title: Development of glyburide fast-dissolving tablets based on the combined use of cyclodextrins and polymers.
abstract: Commercial tablets of glyburide exhibit unsatisfactory dissolution profiles and, consequently, problems of bioinequivalence and poor bioavailability. The aim of this work was to develop glyburide fast-dissolving tablets by exploiting the solubilizing effect of different cyclodextrins (CDs), alone or in combination with hydrophilic polymers. Drug-CD and drug-CD-polymer systems, prepared by different techniques, were characterized by differential scanning calorimetry (DSC), X-ray diffractometry, and Fourier transform infra-red (FT-IR) spectroscopy. Tablets containing binary and ternary systems were prepared by direct compression and evaluated for technological properties and dissolution behavior in comparison with a reference formulation containing the plain drug. A significant improvement of the drug dissolution profile was achieved from tablets containing drug-CD systems (coevaporated products doubled drug dissolution efficiency [DE]), but 100% drug dissolution was never reached. Better results were obtained with ternary systems. In particular, polyvinylpyrrolidone (PVP) emerged as the most effective polymer, and tablets with drug-PVP-hydroxypropyl-betaCD coevaporated products showed the best dissolution profiles, reaching 100% dissolved drug within only 15 min.
authors.affiliation: Department of Pharmaceutical Sciences, University of Florence, Sesto Fiorentino, Florence, Italy.
authors.forename: Marzia
authors.initials: M
authors.lastname: Cirri
authors.forename: M Francesca
authors.initials: MF
authors.lastname: Righi
authors.forename: Francesca
authors.initials: F
authors.lastname: Maestrelli
authors.forename: Paola
authors.initials: P
authors.lastname: Mura
authors.forename: Maurizio
authors.initials: M
authors.lastname: Valleri
mesh_terms: D001682:Biological Availability; D002152:Calorimetry, Differential Scanning; D002626:Chemistry, Pharmaceutical; D003505:Cyclodextrins / Q000737:chemistry*; D005905:Glyburide / Q000737:chemistry / Q000493:pharmacokinetics*; D007004:Hypoglycemic Agents / Q000737:chemistry / Q000493:pharmacokinetics*; D011108:Polymers / Q000737:chemistry*; D011205:Povidone / Q000737:chemistry; D012995:Solubility; D017550:Spectroscopy, Fourier Transform Infrared; D013607:Tablets; D013678:Technology, Pharmaceutical; D013810:Therapeutic Equivalency; D014961:X-Ray Diffraction
chemical_list: D003505:Cyclodextrins; D007004:Hypoglycemic Agents; D011108:Polymers; D013607:Tablets; D011205:Povidone; D005905:Glyburide