Diloxanide furoate binary complexes with B-, methyl-B;-, and hydroxypropyl-B-cyclodextrins: inclusion mode, characterization in solution and in solid state and in vitro dissolution studies

ALOISIO, CAROLINA; LONGHI, MARCELA

PHARMACEUTICAL DEVELOPMENT AND TECHNOLOGY

TAYLOR & FRANCIS INC

Año: 2017 p. 1 - 1

1083-7450

he purpose of this study was to investigate the effect on solubility and dissolution rate of binary complexes of B-(BCD), methyl-(MBCD) and hydroxypropyl-B-cyclodextrin (HPBCD) with diloxanide furoate (DF).The complexation in solution was evaluated by phase solubility studies and1H nuclear magnetic resonance (NMR). Enhanced water solubility of DF was obtained with the DF:M b CD system (61-fold). The mode of inclusion was supported by NMR experiments, which indicated that real inclusion complexes wereformed between DF and M b CD or HP b CD. Solid state analysis was performed using infrared and thermal methods, which suggested the formation of true inclusion complexes of DF with two derivatized cyclodex-trins, M b CD and HP b CD, and an exclusion complex with b CD when the systems were prepared by freeze-dried technique. Dissolution studies conducted in simulated gastric fluid (2 h) and subsequent simulated intestinal fluid (next 4 h) showed increased dissolution rate of DF from the fre