title: Effect of tablet structure on controlled release from supersaturating solid dispersions containing glyceryl behenate.
abstract: The objective of this study was to evaluate the use of glyceryl behenate as a plasticizer and release modifier in solid dispersion systems containing itraconazole and carbamazepine. Amorphous solid dispersions of high molecular weight polyvinylpyrrolidone were prepared by hot-melt extrusion, the processing of which was improved by the inclusion of glyceryl behenate. Dispersions were milled and subsequently compressed into tablets. Solid dispersions were also prepared by KinetiSol Dispersing, which allowed for the manufacture of monolithic tablets of the same composition and shape as compressed tablets. Tablets without glyceryl behenate and all compressed tablets were observed to have an incomplete release profile likely due to drug crystallization within the tablet as this occurred at conditions in which dissolution concentrations were below saturation. Monolithic tablets formulated to be more hydrophobic, by including glyceryl behenate, allowed for sustained release below and above saturation conditions.
authors.affiliation: The University of Texas at Austin , 1 University Station, Austin, Texas 78712, United States.
authors.forename: Justin M
authors.initials: JM
authors.lastname: Keen
authors.forename: Justin R
authors.initials: JR
authors.lastname: Hughey
authors.forename: Ryan C
authors.initials: RC
authors.lastname: Bennett
authors.forename: Vincent
authors.initials: V
authors.lastname: Jannin
authors.forename: Yvonne
authors.initials: Y
authors.lastname: Rosiaux
authors.forename: Delphine
authors.initials: D
authors.lastname: Marchaud
authors.forename: James W
authors.initials: JW
authors.lastname: McGinity
mesh_terms: D002220:Carbamazepine / Q000737:chemistry*; D002851:Chromatography, High Pressure Liquid; D003692:Delayed-Action Preparations; D016503:Drug Delivery Systems; D005227:Fatty Acids / Q000737:chemistry*; D006358:Hot Temperature; D017964:Itraconazole / Q000737:chemistry; D007700:Kinetics; D008055:Lipids / Q000737:chemistry; D008970:Molecular Weight; D010968:Plasticizers; D011205:Povidone / Q000737:chemistry; D011208:Powders; D013607:Tablets / Q000737:chemistry*; D014961:X-Ray Diffraction
chemical_list: D003692:Delayed-Action Preparations; D005227:Fatty Acids; D008055:Lipids; D010968:Plasticizers; D011208:Powders; D013607:Tablets; C086409:glyceryl behenate; D017964:Itraconazole; D002220:Carbamazepine; D011205:Povidone
keywords: amorphous; controlled release; drug release; matrix tablet; solid dispersion