PVP solid dispersions for the controlled release of furosemide from a floating multiple-unit system.
The poor bioavailability of orally dosed furosemide (FUR) is due to the presence of a biological window in the upper gastrointestinal tract. The purpose of the present study was to develop and optimize in vitro a multiple-unit floating system with increased gastric residence time for FUR. The incomplete release of FUR from the units, related to its low water solubility, led to the preparation and evaluation of different FUR samples to be incorporated into the units. The complete dose release over the actual intragastric residence time of the system (about 8 hr) was achieved by loading both the core and the membrane forming the units with a 1:5 FUR/polyvinylpyrrolidone (FUR/PVP) solid dispersion. Physicochemical analyses suggested the predominant role of the amorphous state of FUR in producing enhanced drug solubility and dissolution rate, which led to the desired release profile from the floating units.
Iannuccelli
V
V
Department of Pharmaceutical Sciences, University of Modena and Reggio Emilia, Italy. iannuccelli@unimo.it
Coppi
G
G
Leo
E
E
Fontana
F
F
Bernabei
M T
MT
D002626:Chemistry, Pharmaceutical; D003692:Delayed-Action Preparations; D004232:Diuretics / Q000737:chemistry*; D005665:Furosemide / Q000737:chemistry*; D011205:Povidone / Q000737:chemistry*; D012995:Solubility
D003692:Delayed-Action Preparations; D004232:Diuretics; D005665:Furosemide; D011205:Povidone