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Int J Pharm. 2009 Sep 11;379(2):251-9. doi: 10.1016/j.ijpharm.2009.05.035. Epub 2009 May 23.

Removal of ciprofloxacin in simulated digestive media by activated charcoal entrapped within zinc-pectinate beads.

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Université Paris Sud, UMR 8612, Châtenay-Malabry, F-92290, France.


Beads made of a zinc-pectinate matrix containing activated charcoal were designed for the adsorption of colonic residual antibiotics responsible of the emergence of resistance. Bead stability was shown to correlate with bead zinc content, 0.08 mg/mg being the minimal amount of zinc that protects the egg-box structure against total disintegration. Moreover, the stability in simulated gastro-intestinal media was shown to be related to the composition of the incubation medium. Indeed, gastric medium was shown to extract a large amount of zinc inducing an early disintegration of the beads in the intestinal medium, making necessary their protection by gastro-resistant capsules. Simulated intestinal medium buffered by phosphate was not adapted for the disintegration studies since the formation of a zinc phosphate precipitate on beads surface enhances their resistance to further degradation by pectinases contained in colonic medium. On the other hand, beads incubated in HEPES were stable in intestinal medium and nicely degraded by pectinases contained in simulated colonic medium. Despite this stability, coating with Eudragit RS was needed to prevent the early adsorption of antibiotics in intestinal medium. Adsorption studies in the simulated colonic medium show that the adsorption capacity of activated charcoal is not modified after its encapsulation within pectin beads making the elimination of ciprofloxacin reaching the colon clinically feasible.

[Indexed for MEDLINE]

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