title: Dissolution from solid lipid extrudates containing release modifiers.
abstract: The influence of different types of release modifiers on the dissolution from solid lipid extrudates was investigated. Diprophylline was extruded together with 45% tristearin and 5% (w/w) of a release modifier to suitable extrudates. Three groups of release modifiers were defined: Hydrocolloids, disintegrants and pore formers. All of the release modifier-containing extrudates showed a faster release compared to the reference extrudate, which contained 50% (w/w) of each, API and lipid. Increasing the amount of diprophylline in the binary mixture up to 55% (w/w) also increased its release rate. Compared to this new reference, not all of the release modifier-containing extrudates exhibited an increased dissolution rate. Within the group of pore formers, there was a great discrepancy concerning the dissolution rates. Extrudates containing polyethylene glycol (PEG) exhibited a much higher release rate compared with extrudates containing sodium chloride or mannitol. This behaviour was assumed to be based on the extrusion temperature of 65°C at which PEG exists in the molten state. The hypothesis was tested using different PEGs and another solid lipid.
authors.affiliation: Institute of Pharmaceutics and Biopharmaceutics, Heinrich-Heine-University Duesseldorf, Universitaetsstraße 1, 40225 Duesseldorf, Germany. sinan.gueres@hhu.de
authors.forename: Sinan
authors.initials: S
authors.lastname: Güres
authors.forename: Peter
authors.initials: P
authors.lastname: Kleinebudde
mesh_terms: D002152:Calorimetry, Differential Scanning; D055598:Chemical Phenomena; D003102:Colloids; D003692:Delayed-Action Preparations / Q000008:administration & dosage / Q000737:chemistry; D004058:Diffusion; D004339:Drug Compounding / Q000379:methods*; D016503:Drug Delivery Systems; D004400:Dyphylline / Q000008:administration & dosage / Q000737:chemistry*; D005079:Excipients / Q000737:chemistry*; D007700:Kinetics; D008855:Microscopy, Electron, Scanning; D008970:Molecular Weight; D044367:Phase Transition; D010726:Phosphodiesterase Inhibitors / Q000008:administration & dosage / Q000737:chemistry*; D011092:Polyethylene Glycols / Q000737:chemistry; D016062:Porosity; D012995:Solubility; D013499:Surface Properties; D014280:Triglycerides / Q000737:chemistry*; D014783:Viscosity
chemical_list: D003102:Colloids; D003692:Delayed-Action Preparations; D005079:Excipients; D010726:Phosphodiesterase Inhibitors; D014280:Triglycerides; D004400:Dyphylline; D011092:Polyethylene Glycols; C022618:tristearin