title: Characterization and dissolution properties of ketoprofen in binary and ternary solid dispersions with polyethylene glycol and surfactants.
abstract: The effect of incorporation of an anionic [sodium dodecyl sulfate (SDS) or dioctylsulfosuccinate (DSS)] or nonionic [Tween 60 (TW60)] surfactant on the properties of ketoprofen solid dispersions in polyethylene glycol 15000 (PEG) has been investigated. Physicochemical and morphological properties of the various solid systems were determined by differential scanning calorimetry, hot stage microscopy, X-ray powder diffraction analysis, and scanning electron microscopy. The results from dissolution studies, performed according to the USP 24 basket method, indicated that all ternary dispersed systems were significantly (p < 0.001) more efficacious than the corresponding binary ones, by virtue of the additive wetting and solubilizing effect due to the presence of the surfactant. The relative effectiveness of the incorporated surfactant was in the same order as found in phase-solubility studies (i.e., SDS > DSS > TW60). With regard to the solid dispersion preparation method, coevaporated products always gave better results than the corresponding cofused ones; however, this effect was statistically significant (p < 0.001) only in the initial phase of the dissolution process. The most effective solid dispersion was the 10-80-10 w/w drug-PEG-SDS ternary coevaporate, which allowed dissolution of 50% drug after only 6 min (in comparison with > 120 min for drug alone and 17 min for the binary coevaporate) and dissolution of about 100% drug after 30 min (in comparison with > 120 min for the binary coevaporate).
authors.affiliation: Dipartimento di Scienze Farmaceutiche, Polo Scientifico, Sesto Fiorentino, Firenze, Italia. mura@unifi.it
authors.forename: P
authors.initials: P
authors.lastname: Mura
authors.forename: J R
authors.initials: JR
authors.lastname: Moyano
authors.forename: M L
authors.initials: ML
authors.lastname: González-Rodríguez
authors.forename: A M
authors.initials: AM
authors.lastname: Rabasco-Alvaréz
authors.forename: M
authors.initials: M
authors.lastname: Cirri
authors.forename: F
authors.initials: F
authors.lastname: Maestrelli
mesh_terms: D000894:Anti-Inflammatory Agents, Non-Steroidal / Q000737:chemistry; D002152:Calorimetry, Differential Scanning / Q000379:methods; D004337:Drug Carriers / Q000737:chemistry; D007660:Ketoprofen / Q000737:chemistry*; D008855:Microscopy, Electron, Scanning; D011092:Polyethylene Glycols / Q000737:chemistry*; D012995:Solubility; D013501:Surface-Active Agents / Q000737:chemistry*; D013678:Technology, Pharmaceutical / Q000379:methods; D014961:X-Ray Diffraction / Q000379:methods
chemical_list: D000894:Anti-Inflammatory Agents, Non-Steroidal; D004337:Drug Carriers; D013501:Surface-Active Agents; D011092:Polyethylene Glycols; D007660:Ketoprofen