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

Brazilian Archives of Biology and Technology

Leticia Norma Carpentieri Rodrigues²  Michelle Georges Issa¹  Ana Carolina Cavassin Asbahr¹  Marco Aurélio Carvalho Silva¹  Humberto Gomes Ferraz¹ 

[1] ,Universidade Federal de São Paulo Departamento de Ciências Exatas e da Terra Diadema SP ,Brasil

关键词: Pyrimethamine;    HPβCD;    inclusion complexes;   

DOI  :  10.1590/S1516-89132011000500014

来源: SciELO

【 摘 要 】

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.

【 授权许可】

CC BY-NC   
 All the contents of this journal, except where otherwise noted, is licensed under a Creative Commons Attribution License