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Impact of FaSSIF on the solubility and dissolution-/permeation rate of a poorly water-soluble compound

The poorly water-soluble drug ABT-102, a potent TRPV1 (transient receptor potential cation channel subfamily V member 1) antagonist, was investigated in terms of its solubility and dissolution-permeation rate across Caco-2 cell monolayers in the presence and absence of fasted state simulated intesti...

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Bibliographische Detailangaben
Hauptverfasser: Frank, Kerstin J. (VerfasserIn) , Fricker, Gert (VerfasserIn)
Dokumenttyp: Article (Journal)
Sprache:Englisch
Veröffentlicht: 1 May 2012
In: European journal of pharmaceutical sciences
Year: 2012, Jahrgang: 47, Heft: 1, Pages: 16-20
ISSN:1879-0720
DOI:10.1016/j.ejps.2012.04.015
Online-Zugang:Verlag, Volltext: http://dx.doi.org/10.1016/j.ejps.2012.04.015
Verlag, Volltext: http://www.sciencedirect.com/science/article/pii/S0928098712001844
Volltext
Verfasserangaben:Kerstin J. Frank, Ulrich Westedt, Karin M. Rosenblatt, Peter Hölig, Jörg Rosenberg, Markus Mägerlein, Martin Brandl, Gert Fricker
Beschreibung
Zusammenfassung:The poorly water-soluble drug ABT-102, a potent TRPV1 (transient receptor potential cation channel subfamily V member 1) antagonist, was investigated in terms of its solubility and dissolution-permeation rate across Caco-2 cell monolayers in the presence and absence of fasted state simulated intestinal fluid (FaSSIF). ABT-102 showed a more than 30-fold higher apparent solubility in FaSSIF, compared to Hank’s balanced salt solution (HBSS). On the other hand, the amount of truly dissolved API in the suspension, as assessed by inverse dialysis, was found hardly influenced by FaSSIF. Neither the drug nor FaSSIF adversely affected cell viability or integrity of the Caco-2 monolayer. P-gp-inhibition experiments confirmed that the drug was not a substrate of the export pump. The flux of ABT-102 across the Caco-2 barrier was found virtually the same in FaSSIF and in buffer, i.e. in vitro overall dissolution-/permeation rate of ABT-102 from suspensions appears not affected by its enhanced apparent solubility due to association with TC/PC-micelles.
Beschreibung:Gesehen am 23.04.2018
Beschreibung:Online Resource
ISSN:1879-0720
DOI:10.1016/j.ejps.2012.04.015

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