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Eur J Pharm Biopharm. 2013 Nov;85(3 Pt B):1317-24. doi: 10.1016/j.ejpb.2013.06.018. Epub 2013 Jun 26.

Assessment of absorption potential of poorly water-soluble drugs by using the dissolution/permeation system.

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  • 1Faculty of Pharmaceutical Sciences, Setsunan University, Osaka, Japan. Electronic address: makoto@pharm.setsunan.ac.jp.

Abstract

This study aims to assess the absorption potential of oral absorption of poorly water-soluble drugs by using the dissolution/permeation system (D/P system). The D/P system can be used to perform analysis of drug permeation under dissolution process and can predict the fraction of absorbed dose in humans. When celecoxib at 1/100 of a clinical dose was applied to the D/P system, percentage of dose dissolved and permeated significantly decreased with an increase in the applied amount, resulting in the oral absorption being predicted to be 22-55%. Whereas similar dissolution and permeation profiles of montelukast sodium were observed, estimated absorption (69-85%) was slightly affected. Zafirlukast absorption (33-36%) was not significantly affected by the dose, although zafirlukast did not show complete dissolution. The relationship between clinical dose and predicted oral absorption of drugs corresponded well to clinical observations. The limiting step of the oral absorption of celecoxib and montelukast sodium was solubility, while that of zafirlukast was dissolution rate. However, due to high permeability of montelukast, oral absorption was not affected by dose. Therefore, the D/P system is a useful tool to assess the absorption potential of poorly water-soluble drugs for oral use.

Copyright © 2013 Elsevier B.V. All rights reserved.

KEYWORDS:

Dissolution; Maximum absorbable dose; Poorly water-soluble drug; Rate-limiting step; Solubility

PMID:
23811221
[PubMed - indexed for MEDLINE]
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