Synthesis, characterization and in vitro release studies of a new acetazolamide-HP-beta-CD-TEA inclusion complex.

The aim of our work was to develop a multicomponent inclusion complex of acetazolamide (ACZ) in order to investigate the combined effect of hydroxypropyl-beta-cyclodextrin (HP-beta-CD) and triethanolamine (TEA) on the solubility of ACZ and its possibility of ophthalmic delivery. Phase solubility study was used to evaluate the complexation in solution at 25 degrees C. Complex formation was also evaluated by comparing the infrared (FT-IR) spectra of the solid complexes with a simple physical mixture containing the same amount of ACZ. FT-IR experiments provided data indicating that the carbonamido group of ACZ is involved in the inclusion process. In vitro release data showed that both formulations, containing the freeze-dried ternary complex and the corresponding simple physical mixture of ACZ with HP-beta-CD and TEA presented the fastest release rate of ACZ. These results suggest that the ACZ-HP-beta-CD-TEA complex represents an effective novel formulation to enhance ACZ solubility in water, turning it promising for ophthalmic administration.

Ternary complexes of flurbiprofen with HP-beta-CD and ethanolamines characterization and transdermal delivery.

Binary and multicomponent systems complexes prepared with HP-beta-CD and/or with monoethanolamine (MEA), diethanolamine (DEA) or triethanolamine (TEA) were obtained. The results of solid-state studies indicated the presence of strong interactions between the components in the binary and the ternary systems. Drug solubility and dissolution rate in water were notably improved by employing the HP-beta-CD and the alkanolamines. The combined use of cosolvency and complexation with MEA in the presence of HP-beta-CD on the permeation of flurbiprofen through the human skin was evaluated. The combination of IPM, PG, and HP-beta-CD yield the highest permeation for the flurbiprofen-MEA complex.