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Asian Journal of Biomedical and Pharmaceutical Sciences | Volume 8
May 14-15, 2018 | Montreal, Canada
Global Summit on
Biopharma & Biotherapeutics
I
npharmacotherapy,most drugs are takenorally tobeabsorbed
systemically from the small intestine, and some drugs are
known to have preferential absorption sites in the small
intestine. For example, many substrate drugs for P-glycoprotein
(P-gp) are absorbed mostly in the proximal intestine, because
of the lower P-gp expression and higher luminal drug
concentrations. High luminal concentration of dissolved P-gp
substrate drugs can saturate P-gp-mediated efflux transports. In
contrast, the fraction of unabsorbed P-gp substrate drugs in the
proximal intestine can cause P-gp-mediated drug interactions in
the middle and distal small intestine, where P-gp is abundantly
expressed. Most of P-gp substrate drugs are categorized as BCS
Class 1 and 2 compounds, and BCS Class 2 compounds are low
solubility and high permeability. By increasing the solubility of
such BCS Class 2 drugs, especially the solubility in the stomach,
the absorption rate and bioavailability of P-gp substrate drugs
are improved. In the presentation, I introduce the absorption
sites of orally administered drugs, as well as, influencing factors
and experimental techniques, according to the reported data
collected by PubMed. Also, I will show some examples regarding
the effect of solubilization on absorption site and bioavailability
of orally administered P-gp substrate drugs. Securing the
solubility and stability of drugs prior to reaching to the main
absorption sites and appropriate delivery rates of drugs at
absorption sites are important goals for the development of
effective pharmacological products for pharmacotherapy
Speaker Biography
TeruoMurakami has completed his graduation fromOsaka University of Pharmaceutical
Sciences and his PhD from Graduated School of Pharmaceutical Sciences, Osaka
University, Japan. He has worked for Institute of Pharmaceutical Sciences and Graduate
School of Biomedical Sciences, Hiroshima University for 25 years, and he is now the
Professor of Hiroshima International University, Japan. His research interests are tissue
distribution of weakly basic drugs, and intestinal absorption including intestinal ABC
and SLC transporters. He has over 160 publications that have been cited over 3200
times, and his publication H-index is 30 and has been serving as an Editorial Board
Member of four international journals
e:
t-muraka@ps.hirokoku-u.ac.jpTeruo Murakami
Hiroshima International University, Japan
Modulation of absorption sites and bio-availabilities of orally administered drugs
depending on the solubility
in vivo