In Vitro Dissolution/Permeation System to Predict the Oral Absorption of Poorly Water-Soluble Drugs: Effect of Food and Dose Strength on It
| Autor: | Sachi Itsubata, Yoshie Masaoka, Shinji Sakuma, Shinji Yamashita, Makoto Kataoka |
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| Rok vydání: | 2011 |
| Předmět: |
Absorption (pharmacology)
Administration Oral Tetrazoles Pharmaceutical Science Pharmacology Permeability Food-Drug Interactions In vivo medicine Humans Technology Pharmaceutical Solubility Dissolution Chromatography Dose-Response Relationship Drug Chemistry Water Fasting General Medicine Permeation Postprandial Period In vitro Cilostazol Intestinal Absorption Pharmaceutical Preparations Absorbed dose Caco-2 Cells medicine.drug |
| Zdroj: | Biological and Pharmaceutical Bulletin. 34:401-407 |
| ISSN: | 1347-5215 0918-6158 |
| Popis: | 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: r(2)=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. |
| Databáze: | OpenAIRE |
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