title: Design of prolonged release tablets using new solid acrylic excipients for direct compression.
abstract: The design of new excipients that extend the release of drugs from tablets over prolonged periods is essential in reaching enhanced therapeutic performances. In this sense, the objective of this study was to develop new excipients, based on acrylic monomers (ethyl acrylate, methyl methacrylate, and butyl methacrylate) for use in direct compression (DC). The polymeric excipients were prepared by suspension and emulsion polymerization reactions and were characterized by FTIR to confirm the polymerization reaction. For the success of direct compression, excipients must present good flow and compactability properties. Therefore, excipients were submitted to analysis of morphology (SEM), particle size and size distribution by laser diffraction, and powder density (bulk density and tapped density). The Carr index, Hausner ratio, flow ratio, and cotangent of the angle α were determined. Thereafter, the polymeric excipients were used to prepare inert matrices by DC using propranolol hydrochloride (PHCl) as a model drug. The tablets were evaluated for average weight, breaking force, and friability tests. The release profiles were determined, and the dissolution kinetics was studied. The results indicated that matrices prepared from excipients obtained by suspension polymerization (NWCB and PECB) presented a release of PHCl for a period exceeding 12h, most likely due to the higher micromeritic properties. The results suggested that the increase in the percentage of polymers, as well as in the compression time, resulted in a higher hardness of the matrix with a reduced rate release of the PHCl. Finally, in vitro preliminary tests showed that the polymeric excipients produced were non-toxic for the gingival fibroblasts.
authors.affiliation: Universidade Federal de Minas Gerais - UFMG, Escola de Engenharia, Departamento de Engenharia de Materiais, Belo Horizonte, MG, Brazil. pharmacotecnica@yahoo.com.br
authors.forename: J C O
authors.initials: JC
authors.lastname: Villanova
authors.forename: E
authors.initials: E
authors.lastname: Ayres
authors.forename: R L
authors.initials: RL
authors.lastname: Oréfice
mesh_terms: D000179:Acrylates / Q000138:chemical synthesis / Q000737:chemistry* / Q000633:toxicity; D002460:Cell Line; D002470:Cell Survival / Q000187:drug effects; D003692:Delayed-Action Preparations / Q000737:chemistry*; D004339:Drug Compounding / Q000379:methods*; D015195:Drug Design; D005079:Excipients / Q000138:chemical synthesis / Q000737:chemistry* / Q000633:toxicity; D005347:Fibroblasts / Q000187:drug effects; D005881:Gingiva / Q000166:cytology / Q000187:drug effects; D006801:Humans; D008689:Methacrylates / Q000737:chemistry; D020366:Methylmethacrylate / Q000737:chemistry; D008855:Microscopy, Electron, Scanning; D010316:Particle Size; D012995:Solubility; D017550:Spectroscopy, Fourier Transform Infrared; D013499:Surface Properties; D013607:Tablets
chemical_list: D000179:Acrylates; D003692:Delayed-Action Preparations; D005079:Excipients; D008689:Methacrylates; D013607:Tablets; D020366:Methylmethacrylate; C040833:ethyl acrylate; C016284:butyl methacrylate