Micromilling and co-micromilling of small quantities of poorly water-s
Instrument: Precellys® 24 Dual
Sample: Ketoprofen
Protocol:
- Precellys kits: 03961-1-008 (2.8mm metal beads).
- Sample: 200 mg of Ketoprofen (as a model poorly water-soluble API) blended with various excipients (ratio 70/30) in a mortar (physical mixture).
- Run the Precellys at 5500 rpm, 3x30sec (10s break).
- Controls made on the produces formulations include: in vitro dissolution profile, scanning electronic microscopy, X-Ray diffraction and DSC.
Results:
A significant increase of the Ketoprofen dissolution rate is observed after co-micromilling using various excipients, compared to non micromilled material. This increase is observed for excipients which have or do not have solubilizing properties (surfactant vs PVP derivatives)
Significant particle size reduction is observed for comicromilled formulations such as Crospovidone-Ketoprofen. Drug dissolution following comicronisation has been significantly improved. No amorphisation of the API was found after the process.
