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US5622938A Expired / Lapsed US ⏱️ 0.0 years remaining

Sugar base surfactant for nanocrystals

Assignee: PARTICULATE PROSPECTS CORP
•
Filing: 1995-05-19
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Granted: 1997-04-22
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Expires: 2015-05-19
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Abstract

Abstract Dispersible particles consisting essentially of a crystalline drug substance having a surface modifier having the formula: <IMAGE> +TR <IMAGE> wherein R is phenyl-(CH2)10CO or C12H25NHCO 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

  • 👤 Sui-Ming Wong

Bibliographic Details

Application Number —
Jurisdiction US
Data Source google_patents
Last Synchronized 2026-11-06 04:40
CPC Classifications
B; B82; B82Y; B82Y5/00; A; A61; A61K; A61K49/00; A61K49/04; A61K49/0433; A61K49/0447; A61K49/0476; A61K49/0485; A61K49/049; A61K9/00; A61K9/14; A61K9/141; A61K9/145

Claims Analysis

Total Claims: 22
Claim 1
Independent Claim 52 words
Particles consisting essentially of a crystalline drug substance having a surface modifier having the structure: ##STR7## wherein R is Ph(CH 2 ) 10 CO or C 12 H 25 NHCO 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 52 words
Particles consisting essentially of a crystalline drug substance having a surface modifier having the structure: ##STR7## wherein R is Ph(CH 2 ) 10 CO or C 12 H 25 NHCO adsorbed on the surface thereof in an amount sufficient to maintain an effective average particle size of less than about 400 nm.
Claim 3
Dependent Claim 16 words
The particles of claim 1 having an effective average particle size of less than 250 nm.
Claim 4
Dependent Claim 16 words
The particles of claim 1 having an effective average particle size of less than 100 nm.
Claim 5
Dependent Claim 80 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, 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.
Claim 6
Dependent Claim 13 words
The particles of claim 1 wherein the drug substance is a diagnostic agent.
Claim 7
Dependent Claim 11 words
The particles of claim 5 wherein the drug substance is ##STR8##
Claim 8
Dependent Claim 11 words
The particles of claim 5 wherein the drug substance is ##STR9##
Claim 9
Dependent Claim 11 words
The particles of claim 1 wherein the surface modifier is ##STR10##
Claim 10
Dependent Claim 11 words
The particles of claim 1 wherein the surface modifier is ##STR11##
Claim 11
Dependent Claim 38 words
Particles consisting essentially of a discrete phase of 5,17,-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 12
Dependent Claim 38 words
Particles consisting essentially of a discrete phase of 5,17,-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 13
Dependent Claim 16 words
A stable dispersion consisting essentially of a liquid dispersion medium and the particles of claim 1.
Claim 14
Dependent Claim 11 words
The dispersion of claim 10 wherein said dispersion medium is water.
Claim 15
Dependent Claim 23 words
The dispersion of claim 10 wherein said dispersion medium is selected from the group consisting of safflower oil, ethanol, t-butanol, hexane and glycol.
Claim 16
Dependent Claim 15 words
A pharmaceutical composition comprising the particles of claim 1 and a pharmaceutically acceptable carrier therefor.
Claim 17
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 13.
Claim 18
Dependent Claim 14 words
Particles of claim 1 in a stable dispersion containing with a liquid dispersion medium.
Claim 19
Dependent Claim 9 words
Particles of claims 1 in a stable aqueous dispersion.
Claim 20
Dependent Claim 25 words
Particles of claim 1 in a stable dispersion containing with a liquid dispersion medium, wherein the medium is safflower oil, ethanol, t-butanol, hexane or glycol.
Claim 21
Dependent Claim 16 words
Particles of claim 1 in a pharmaceutical composition containing a pharmaceutical acceptable carrier for the particles.
Claim 22
Dependent Claim 20 words
Particles of claim 1 used in a method of treating a mammal wherein the particles are administered to the mammal.

References Cited (Backward Citations)

US4107288A Cited
US4540602A Cited
US5118528A Cited
US5145684A Cited
US5403922A Cited

USPTO Annuity & Maintenance Windows

Annuity Stage Window Opens Payment Deadline Surcharge Period Until Estimated Fee Status
3.5 Years (Year 4) 2000-04-21 2000-10-21 2001-04-22 $2000.00 Window Closed / Lapsed
7.5 Years (Year 8) 2004-04-21 2004-10-21 2005-04-22 $3760.00 Window Closed / Lapsed
11.5 Years (Year 12) 2008-04-21 2008-10-21 2009-04-22 $7700.00 Window Closed / Lapsed

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