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(Reference retrieved automatically from Web of Science through information on FAPESP grant and its corresponding number as mentioned in the publication by the authors.)

Local Structure of Ion Pair Interaction in Lapatinib Amorphous Dispersions characterized by Synchrotron X-Ray diffraction and Pair Distribution Function Analysis

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Author(s):
de Araujo, Gabriel L. B. ; Benmore, Chris J. ; Byrn, Stephen R.
Total Authors: 3
Document type: Journal article
Source: SCIENTIFIC REPORTS; v. 7, APR 11 2017.
Web of Science Citations: 8
Abstract

For many years, the idea of analyzing atom-atom contacts in amorphous drug-polymer systems has been of major interest, because this method has always had the potential to differentiate between amorphous systems with domains and amorphous systems which are molecular mixtures. In this study, local structure of ionic and noninonic interactions were studied by High-Energy X-ray Diffraction and Pair Distribution Function (PDF) analysis in amorphous solid dispersions of lapatinib in hypromellose phthalate (HPMCP) and hypromellose (HPMC-E3). The strategy of extracting lapatinib intermolecular drug interactions from the total PDF x-ray pattern was successfully applied allowing the detection of distinct nearest neighbor contacts for the HPMC-E3 rich preparations showing that lapatinib molecules do not cluster in the same way as observed in HPMC-P, where ionic interactions are present. Orientational correlations up to nearest neighbor molecules at about 4.3 (A) over circle were observed for polymer rich samples; both observations showed strong correlation to the stability of the systems. Finally, the superior physical stability of 1: 3 LP: HPMCP was consistent with the absence of significant intermolecular interactions in (Delta D-LP(inter)(r)) in the range of 3.0 to 6.0 (A) over circle, which are attributed to C-C, C-N and C-O nearest neighbor contacts present in drug-drug interactions. (AU)

FAPESP's process: 15/05685-7 - Crystallization and polymorphism of Flubendazole and other ill-characterized drugs
Grantee:Gabriel Lima Barros de Araujo
Support Opportunities: Regular Research Grants
FAPESP's process: 15/15456-5 - Study of polymorphism of small molecule tyrosine kinase inhibitors.
Grantee:Gabriel Lima Barros de Araujo
Support Opportunities: Scholarships abroad - Research