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Claims for Patent: 5,145,684

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Claims for Patent: 5,145,684

Title: Surface modified drug nanoparticles
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.
Inventor(s): Liversidge; Gary G. (West Chester, PA), Cundy; Kenneth C. (Pottstown, PA), Bishop; John F. (Rochester, NY), Czekai; David A. (Honeoye Falls, NY)
Assignee: Sterling Drug Inc. (New York, NY)
Application Number:07/647,105
Patent Claims: 1. 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.

2. The particles of claim 1 having an effective average particle size of less than 250 nm.

3. The particles of claim 1 having an effective average particle size of less than 100 nm.

4. The particles of claim 1 wherein said drug substance is selected from analgesics, anti-inflammatory agents, anthelmintics, anti-arrhythmic agents, antibiotics, anticoagulants, antidepressants, antidiabetic agents, antiepileptics, antihistamines, antihypertensive agents, antimuscarinic agents, antimycobacterial agents, antineoplastic agents, immunosuppressants, antithyroid agents, antiviral agents, anxiolytic sedatives, astringents, beta-adrenoceptor blocking agents, contrast media, corticosteroids, cough suppressants, diagnostic agents, diagnostic imaging agents, diuretics, dopaminergics, haemostatics, immuriological agents, lipid regulating agents, muscle relaxants, parasympathomimetics, parathyroid calcitonin, prostaglandins, radio-pharmaceuticals, sex hormones, anti-allergic agents, stimulants, sympathomimetics, thyroid agents, vasodilators and xanthines.

5. The particles of claim 1 wherein said drug substance is a steroid.

6. 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.

7. The particles of claim 1 wherein said surface modifier is selected from the group consisting of gelatin, casein, lecithin, gum acacia, cholesterol, tragacanth, stearic acid, benzalkonium chloride, calcium stearate, glyceryl monostearate, cetostearyl alcohol, cetomacrogol emulsifying wax, sorbitan esters, polyoxyethylene alkyl ethers, polyoxyethylene caster oil derivatives, polyoxyethylene sorbitan fatty acid esters, polyethylene glycols, polyoxyethylene stearates, colloidol silicon dioxide, phosphates, sodium dodecylsulfate, carboxymethylcellulose calcium, carboxymethylcellulose sodium, methylcellulose, hydroxyethylcellulose, hydroxypropylcellulose, hydroxypropylmethycellulose phthalate, noncrystalline cellulose, magnesium aluminum silicate, triethanolamine, polyvinyl alcohol, and polyvinylpyrrolidone.

8. The particles of claim 1 wherein said surface modifier is selected from the group consisting of polyvinylpyrrolidone, an ethylene oxide-propylene oxide block copolymer, lecithin, an alkyl aryl polyether sulfonate, gum acacia, sodium dodecylsulfate, and a dioctylester of sodium sulfosuccinic acid.

9. 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.

10. 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.

11. A stable dispersion consisting essentially of a liquid dispersion medium and the particles of claim 1.

12. The dispersion of claim 11 wherein said dispersion medium is water.

13. The dispersion of claim 11 wherein said dispersion medium is selected from the group consisting of safflower oil, ethanol, t-butanol, hexane and glycol.

14. A pharmaceutical composition comprising the particles of claim 1 and a pharmaceutically acceptable carrier therefor.

15. A method of treating a mammal comprising the step of administering to the mammal an effective amount of the pharmaceutical composition of claim 14.

16. A method of preparing the particles of claim 1 comprising the steps of dispersing a drug substance in a liquid dispersion medium and wet grinding said drug substance in the presence of rigid grinding media having an average particle size of less than 3 mm and a surface modifier to reduce the particle size of said drug substance to an effective average particle size of less than about 400 nm.

17. A method of preparing the particles of claim 1 comprising the steps of dispersing a drug substance in a liquid dispersion medium, wet grinding said drug substance in the presence of rigid grinding media having an average particle size of less than 3 mm, thereafter contacting said drug substance with a surface modifier by mixing said surface modifier with said dispersion medium to form particles having an effective average particle size of less than about 400 nm.

18. The method of claim 17 further including the step of subjecting the dispersion medium containing said drug substance and said surface modifier to ultrasonic energy.

19. The method of claim 16 wherein said grinding media have an average particle size of less than 1 mm.

20. The method of claim 16 wherein said grinding media have a density greater than 3 g/cm.sup.3.
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