Processes to generate submicron particles of water-insoluble compounds
AssigneeRTP Pharma Inc.
InventorsGary W. Pace, Michael G. Vachon, Awadhesh K. Mishra, Inge B. Henrikson, Val Krukonis
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Abstract
Submicron particles of water-insoluble compounds, particularly drugs, are prepared by simultaneously stabilizing microparticulate suspensions of same with surface modifier molecules by rapid expansion into an aqueous medium from a compressed solution of the compound and surface modifiers in a liquefied gas and optionally homogenizing the aqueous suspension thus formed with a high pressure homogenizer.
Claims15
A process of preparing a stable suspension of sub-micron particles of a water-insoluble or substantially water-insoluble biologically active compound of up to 2000 nm in size comprising the successive steps of:
- (a) dissolving a water-insoluble or substantially water-insoluble biologically active compound and a first surface modifier in a liquefied compressed gas solvent therefor and forming a solution of greater than 1% w/w of said compound in said solvent and thereafter;
- (b) expanding the compressed fluid solution prepared in step (a) into water or aqueous solution containing a second surface modifier and water-soluble agents thereby producing a suspension of microparticles, and thereafter
- (c) homogenizing the suspension of step (b) at high pressure.
Dependencies are inferred from the claim text.