• Maria Brusnikina
  • Oleg Silyukov
  • Mikhail Chislov
  • Tatyana Volkova
  • Alexey Proshin
  • Irina Terekhova

Effect of cyclodextrins on aqueous solubility of 1-[5-(3-chloro-phenylamino)-1,2,4-thiadiazol-3-yl]-propan-2-ol (I), which was synthesized and proposed for the treatment of Alzheimer’s disease, was studied. First of all, inclusion complex formation of I with different cyclodextrins was studied in aqueous solutions. Formation of more stable complexes with β- and hydroxypropyl-β-cyclodextrins was revealed. Next, solid inclusion complexes of I with β- and hydroxypropyl-β-cyclodextrins were prepared by the mechanical grinding, and their existence in the solid state was confirmed by powder X-ray diffraction, FTIR spectroscopy, microscopy, and thermochemical methods. Dissolution testing of the tablets of pure I and its complexes with β- and hydroxypropyl-β-cyclodextrins in the aqueous buffered solutions simulated the biological environment was carried out. The observed drastic enhancement of dissolution extent and dissolution rate of the complexes was attributed to the inclusion complex formation.

Original languageEnglish
Pages (from-to)1815-1824
Number of pages10
JournalJournal of Thermal Analysis and Calorimetry
Volume127
Issue number2
DOIs
StatePublished - 1 Feb 2017

    Scopus subject areas

  • Condensed Matter Physics
  • Physical and Theoretical Chemistry

    Research areas

  • 1,2,4-Thiadiazole, Cyclodextrin, Inclusion complex, Thermal analysis, Thermodynamics, Water-soluble dosage forms

ID: 37016598