Literature DB >> 21540091

Degradation kinetics of metronidazole and olsalazine by bacteria in ascending colon and in feces of healthy adults.

Maria Vertzoni1, Anders Carlsson, Bertil Abrahamsson, Konstantinos Goumas, Christos Reppas.   

Abstract

PURPOSE: To compare the degradation kinetics of metronidazole and olsalazine by the bacteria of ascending colon and the bacteria of feces of healthy adults.
METHODS: Contents of the ascending colon of seven healthy adults were collected under conditions simulating the bioavailability/bioequivalence studies in the fasted and in the fed states on a crossover basis. Material from the contents of the ascending colon was prepared by ultracentrifuging and diluting the precipitate with a volume of normal saline equivalent to that of the supernatant. Fecal material was prepared from feces of three healthy adults collected at two occasions that were separated by at least 6 months. Ex vivo drug degradation kinetics were evaluated under anaerobic conditions.
RESULTS: Mean half-lives of metronidazole degradation in material from the contents of the ascending colon collected in the fasted state and in fecal material were 16.1 and 2.4 min, respectively (p<0.001). The corresponding numbers for olsalazine were 57.8 and 9.2 min, respectively (p<0.001). Both compounds were stable in material from the contents of ascending colon collected in the fed state.
CONCLUSIONS: Compared with data in fecal material, degradation of metronidazole and olsalazine in material from the contents of the ascending colon is significantly slower and it becomes non-significant during the arrival of fresh food remnants in the region.
Copyright © 2011 Elsevier B.V. All rights reserved.

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Year:  2011        PMID: 21540091     DOI: 10.1016/j.ijpharm.2011.04.028

Source DB:  PubMed          Journal:  Int J Pharm        ISSN: 0378-5173            Impact factor:   5.875


  5 in total

1.  Characterization of Contents of Distal Ileum and Cecum to Which Drugs/Drug Products are Exposed During Bioavailability/Bioequivalence Studies in Healthy Adults.

Authors:  Christos Reppas; Eleni Karatza; Constantinos Goumas; Constantinos Markopoulos; Maria Vertzoni
Journal:  Pharm Res       Date:  2015-05-22       Impact factor: 4.200

2.  Biopharmaceutical considerations and characterizations in development of colon targeted dosage forms for inflammatory bowel disease.

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Journal:  Drug Deliv Transl Res       Date:  2014-04       Impact factor: 4.617

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Journal:  Environ Sci Pollut Res Int       Date:  2013-10-22       Impact factor: 4.223

4.  Physiologically Based Biopharmaceutics Modeling of Regional and Colon Absorption in Dogs.

Authors:  Emma Eckernäs; Christer Tannergren
Journal:  Mol Pharm       Date:  2021-03-15       Impact factor: 4.939

5.  Metronidazole or Cotrimoxazole therapy is associated with a decrease in intestinal bioavailability of common antiretroviral drugs.

Authors:  Flore Dossou-Yovo; Godefroy Mamadou; Imar Djibrine Soudy; Nicolas Limas-Nzouzi; Joe Miantezila; Jehan-François Desjeux; Bruno Eto
Journal:  PLoS One       Date:  2014-02-26       Impact factor: 3.240

  5 in total

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