title: Design and evaluation of a specific, bi-phase extended release system based on differently coated mini-tablets.
abstract: Mini-tablets are gaining great attention as systems capable of being formulated into multiple unit systems providing a specific drug release pattern. Within the presented research a combined, multiple-unit system, based on different coated matrix mini-tablets, has been developed in order to achieve 24-h specific sigmoid extended release of the model drug paliperidone. The mini-tablets were based on different amounts of polyvinyl acetate/polyvinyl pyrolidone mixture as the matrix former, providing extended release, and two different types of pH-dependent, acrylic polymer coatings, providing delay in release onset, and thus achieving the required specific sigmoid release pattern imposed by the original drug on the market. The selected formulation proved to be consistent with pharmacopoeial requirements. It was also in vitro similar (f2) to the original drug and the theoretical linear release profile, as well as robust and reproducible regarding in vitro release in different fasted gastro-intestinal conditions. This is proof of concept that 24-h, specific, and almost linear release profile of drugs with high solubility can be achieved by employing technology of coated matrix mini-tablets.
authors.affiliation: Department of Pharmaceutical Technology, Faculty of Pharmacy, University of Ljubljana, Aškerčeva 7, 1000 Ljubljana, Slovenia.
authors.forename: Aleksandar
authors.initials: A
authors.lastname: Aleksovski
authors.affiliation: Department of Pharmaceutical Technology, Faculty of Pharmacy, University of Ljubljana, Aškerčeva 7, 1000 Ljubljana, Slovenia.
authors.forename: Matevž
authors.initials: M
authors.lastname: Luštrik
authors.affiliation: Department of Pharmaceutical Technology, Faculty of Pharmacy, University of Ljubljana, Aškerčeva 7, 1000 Ljubljana, Slovenia.
authors.forename: Rok
authors.initials: R
authors.lastname: Šibanc
authors.affiliation: Department of Pharmaceutical Technology, Faculty of Pharmacy, University of Ljubljana, Aškerčeva 7, 1000 Ljubljana, Slovenia. Electronic address: rok.dreu@ffa.uni-lj.si.
authors.forename: Rok
authors.initials: R
authors.lastname: Dreu
mesh_terms: D003692:Delayed-Action Preparations / Q000737:chemistry; D065546:Drug Liberation; D004355:Drug Stability; D006863:Hydrogen-Ion Concentration; D065347:Hypromellose Derivatives / Q000737:chemistry; D008689:Methacrylates / Q000737:chemistry; D000068882:Paliperidone Palmitate / Q000737:chemistry*; D011108:Polymers / Q000737:chemistry; D012995:Solubility; D013607:Tablets
chemical_list: D003692:Delayed-Action Preparations; C477852:Eudragit L 30 D-55; D008689:Methacrylates; D011108:Polymers; D013607:Tablets; D065347:Hypromellose Derivatives; D000068882:Paliperidone Palmitate
keywords: Coating; Extended release; Matrix; Mini-tablets; Paliperidone; Similarity factor