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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.jp

Teruo Murakami

Hiroshima International University, Japan

Modulation of absorption sites and bio-availabilities of orally administered drugs

depending on the solubility

in vivo