Eli Breuer
Israel
Research Article
Investigation of Intestinal Absorption Enhancers: Individual vs. Blends with the Carbamoylphosphonate JS403
Author(s): Reut Bitton, Marina Tsuriel, Rama Suresh, Eli Breuer, Reuven Reich and Amnon Hoffman
Reut Bitton, Marina Tsuriel, Rama Suresh, Eli Breuer, Reuven Reich and Amnon Hoffman
JS403 is a carbamoylphosphonate (CPO) molecule that showed anti-metastatic properties in mice. Since JS403 is intended to be a chronic prophylactic drug, the preferred route of administration should be oral. However, it exhibits poor oral bioavailability of less than 1%. The poor intestinal permeability and high solubility implies its classification as BCS class III drug. The aim of this study was to overcome the limited intestinal permeation of JS403 that is regarded as an unmet need in the pharmaceutical industry for this class of drugs. Therefore, the impact of acceptable absorption enhancers on the intestinal permeability of JS403 were examined using established experimental models. The absorption enhancers were: I) sodium caprate (C10), II) sodium deoxycholate (SDC) and III) mono-carboxymethylated chitosan (MCC). The effect of each enhancer was examined alone and also in combinat.. View More»
DOI:
10.4172/0975-0851.1000372