title: Evaluation of the hyperbranched polymer Hybrane H1500 for production of matricial controlled-release particles by hot-melt extrusion.
abstract: Extrudates of the hyperbranched polymer Hybrane H1500 prepared by hot melt extrusion, with five particle sizes (from <250 μm to 1.5-2.0 mm) and three drug content (10, 20 and 30%) of acetaminophen or caffeine, were evaluated in this study as potential multiparticulate controlled release systems. Hybrane H1500 extrudates (of very low porosity), experienced a very slow hydration, with a limited swelling capacity, and they do not behave as true gels when fully hydrated. Hot melt extrusion provokes the conversion of the acetaminophen into an amorphous state inside the extrudates, whereas for those containing caffeine, some crystals remain for the highest drug proportions (20 and 30%). From both drug extrudates a wide range of dissolution profiles are obtained. Drug release rate depends mostly on extrudate particle size, and in those extrudates containing caffeine, a slight effect of the drug proportion is observed. Dissolution profiles' kinetic analysis suggests that drug release is controlled by the diffusion of the drug through the polymeric hydrated structure, although this mechanism is only clearly and efficiently displayed for the greatest extrudate particles (1.5-2.0 mm).
authors.affiliation: Department of Pharmacy and Pharmaceutical Technology, Faculty of Pharmacy, University of Santiago de Compostela, Spain.
authors.forename: Elena
authors.initials: E
authors.lastname: Raviña-Eirín
authors.affiliation: Department of Pharmacy and Pharmaceutical Technology, Faculty of Pharmacy, University of Santiago de Compostela, Spain.
authors.forename: Blanca
authors.initials: B
authors.lastname: Sánchez-Rodríguez
authors.affiliation: Department of Pharmacy and Pharmaceutical Technology, Faculty of Pharmacy, University of Santiago de Compostela, Spain.
authors.forename: Jose Luis
authors.initials: JL
authors.lastname: Gómez-Amoza
authors.affiliation: Department of Pharmacy and Pharmaceutical Technology, Faculty of Pharmacy, University of Santiago de Compostela, Spain. Electronic address: ramon.martinez@usc.es.
authors.forename: Ramón
authors.initials: R
authors.lastname: Martínez-Pacheco
mesh_terms: D000082:Acetaminophen / Q000008:administration & dosage* / Q000737:chemistry; D002110:Caffeine / Q000008:administration & dosage* / Q000737:chemistry; D002626:Chemistry, Pharmaceutical / Q000379:methods; D003460:Crystallization; D003509:Cyclohexanecarboxylic Acids / Q000737:chemistry*; D003692:Delayed-Action Preparations; D004337:Drug Carriers / Q000737:chemistry*; D004339:Drug Compounding / Q000379:methods; D004355:Drug Stability; D006358:Hot Temperature; D007700:Kinetics; D010316:Particle Size; D011091:Polyesters / Q000737:chemistry*; D016062:Porosity; D011412:Propanolamines / Q000737:chemistry*; D012995:Solubility
chemical_list: D003509:Cyclohexanecarboxylic Acids; D003692:Delayed-Action Preparations; D004337:Drug Carriers; D011091:Polyesters; D011412:Propanolamines; D000082:Acetaminophen; D002110:Caffeine
keywords: Acetaminophen; Caffeine; Controlled release particles; Hot melt extrusion; Hybrane H1500; Hyperbranched polymer