Insoluble drug delivery
AssigneesSkyePharma Canada Inc., Board of Regents, The University of Texas System
InventorsInge B Henriksen, Awadesh K. Mishra, Gary W. Pace, Keith P. Johnston, Simon Mawson
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Abstract
Particles of water insoluble biologically active compounds, particularly water-insoluble drugs, with an average size of 100 nm to about 300 nm, are prepared by dissolving the compound in a solution then spraying the solution into compressed gaz, liquid or supercritical fluid in the presence of appropriate surface modifiers.
Claims69
A process of preparing a surface modifier-stabilized aqueous suspension of submicron sized surface modified microparticles with an average particle size up to 300 nm and a narrow size distribution, wherein 99% of the microparticles produced are below 500 nm, without particle aggregation or flocculation of a water-insoluble or substantially water-insoluble biologically active compound, said process comprising:
- (1) dissolving a water-insoluble or substantially water-insoluble biologically active compound in a solvent for said biologically active compound to form a solution;
- and
- (2) spraying the solution prepared in (1) into a compressed gas, compressed liquid or supercritical fluid miscible with said solution but antisolvent for said water-insoluble compound in the presence of an agitated aqueous phase and a surface modifier which may be present in said agitated aqueous phase or in a compressed gas, compressed liquid or supercritical fluid or both.
A process of preparing a surface modifier-stabilized aqueous suspension of submicron sized surface modified microparticles with an average particle size up to 300 nm and a narrow size distribution, wherein 99% of the microparticles produced are below 500 nm, without particle aggregation or flocculation of a water-insoluble or substantially water-insoluble biologically active compound, said process comprising:
- (1) dissolving a water-insoluble or substantially water-insoluble biologically active compound in a compressed fluid to form a solution;
- (2) preparing an agitated aqueous phase containing a surface modifier;
- and
- (3) spraying the compressed fluid solution of (1) into the agitated aqueous phase of (2).
A process of preparing a surface modifier-stabilized aqueous suspension of surface modified microparticles comprising:
- (1) dissolving a water-insoluble or substantially water-insoluble biologically active compound in a solvent for said biologically active compound to form a solution;
- and
- (2) spraying the solution prepared in (1) into a compressed gas, compressed liquid or supercritical fluid miscible with said solution but antisolvent for said compound in the presence of an aqueous phase containing a surface modifier.
A process of preparing a surface modifier stabilized aqueous suspension of surface modified microparticles with an average particle size up to 300 nm and a narrow size distribution, wherein 99% of the microparticles produced are below 500 nm comprising:
- (1) dissolving a water-insoluble or substantially water-insoluble biologically active compound in a compressed fluid to form a solution;
- (2) preparing an aqueous phase containing a surface modifier;
- and
- (3) spraying the compressed fluid solution of (1) into the aqueous phase of (2).
A process of preparing microparticles of a water-insoluble or substantially water-insoluble biologically active compound comprising:
- (1) dissolving a water-insoluble or substantially water-insoluble biologically active compound in a compressed fluid;
- (2) preparing an aqueous phase containing a surface modifier comprising a phospholipid;
- and
- (3) spraying the compressed fluid solution of (1) into the aqueous phase of (2) to form microparticles of the compound.
A process of preparing microparticles of a water-insoluble or substantially water-insoluble biologically active compound comprising:
- (1) dissolving a water-insoluble or substantially water-insoluble biologically active compound in a compressed fluid;
- (2) preparing an aqueous phase containing a surface modifier comprising a mixture of two or more surfactants;
- and
- (3) spraying the compressed fluid solution of (1) into the aqueous phase of (2) to form microparticles of the compound.
A process of preparing microparticles of a water-insoluble or substantially water-insoluble biologically active compound comprising:
- (1) dissolving a water-insoluble or substantially water-insoluble biologically active compound in a compressed fluid comprising carbon dioxide;
- (2) preparing an aqueous phase containing a surface modifier;
- and
- (3) spraying the compressed fluid solution of (1) into the aqueous phase of (2) to form microparticles of the compound.
Dependencies are inferred from the claim text.