title: Taste-masking properties of solid lipid based micropellets obtained by cold extrusion-spheronization.
abstract: Taste-masked properties of micropellets based on hard fat and/or solid lipid mixtures (prepared by solvent-free cold extrusion/spheronization), containing metformin hydrochloride were investigated. An in-line and an on-line drug release profile evaluation of the pellets was performed and further correlated with an electronic tongue investigation. The pellets based on more than 30% of lipid binders showed metformin HCl releases below 10% after 30s of dissolution. Micropellets based on 20 and 30% of lipids showed immediate drug release profiles. Likewise, the electronic tongue assay showed a decrease in the sensor responses related to the increase of lipid amount in the formulations denoting a significant improvement in the taste masking properties of pellets based on more than 30% of lipid binders. A slight difference between pellets based on hard fat only and pellets based on ternary lipid mixtures was evidenced. Solvent-free cold extrusion/spheronization using solid lipids showed to be a robust method to obtain high drug loaded metformin HCl micropellets with adequate taste-masked properties and immediate drug release profile.
authors.affiliation: Institute of Pharmaceutics and Biopharmaceutics, Heinrich-Heine-University, Universitaetstrasse 1, 40225, Duesseldorf, Germany. Electronic address: Gustavo.Petrovick@hhu.de.
authors.forename: Gustavo Freire
authors.initials: GF
authors.lastname: Petrovick
authors.affiliation: Institute of Pharmaceutics and Biopharmaceutics, Heinrich-Heine-University, Universitaetstrasse 1, 40225, Duesseldorf, Germany.
authors.forename: Jörg
authors.initials: J
authors.lastname: Breitkreutz
authors.affiliation: Institute of Pharmaceutics and Biopharmaceutics, Heinrich-Heine-University, Universitaetstrasse 1, 40225, Duesseldorf, Germany; Life Science Technologies, University of Applied Sciences Ostwestfalen-Lippe, Georg-Weerth-Strasse 20, 32756 Detmold, Germany.
authors.forename: Miriam
authors.initials: M
authors.lastname: Pein-Hackelbusch
mesh_terms: D002626:Chemistry, Pharmaceutical / Q000379:methods*; D065546:Drug Liberation; D005079:Excipients / Q000737:chemistry; D007004:Hypoglycemic Agents / Q000008:administration & dosage / Q000737:chemistry; D008055:Lipids / Q000737:chemistry*; D008687:Metformin / Q000008:administration & dosage* / Q000737:chemistry; D012995:Solubility; D013649:Taste
chemical_list: D005079:Excipients; D007004:Hypoglycemic Agents; D008055:Lipids; D008687:Metformin
keywords: Cold extrusion; Drug release; Electronic tongue; Lipid pellets; Metformin hydrochloride; Metformin hydrochloride (PubChem CID: 14219); Spheronization; Taste masking; glyceryl distearate (PubChem CID: 114690); glyceryl trimyristate (PubChem CID: 11148)