An oral controlled release matrix pellet formulation containing nanocrystalline ketoprofen

Int J Pharm. 2001 May 21;219(1-2):81-7. doi: 10.1016/s0378-5173(01)00628-7.

Abstract

A controlled release pellet formulation using a NanoCrystal colloidal dispersion of ketoprofen was developed. In order to be able to process the aqueous NanoCrystal colloidal dispersion into a hydrophobic solid dosage form a spray drying procedure was used. The in vitro dissolution profiles of wax based pellets loaded with nanocrystalline ketoprofen are compared with the profiles of wax based pellets loaded with microcrystalline ketoprofen and of a commercial sustained release ketoprofen formulation. Pellets were produced using a melt pelletisation technique. All pellet formulations were composed of a mixture of microcrystalline wax and starch derivatives. The starch derivatives used were waxy maltodextrin and drum dried corn starch. Varying the concentration of drum dried corn starch increased the release rate of ketoprofen but the ketoprofen recovery remained problematic. To increase the dissolution yield surfactants were utilised. The surfactants were either added during the production process of the NanoCrystal colloidal dispersion (sodium laurylsulphate) or during the pellet manufacturing process (Cremophor RH 40). Both methods resulted in a sustained but complete release of nanocrystalline ketoprofen from the matrix pellet formulations.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Administration, Oral
  • Anti-Inflammatory Agents, Non-Steroidal / administration & dosage*
  • Anti-Inflammatory Agents, Non-Steroidal / pharmacokinetics*
  • Crystallization
  • Excipients
  • Freeze Drying
  • Hydrogen-Ion Concentration
  • Ketoprofen / administration & dosage*
  • Ketoprofen / chemistry
  • Ketoprofen / pharmacokinetics*
  • Microscopy, Electron, Scanning
  • Porosity
  • Solubility
  • Starch
  • Surface Properties
  • Tablets, Enteric-Coated
  • Waxes
  • X-Ray Diffraction

Substances

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