Influence of cryogenic grinding on properties of a self-emulsifying formulation

Int J Pharm. 2004 Jun 18;278(1):79-89. doi: 10.1016/j.ijpharm.2004.02.033.

Abstract

Recently, self-emulsifying drug delivery systems (SEDDS) have been developed as a method to deliver lipophilic drugs. Gelucire 44/14 is an excipient, from the lauroyl macrogolglycerides family, producing a fine oil-in-water emulsion when introduced into an aqueous phase under gentle agitation as SEDDS, improving thereby solubility of poorly water-soluble drugs and their bioavailability. The aims of this study were to process Gelucire 44/14 into a powder by cryogenic grinding to produce solid oral dosage forms and to investigate influence of this process on different properties of a formulation made of Gelucire 44/14 and ketoprofen (90/10). Cryogenic grinding produced Gelucire 44/14 in a powder form and this process did not change its physical properties, emulsification capacities and dissolution performances of the formulation tested. However, interactions took place between ketoprofen and Gelucire 44/14 with a decrease of the melting peak and a reduction of the droplet size of the formed emulsion. The influence of drug-Gelucire 44/14 interactions must be investigated case by case in any formulations.

MeSH terms

  • Chemistry, Pharmaceutical
  • Drug Delivery Systems / methods
  • Emulsifying Agents / administration & dosage
  • Emulsifying Agents / chemistry*
  • Freeze Drying
  • Microscopy, Electron, Scanning
  • Polyethylene Glycols / administration & dosage
  • Polyethylene Glycols / chemistry*
  • Solubility / drug effects
  • Technology, Pharmaceutical / methods*

Substances

  • Emulsifying Agents
  • gelucire 44-14
  • Polyethylene Glycols