararlas con una solución de un estándar conocido del fármaco. Los datos obtenidos fundamentan que las formulaciones estudiadas muestran una biodispsonibilidad relativa satisfactoria y son bioequivalentes, lo que sugiere una buena absorción del fármaco y la posibilidad de obtener con el mismo un efecto terapéutico adecuado
Subject(s)
Humans , Biological Availability , Metronidazole/metabolism , Therapeutic EquivalencyABSTRACT
Preliminary studies on the in vivo and in vitro interactions of 14C-metronidazole with macromolecules showed that the agent or its metabolite(s) can interact with nucleic acids and proteins in vivo. In vitro studies suggest that in absence of DNA synthesis trace amount of metronidazole does bind to DNA/protein and addition of metabolic activation system (from mouse liver) generates more reactive species from metronidazole.