Surface modified drug nanoparticles
AssigneeSterling Drug Inc.
InventorsGary G. Liversidge, Kenneth C. Cundy, John F. Bishop, David A. Czekai
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Abstract
Dispersible particles consisting essentially of a crystalline drug substance having a surface modifier adsorbed on the surface thereof in an amount sufficient to maintain an effective average particle size of less than about 400 nm, methods for the preparation of such particles and dispersions containing the particles. Pharmaceutical compositions containing the particles exhibit unexpected bioavailability and are useful in methods of treating mammals.
Claims20
Particles consisting essentially of 99.9-10% by weight of a crystalline drug substance having a solubility in water of less than 10 mg/ml, said drug substance having a non-crosslinked surface modifier adsorbed on the surface thereof in an amount of 0.1-90% by weight and sufficient to maintain an effective average particle size of less than about 400 nm.
Particles consisting essentially of 99.9-10% by weight of a crystalline drug substance having a solubility in water of less than 10 mg/ml, said drug substance having a non-crosslinked surface modifier absorbed on the surface thereof in an amount of 0.1-90% by weight and sufficient to maintain an effective average particle size of less than about 400 nm, wherein said drug substance is selected from the group consisting of Danazol, 5.alpha.,17.alpha.,-1'-(methylsulfonyl)-1'H-pregn-20-yno-[3,2-c]-pyrazol-1 7-ol, piposulfam, piposulfan, camptothecin, and ethyl-3,5-diacetamido-2,4,6-triiodobenzoate.
Particles consisitng essentially of 80-40% by weight of crystalline danazol having polyvinyl pyrrolidone adsorbed on the surface thereof in an amount of 20-60% by weight and sufficient to maintain an effective average particle size of less than about 100 nm.
Particles consisting essentially of 99.9-10% by weight of crystalline 5.alpha., 17.alpha.,-1'-(methylsulfonyl)-1'H-pregn-20-yno-pyrazol-17-ol having an ethylene oxide propylene-oxide block copolymer adsorbed on the surface thereof in an amount of 0.1-90% by weight and sufficient to maintain an effective average particle size of less than about 400 nm.
Dependencies are inferred from the claim text.