In Vitro Dissolution/Permeation System to Predict the Oral Absorption of Poorly Water-Soluble Drugs: Effect of Food and Dose Strength on It

The aim of the present work was to confirm the usefulness of the dissolution/permeation system (D/P system) in the estimation of human oral absorption of poorly water-soluble drugs. The D/P system, which can simultaneously evaluate drug absorption processes, dissolution and permeation, can predict t...

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Bibliographic Details
Published in:Biological & pharmaceutical bulletin 2011/03/01, Vol.34(3), pp.401-407
Main Authors: Kataoka, Makoto, Itsubata, Sachi, Masaoka, Yoshie, Sakuma, Shinji, Yamashita, Shinji
Format: Article
Language:English
Subjects:
absorption
Administration, Oral
Caco-2 Cells
Cilostazol
dissolution
Dose-Response Relationship, Drug
Fasting
food effect
Food-Drug Interactions
Humans
Intestinal Absorption
Permeability
Pharmaceutical Preparations - analysis
poorly water-soluble drug
Postprandial Period
Solubility
Technology, Pharmaceutical - methods
Tetrazoles - pharmacokinetics
Water
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Summary:The aim of the present work was to confirm the usefulness of the dissolution/permeation system (D/P system) in the estimation of human oral absorption of poorly water-soluble drugs. The D/P system, which can simultaneously evaluate drug absorption processes, dissolution and permeation, can predict the oral absorption of poorly water-soluble drugs in fasted and fed humans, with a correlation between in vivo oral absorption (% of absorbed) and in vitro permeated amount (% of dose/2 h) in the D/P system. The oral absorption (fraction of absorbed dose, %) of poorly water-soluble drugs in the fasted and fed states was predicted using the D/P system. The effect of food on the oral absorption of various drugs estimated by the D/P system significantly correlated with clinical data (correlation coefficient: r2=0.924). Moreover, the proportion of oral absorption of cilostazol was predicted to decrease with an increase in its dose strength, which significantly correlated with in vivo human absorption. Consequently, the D/P system was demonstrated to be a useful in vitro system for prediction of the oral absorption of poorly water-soluble drugs.
ISSN:0918-6158
1347-5215
DOI:10.1248/bpb.34.401