In vivo evaluation of matrix pellets containing nanocrystalline ketoprofen

Int J Pharm. 2002 Jun 20;240(1-2):79-84. doi: 10.1016/s0378-5173(02)00114-x.

Abstract

The aim of this study was to evaluate the in-vivo behaviour of matrix pellets formulated with nanocrystalline ketoprofen after oral administration to dogs. No significant differences in AUC-values were seen between pellet formulations containing nanocrystalline or microcrystalline ketoprofen and a commercial ketoprofen formulation (reference: Rofenid 200 Long Acting). C(max) of the formulations containing nano- or microcrystalline ketoprofen was significantly higher compared to reference, whereas t(max) was significantly lower. The in-vivo burst release observed for the spray dried nanocrystalline ketoprofen matrix pellets was reduced following compression of the pellets in combination with placebo wax/starch pellets. These matrix tablets sustained the ketoprofen plasma concentrations during 5.6 and 5.4 h for formulations containing nano- and microcrystalline ketoprofen, respectively.

MeSH terms

  • Administration, Oral
  • Animals
  • Anti-Inflammatory Agents, Non-Steroidal / administration & dosage
  • Anti-Inflammatory Agents, Non-Steroidal / blood
  • Anti-Inflammatory Agents, Non-Steroidal / pharmacokinetics*
  • Biological Availability
  • Chromatography, High Pressure Liquid
  • Dogs
  • Female
  • Ketoprofen / administration & dosage
  • Ketoprofen / blood
  • Ketoprofen / pharmacokinetics*
  • Male
  • Nanotechnology*
  • Particle Size
  • Solubility
  • Tablets, Enteric-Coated
  • Time Factors

Substances

  • Anti-Inflammatory Agents, Non-Steroidal
  • Tablets, Enteric-Coated
  • Ketoprofen