title: Fast-dissolving tablets of glyburide based on ternary solid dispersions with PEG 6000 and surfactants.
abstract: Marketed glyburide tablets present unsatisfying dissolution profiles that give rise to variable bioavailability. With the purpose of developing a fast-dissolving tablet formulation able to assure a complete drug dissolution, we investigated the effect of the addition to a reference tablet formulation of different types (anionic and nonionic) and amounts of hydrophilic surfactants, as well as the use of a new technique, based on ternary solid dispersions of the drug with an hydrophilic carrier (polyethylene glycol [PEG] 6000) and a surfactant. Tablets were prepared by direct compression or previous wet granulation of suitable formulations containing the drug with each surfactant or drug:PEG:surfactant ternary dispersions at different PEG:surfactant w/w ratios. The presence of surfactants significantly increased (p<0.01) the drug dissolution rate, but complete drug dissolution was never achieved. On the contrary, in all cases tablets containing ternary solid dispersions achieved 100% dissolved drug within 60 min. The best product was the 10:80:10 w/w ternary dispersion with PEG 6000 and sodium laurylsulphate, showing a dissolution efficiency 5.5-fold greater than the reference tablet formulation and 100% drug dissolution after only 20 min.
authors.affiliation: Department of Pharmaceutical Sciences, University of Florence, Firenze, Italy.
authors.forename: Marzia
authors.initials: M
authors.lastname: Cirri
authors.forename: Francesca
authors.initials: F
authors.lastname: Maestrelli
authors.forename: Giovanna
authors.initials: G
authors.lastname: Corti
authors.forename: Paola
authors.initials: P
authors.lastname: Mura
authors.forename: Maurizio
authors.initials: M
authors.lastname: Valleri
mesh_terms: D002626:Chemistry, Pharmaceutical; D004337:Drug Carriers; D005905:Glyburide / Q000737:chemistry*; D007004:Hypoglycemic Agents / Q000737:chemistry*; D011092:Polyethylene Glycols / Q000737:chemistry*; D012995:Solubility; D013501:Surface-Active Agents / Q000737:chemistry*; D013607:Tablets; D013678:Technology, Pharmaceutical / Q000379:methods; D013997:Time Factors; D017155:Wettability
chemical_list: D004337:Drug Carriers; D007004:Hypoglycemic Agents; D013501:Surface-Active Agents; D013607:Tablets; D011092:Polyethylene Glycols; D005905:Glyburide