A1 Refereed original research article in a scientific journal
Tablet preformulations of indomethacin-loaded mesoporous silicon microparticles
Authors: Tahvanainen M, Rotko T, Makila E, Santos HA, Neves D, Laaksonen T, Kallonen A, Hamalainen K, Peura M, Serimaa R, Salonen J, Hirvonen J, Peltonen L
Publisher: ELSEVIER SCIENCE BV
Publication year: 2012
Journal: International Journal of Pharmaceutics
Journal name in source: INTERNATIONAL JOURNAL OF PHARMACEUTICS
Journal acronym: INT J PHARMACEUT
Number in series: 1-2
Volume: 422
Issue: 1-2
First page : 125
Last page: 131
Number of pages: 7
ISSN: 0378-5173
DOI: https://doi.org/10.1016/j.ijpharm.2011.10.040
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. (C) 2011 Elsevier B.V. All rights reserved.
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. (C) 2011 Elsevier B.V. All rights reserved.
Keywords:
Dissolution rate, Indomethacin, Mesoporous silicon, Microparticles, Poorly soluble drug, Tablet formulation
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