title: Lean production of taste improved lipidic sodium benzoate formulations.
abstract: Sodium benzoate is a highly soluble orphan drug with unpleasant taste and high daily dose. The aim of this study was to develop a child appropriate, individually dosable, and taste masked dosage form utilizing lipids in melt granulation process and tableting. A saliva resistant coated lipid granule produced by extrusion served as reference product. Low melting hard fat was found to be appropriate as lipid binder in high-shear granulation. The resulting granules were compressed to minitablets without addition of other excipients. Compression to 2mm minitablets decreased the dissolved API amount within the first 2 min of dissolution from 33% to 23%. The Euclidean distances, calculated from electronic tongue measurements, were reduced, indicating an improved taste. The reference product showed a lag time in dissolution, which is desirable for taste masking. Although a lag time was not achieved for the lipidic minitablets, drug release in various food materials was reduced to 2%, assuming a suitable taste masking for oral sodium benzoate administration.
authors.affiliation: Institute of Pharmaceutics and Biopharmaceutics, Heinrich-Heine University Duesseldorf, Germany.
authors.forename: C
authors.initials: C
authors.lastname: Eckert
authors.affiliation: Institute of Pharmaceutics and Biopharmaceutics, Heinrich-Heine University Duesseldorf, Germany.
authors.forename: M
authors.initials: M
authors.lastname: Pein
authors.affiliation: Institute of Pharmaceutics and Biopharmaceutics, Heinrich-Heine University Duesseldorf, Germany. Electronic address: joerg.breitkreutz@uni-duesseldorf.de.
authors.forename: J
authors.initials: J
authors.lastname: Breitkreutz
mesh_terms: D002152:Calorimetry, Differential Scanning; D002626:Chemistry, Pharmaceutical; D008055:Lipids / Q000737:chemistry*; D008855:Microscopy, Electron, Scanning; D010599:Pharmacokinetics; D020160:Sodium Benzoate / Q000737:chemistry*; D012995:Solubility; D013649:Taste; D014059:Tongue
chemical_list: D008055:Lipids; D020160:Sodium Benzoate
keywords: Electronic tongue; Food interaction; Hard fat; Melt granulation; Orphan drug; Sodium benzoate; Taste masking