We evaluated the potential bioavailability of alkylamides and caffeate conjugates in Caco-2 monolayer abuse and compared them to actual bioavailability in highly ongoing Phase I clinical trials. Caffeic acid conjugates are almost impervious to the Caco-2 monomolecular layer [1]. Alkylamides have been found to diffuse rapidly through the Caco-2 monolayer. Fluctuations in the diffusion rate of each alkyl amide are associated with structural variation, with saturation and N-terminal methylation contributing to the reduced diffusion rate. The results of artificial alkylamides were consistent with those found in related grade ethanol formulations of the genus Echinacea, as diffusion of alkylamides is not accompanied by the presence of alternative components [2].
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