A1 Vertaisarvioitu alkuperäisartikkeli tieteellisessä lehdessä
Tablet preformulations of indomethacin-loaded mesoporous silicon microparticles
Tekijät: 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
Kustantaja: ELSEVIER SCIENCE BV
Julkaisuvuosi: 2012
Journal: International Journal of Pharmaceutics
Tietokannassa oleva lehden nimi: INTERNATIONAL JOURNAL OF PHARMACEUTICS
Lehden akronyymi: INT J PHARMACEUT
Numero sarjassa: 1-2
Vuosikerta: 422
Numero: 1-2
Aloitussivu: 125
Lopetussivu: 131
Sivujen määrä: 7
ISSN: 0378-5173
DOI: https://doi.org/10.1016/j.ijpharm.2011.10.040
Tiivistelmä
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.
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