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Importance of in vitro dissolution conditions for the in vivo predictability of an amorphous solid dispersion containing a pH-sensitive carrier.

Abstract：

:The present study investigated the influence of in vitro dissolution conditions on the in vivo predictability of an amorphous solid dispersion of celecoxib (CCX) in the pH-sensitive polymer Eudragit® S 100. Different doses of a 25:75w/w% CCX:Eudragit® S 100 amorphous solid dispersion (CCX:EUD) were investigated. During in vitro dissolution a significant effect of the pH of the dissolution media on the release of CCX was observed. In fasted state simulated intestinal fluid (FaSSIF) pH 6.5, the release of CCX from the amorphous solid dispersion was comparable to that of crystalline CCX and lower than that of amorphous CCX whereas in FaSSIF pH 7.4, the release was significantly increased compared to both crystalline and amorphous CCX. With a 3-fold increase in the exposure of CCX:EUD compared to crystaline CCX. The in vivo data also suggested that Eudragit® S 100 was suitable as a carrier in amorphous solid dispersions of CCX. In vitro-in vivo correlation demonstrated that the in vitro data obtained in FaSSIF pH 7.4 was more predictive for the in vivo performance than that obtained in FaSSIF pH 6.5. Consequently, the findings of this study underline that when predicting the in vivo performance of amorphous solid dispersions with pH-sensitive polymers, it is imperative that the in vitro dissolution conditions are carefully considered.

journal_name

Int J Pharm

journal_title

International journal of pharmaceutics

authors

Wendelboe J,Knopp MM,Khan F,Chourak N,Rades T,Holm R

doi

10.1016/j.ijpharm.2017.08.078

subject

Has Abstract

pub_date

2017-10-05 00:00:00

pages

324-331

issue

1

eissn

0378-5173

issn

1873-3476

pii

S0378-5173(17)30785-8

journal_volume

531

pub_type

杂志文章

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