title: Tablet preformulations of indomethacin-loaded mesoporous silicon microparticles.
abstract: In this study, indomethacin-loaded thermally oxidized mesoporous silicon microparticles (TOPSi-IMC) were formulated into tablets with excipients in order to improve the dissolution and permeability properties of the poorly soluble drug. Formulations of TOPSi-IMC particles and excipients were prepared at different TOPSi-IMC particle ratios (25, 30 and 35%). The formulations were compressed by direct compression technique with a single punch tablet machine. For comparison, a formulation containing the bulk IMC (indomethacin) and the same excipients without thermally oxidized mesoporous silicon microparticles particles (TOPSi) was prepared and compressed into tablets. The TOPSi-IMC tablets were characterised according to weight, thickness, crushing strength, disintegration time and dissolution rate. The results of this study show that TOPSi-IMC particles can be compressed to a conventional tablet. The release rate of the drug and its permeation across intestinal cells model (Caco-2) from TOPSi-IMC tablets was improved compared to the bulk IMC tablets. The dissolution rate and permeability of IMC from the tablets decreased with increasing ratio of the TOPSi-IMC particles in the formulation. The phenomenon is, presumably, a result of the loss of unique pore structure of the particles due to deformation of the particles under the compression load.
authors: Division of Pharmaceutical Technology, Faculty of Pharmacy, FI-00014, University of Helsinki, Finland. maria.tahvanainen@helsinki.fi
authors: Maria
authors: M
authors: Tahvanainen
authors: Tanja
authors: T
authors: Rotko
authors: Ermei
authors: E
authors: Mäkilä
authors: Hélder A
authors: HA
authors: Santos
authors: Diogo
authors: D
authors: Neves
authors: Timo
authors: T
authors: Laaksonen
authors: Aki
authors: A
authors: Kallonen
authors: Keijo
authors: K
authors: Hämäläinen
authors: Marko
authors: M
authors: Peura
authors: Ritva
authors: R
authors: Serimaa
authors: Jarno
authors: J
authors: Salonen
authors: Jouni
authors: J
authors: Hirvonen
authors: Leena
authors: L
authors: Peltonen
mesh_terms: D000894:Anti-Inflammatory Agents, Non-Steroidal / Q000737:chemistry* / Q000378:metabolism; D018938:Caco-2 Cells; D002626:Chemistry, Pharmaceutical; D019245:Compressive Strength; D004337:Drug Carriers; D004339:Drug Compounding; D005079:Excipients / Q000737:chemistry; D006801:Humans; D007213:Indomethacin / Q000737:chemistry* / Q000378:metabolism; D007408:Intestinal Absorption; D007413:Intestinal Mucosa / Q000378:metabolism; D007700:Kinetics; D010084:Oxidation-Reduction; D010316:Particle Size; D010539:Permeability; D016062:Porosity; D012825:Silicon / Q000737:chemistry*; D012995:Solubility; D013607:Tablets; D013678:Technology, Pharmaceutical / Q000379:methods; D013696:Temperature
chemical_list: D000894:Anti-Inflammatory Agents, Non-Steroidal; D004337:Drug Carriers; D005079:Excipients; D013607:Tablets; D007213:Indomethacin; D012825:Silicon