title: Increased dissolution rates of tranilast solid dispersions extruded with inorganic excipients.
abstract: The purpose of this study was to evaluate the performance of Neusilin® (NEU) a synthetic magnesium aluminometasilicate as an inorganic drug carrier co-processed with the hydrophilic surfactants Labrasol and Labrafil to develop Tranilast (TLT)-based solid dispersions using continuous melt extrusion (HME) processing. Twin-screw extrusion was optimized to develop various TLT/excipient/surfactant formulations followed by continuous capsule filling in the absence of any downstream equipment. Physicochemical characterization showed the existence of TLT in partially crystalline state in the porous network of inorganic NEU for all extruded formulations. Furthermore, in-line NIR studies revealed a possible intermolecular H-bonding formation between the drug and the carrier resulting in the increase of TLT dissolution rates. The capsules containing TLT-extruded solid dispersions showed enhanced dissolution rates and compared with the marketed Rizaben®product.
authors.affiliation: a Faculty of Engineering and Science , School of Science, University of Greenwich, Chatham Maritime , Chatham , Kent , UK.
authors.forename: Mohammed
authors.initials: M
authors.lastname: Maniruzzaman
authors.affiliation: a Faculty of Engineering and Science , School of Science, University of Greenwich, Chatham Maritime , Chatham , Kent , UK.
authors.forename: Steven A
authors.initials: SA
authors.lastname: Ross
authors.affiliation: a Faculty of Engineering and Science , School of Science, University of Greenwich, Chatham Maritime , Chatham , Kent , UK.
authors.forename: Muhammad Tariqul
authors.initials: MT
authors.lastname: Islam
authors.affiliation: a Faculty of Engineering and Science , School of Science, University of Greenwich, Chatham Maritime , Chatham , Kent , UK.
authors.forename: Nikolaos
authors.initials: N
authors.lastname: Scoutaris
authors.affiliation: b Fuji Chemical Industry Co, Ltd, International Business Division , Minato-Ward , Tokyo , Japan.
authors.forename: Arun
authors.initials: A
authors.lastname: Nair
authors.affiliation: a Faculty of Engineering and Science , School of Science, University of Greenwich, Chatham Maritime , Chatham , Kent , UK.
authors.forename: Dennis
authors.initials: D
authors.lastname: Douroumis
mesh_terms: D017607:Aluminum Compounds; D002214:Capsules; D003460:Crystallization; D004337:Drug Carriers; D004339:Drug Compounding; D005079:Excipients / Q000737:chemistry*; D006634:Histamine H1 Antagonists / Q000008:administration & dosage / Q000737:chemistry*; D007700:Kinetics; D017616:Magnesium Compounds; D010316:Particle Size; D017640:Silicates; D012995:Solubility; D019265:Spectroscopy, Near-Infrared; D013501:Surface-Active Agents; D014961:X-Ray Diffraction; D062367:ortho-Aminobenzoates / Q000008:administration & dosage / Q000737:chemistry*
chemical_list: D017607:Aluminum Compounds; D002214:Capsules; D004337:Drug Carriers; D005079:Excipients; D006634:Histamine H1 Antagonists; D017616:Magnesium Compounds; D017640:Silicates; D013501:Surface-Active Agents; D062367:ortho-Aminobenzoates; C033065:aluminum magnesium silicate; C012293:tranilast
keywords: Extrusion; drug–excipient interactions dissolution; inorganic excipients; solid dispersions