Abstract:
:Solid solutions of felodipine with EUDRAGIT E and EUDRAGIT E/NE were shown to dramatically increase the dissolution rate of felodipine in biorelevant media. Of the two polymer systems, extrudates containing 5% EUDRAGIT NE showed a faster dissolution rate and less recrystallization (no precipitation within 2 h). Although differential scanning calorimetry (DSC) and conventional X-ray powder diffraction (XRPD) were able to verify the amorphous state of the drug after melt extrusion, it was not possible to differentiate the two extrudate compositions further with these methods. We then applied pair distribution function (PDF) analysis to investigate extrudates. It was possible to more closely characterize the solid state of the amorphous extrudates in terms of local structural order: PDF analysis revealed that addition of minor amounts of EUDRAGIT NE to the main component EUDRAGIT E during extrusion changed the local structure of EUDRAGIT E in a nonadditive way. We conclude that local ordering can be important to the release characteristics of extrudates, even when the components are present in the amorphous state.
journal_name
J Pharm Scijournal_title
Journal of pharmaceutical sciencesauthors
Nollenberger K,Gryczke A,Meier Ch,Dressman J,Schmidt MU,Brühne Sdoi
10.1002/jps.21534subject
Has Abstractpub_date
2009-04-01 00:00:00pages
1476-86issue
4eissn
0022-3549issn
1520-6017pii
S0022-3549(16)32934-3journal_volume
98pub_type
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