Multicomponent complex formation between pyrimethamine, cyclodextrins and water-soluble polymers

Autor: Leticia Norma Carpentieri Rodrigues, Michelle Georges Issa, Ana Carolina Cavassin Asbahr, Marco Aurélio Carvalho Silva, Humberto Gomes Ferraz
Jazyk: angličtina
Rok vydání: 2011
Předmět:
Zdroj: Brazilian Archives of Biology and Technology, Vol 54, Iss 5, Pp 965-972 (2011)
Druh dokumentu: article
ISSN: 1516-8913
1678-4324
DOI: 10.1590/S1516-89132011000500014
Popis: The combined effect of hydroxypropyl-β-cyclodextrin (HPβCD) and polyvinylpyrrolidone (PVP) or sodium carboxymethylcellulose (CMC) on the solubility of pyrimethamine (PYR) was studied. Equimolar PYR-HPβCD solid systems, in the presence or the absence of 0.25% (w/v) PVP or 0.10% (w/v) CMC were prepared by coevaporation or freeze-drying, and characterized by differential scanning calorimetry, X-ray diffraction analysis and dissolution profile. Phase-solubility analysis was used to investigate the interactions in aqueous solution between PYR and HPβCD, in the absence or presence of polymers, which showed a linear increase of PYR solubility depending on the concentration of HPβCD. The presence of polymer did not alter the stoichiometry of the complexes. DSC results were indicative of complexation, due to the loss of the characteristic endothermic peak of PYR. X-ray diffraction analysis confirmed the DSC results. Binary and ternary complexes showed higher dissolution rate when compared with the pure drug.
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