Tablet preformulations of indomethacin-loaded mesoporous silicon microparticles

Int J Pharm. 2012 Jan 17;422(1-2):125-31. doi: 10.1016/j.ijpharm.2011.10.040. Epub 2011 Oct 28.

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.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Anti-Inflammatory Agents, Non-Steroidal / chemistry*
  • Anti-Inflammatory Agents, Non-Steroidal / metabolism
  • Caco-2 Cells
  • Chemistry, Pharmaceutical
  • Compressive Strength
  • Drug Carriers*
  • Drug Compounding
  • Excipients / chemistry
  • Humans
  • Indomethacin / chemistry*
  • Indomethacin / metabolism
  • Intestinal Absorption
  • Intestinal Mucosa / metabolism
  • Kinetics
  • Oxidation-Reduction
  • Particle Size
  • Permeability
  • Porosity
  • Silicon / chemistry*
  • Solubility
  • Tablets
  • Technology, Pharmaceutical / methods
  • Temperature

Substances

  • Anti-Inflammatory Agents, Non-Steroidal
  • Drug Carriers
  • Excipients
  • Tablets
  • Indomethacin
  • Silicon