Journal of Bioequivalence & Bioavailability

Institute for Drug Research, School of Pharmacy, Faculty of Medicine, The Hebrew University of Jerusalem, P.O. Box 12065, Jerusalem 91120, Israel

Publications

• Research Article   
  The Effect of Chemical Modifications of Chitosan on Intestinal Permeability and Oral Bioavailability of Carbamoylphosphonate JS403
  Author(s): Reut Bitton-Dotan, Joerg Bohrisch, Christian Schmidt, Marina Tsuriel, R. N. Prasad Tulichala, Eli Breuer, Reuven Reich, Amnon Hoffman* and Joachim Storsberg
  
  JS403, Carbamoylphosphonate molecule, is a promising drug candidate with anti-metastatic activity. The polarity and water solubility of JS403 evolve from the phosphonate moiety that is ionized at physiologic pH. JS403 is regarded as a BCS class III molecule, and exhibit poor absolute oral bioavailability of less than 1%. The aim of this investigation is to identify proper chitosan based absorption enhancer compound(s) that upon oral co-administration with JS403 which would enhance its bioavailability. To determine the optimal properties of the chitosan derivative (CD), 11 relevant compounds were synthesized, each with different attribute, and their impact on the intestinal permeability of JS403 was examined in-vitro using the CaCO2 monolayer model. Then, the oral bioavailability of JS403 coadministered with the selected CD was examined i.. View more»
  

  DOI: 10.35248/0975-0851.20.12.392

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