EP0499299A2
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Surface modified drug nanoparticles
Assignee: Perrigo Pharma International DAC
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Filing: 1992-01-20
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Granted: —
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Expires: 2012-01-20
Abstract
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.
Inventors
- 👤 Gary c/o Sterling Winthrop Inc. Liversidge
- 👤 Kenneth c/o Sterling Winthrop Inc. Cundy
- 👤 John c/o Sterling Winthrop Inc. Bishop
- 👤 David c/o Sterling Winthrop Inc. Czekai
Bibliographic Details
Application Number
—
Jurisdiction
EP
Data Source
google_patents
Last Synchronized
2026-11-07 08:40
CPC Classifications
A; A61; A61K; A61K49/00; A61K49/04; A61K49/0433; A61K49/0447; A61K49/0476; A61K49/0485; A61K49/049; A61K9/00; A61K9/10; A61K49/0409; A61K49/0414; A61K49/0423; A61K49/0428; A61K9/14; A61K9/141; A61K9/145; A61K9/146; B; B82; B82Y; B82Y5/00
Claims Analysis
Total Claims: 20
Claim 1
Independent Claim
34 words
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.
Claim 2
Dependent Claim
16 words
The particles of claim 1 having an effective average particle size of less than 250 nm.
Claim 3
Dependent Claim
16 words
The particles of claim 1 having an effective average particle size of less than 100 nm.
Claim 4
Dependent Claim
92 words
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, blood products and substitutes, cardiac suppressants agents, contrast media, corticosteroids, cough suppressants, diagnostic agents, diagnostic imaging agents, diuretics, dopaminergics, haemostatics, immunological agents, lipid regulating agents, muscle relaxants, parasympathomimetics, parathyroid calcitonin and biphosphonates, prostaglandins, radio-pharmaceuticals, sex hormones, steroids, anti-allergic agents, stimulants and anoretics, sympathomimetics, thyroid agents, vasodilators and xanthines.
Claim 5
Dependent Claim
29 words
The particles of claim 1 wherein said drug substance is selected from an antiviral agent, an anti-inflammatory agent, an antineoplastic agent, a radiopharmaceutical agent, and a diagnostic imaging agent.
Claim 6
Dependent Claim
23 words
The particles of claim 1 wherein said drug substance is selected from the group consisting of Danazol, 5α,17α,-1'-(methylsulfonyl)-1'H-pregn-20-yno-[3,2-c]-pyrazol-17-ol, piposulfam, piposulfan, camptothecin, and ethyl-3,5-diacetamido-2,4,6-triiodobenzoate.
Claim 7
Dependent Claim
96 words
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 castor oil derivatives, polyoxyethylene sorbitan fatty acid esters, polyethylene glycols, polyoxyethylene stearates, colloidol silicon dioxide, phosphates, sodium dodecylsulfate, carboxymethylcellulose calcium, carboxymethylcellulose sodium, methylcellulose, hydroxyethylcellulose, hydroxypropylcellulose, hydroxypropylmethylcellulose phthalate, noncrystalline cellulose, magnesium aluminum silicate, triethanolamine, polyvinyl alcohol, polyvinylpyrrolidone, an ethylene oxide-propylene oxide block copolymer, an alkyl aryl polyether sulfonate, and a dioctylester of sodium sulfosuccinic acid.
Claim 8
Dependent Claim
29 words
The particles of claim 1 wherein said surface modifier is present in an amount of 0.1 to 90% by weight based on the total weight of the dry particle.
Claim 9
Dependent Claim
34 words
Particles according to claim 1 consisting essentially of crystalline Danazol having polyvinyl pyrrolidone adsorbed on the surface thereof in an amount sufficient to maintain an effective average particle size of less than 100 nm.
Claim 10
Dependent Claim
39 words
Particles according to claim 1 consisting essentially of crystalline 5α,17α,-1'-(methylsulfonyl)-1'H-pregn-20-yno-[3,2-c]pyrazol-17-ol having an ethylene oxide propylene-oxide block copolymer adsorbed on the surface thereof in an amount sufficient to maintain an effective average particle size of less than about 400 nm.
Claim 11
Dependent Claim
19 words
A stable dispersion consisting essentially of a liquid dispersion medium and the particles of any one of claims 1-10.
Claim 12
Dependent Claim
11 words
The dispersion of claim 11 wherein said dispersion medium is water.
Claim 13
Dependent Claim
23 words
The dispersion of claim 11 wherein said dispersion medium is selected from the group consisting of safflower oil, ethanol, t-butanol, hexane and glycol.
Claim 14
Dependent Claim
18 words
A pharmaceutical composition comprising the particles of any one of claims 1-10 and a pharmaceutically acceptable carrier therefor.
Claim 15
Dependent Claim
24 words
A method of treating a mammal comprising the step of administering to the mammal an effective amount of the pharmaceutical composition of claim 14.
Claim 16
Dependent Claim
70 words
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.
Claim 17
Dependent Claim
78 words
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, and 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.
Claim 18
Dependent Claim
25 words
The method of claim 18 further including the step of subjecting the dispersion medium containing said drug substance and said surface modifier to ultrasonic energy.
Claim 19
Dependent Claim
18 words
The method of claim 17 or 18 wherein said grinding media have a density greater than 3 g/cm³.
Claim 20
Dependent Claim
21 words
The method of claim 17 or 18 wherein said grinding media have an average particle size of less than 1 mm.
References Cited (Backward Citations)
No citation records indexed.
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