FORMATION, BIOAVAILABILITY AND ORGANOLEPTIC PROPERTIES OF AN INCLUSION COMPLEX OF FEMOXETINE WITH BETA-CYCLODEXTRIN

Femoxetine, a new selective serotonin uptake inhibitor with antidepressant properties, possesses a very bitter taste which hinders the development of oral liquid formulations. It is possible to improve the organoleptic properties by inclusion complexation of the drug with .beta.-cyclodextrin. Phase solubility diagrams and UV-spectroscopic studies revealed the formation of 1:1 and 1:2 inclusion complexes, the strongest complex being obtained for femoxetine in free-base form. A microcrystalline inclusion complex was isolated and had the stoichiometric composition of 1:2 (femoxetine:.beta.-cyclodextrin). In a single dose cross-over study in 5 volunteers, the bioavailability of the solid complex formulated as a aqueous suspension was similar to that observed for a sugar-coated tablet of femoxetine hydrochloride.