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Acta Chim Slov ; 59(1): 18-23, 2012 Mar.
Artículo en Inglés | MEDLINE | ID: mdl-24061168

RESUMEN

In this paper the procedure for the preparation of inclusion compounds of bioactive substance 2-[(2-aminoetoxy)-methyl]-4-(2-chlorophenyl)-1,4-dihydro-6-methyl-3,5-pyridine dicarboxylic acid 3-ethyl-5-methyl esterbenzene sulfonate, called amlodipine besylate with ß-cyclodextrin (ß-CD) and their structural characterization was described. Molecular inclusion compound of amlodipine besylate is obtained by different preparation method: kneading, co-precipitation and freeze-drying. The so obtained compounds were investigated by FTIR spectroscopy, X-ray diffraction method and differential scanning calorimetric measurements (DSC) to evidence their formation. Molecular modeling (using DFT theoretical computations) shows the spatial architecture of the inclusion compound in good agreement with FTIR experimental data: the drug is included with dihydropyridine dicarboxylate part inside ß-cyclodextrin cavity. The inclusion of amlodipine besylate in ß-cyclodextrin increases the stability and bioavailability of the drug.

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