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US4530840A Expired / Lapsed US ⏱️ 0.0 years remaining

Injectable, long-acting microparticle formulation for the delivery of anti-inflammatory agents

Assignee: Stolle Research and Development Corp
•
Filing: 1982-07-29
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Granted: 1985-07-23
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Expires: 2002-07-29
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Abstract

Abstract An anti-inflammatory agent containing microparticle composition prepared by a process, comprising (a) dissolving or dispersing an anti-inflammatory agent in a solvent and dissolving a biocompatible and biodegradable wall forming material in said solvent; (b) dispersing said solvent containing said anti-inflammatory agent and wall forming material in a continuous phase processing medium; (c) evaporating a portion of said solvent from said dispersion of step (b), thereby forming microparticles containing said anti-inflammatory agent in the suspension; and (d) extracting the remainder of the solvent from said microcapsules.

Inventors

  • 👤 Thomas R. Tice
  • 👤 Danny H. Lewis
  • 👤 Donald R. Cowsar
  • 👤 Lee R. Beck

Bibliographic Details

Application Number —
Jurisdiction US
Data Source google_patents
Last Synchronized 2026-10-23 19:26
CPC Classifications
A; A61; A61K; A61K9/00; A61K9/14; A61K9/16; A61K9/1682; A61K9/1694; A61K9/1605; A61K9/1629; A61K9/1641; A61K9/1647; A61P; A61P29/00

Claims Analysis

Total Claims: 13
Claim 1
Independent Claim 135 words
An anti-inflammatory agent containing microparticle composition prepared by a process, comprising: (a) dissolving or dispersing an anti-inflammatory agent selected from the group consisting of a prednisolone, a triamicinolone, a dexamethasone and a β-methasone in a solvent selected from the group consisting of acetone, a halogenated hydrocarbon, an aromatic hydrocarbon. a halogenated aromatic hydracarbon, a cyclic ether, an alcohol and water and dissolving a biocompatible and biodegradable wall forming material in said solvent; (b) dispersing said solvent containing said anti-inflammatory agent and wall forming material in a continuous phase processing medium of water, toluene, xylene, a synthetic oil or a natural oil; (c) evaporating a portion of said solvent from said dispersion of step (b), thereby forming microparticles containing said anti-inflammatory agent in the suspension; and (d) extracting the remainder of the solvent from said microparticles.
Claim 2
Dependent Claim 135 words
An anti-inflammatory agent containing microparticle composition prepared by a process, comprising: (a) dissolving or dispersing an anti-inflammatory agent selected from the group consisting of a prednisolone, a triamicinolone, a dexamethasone and a β-methasone in a solvent selected from the group consisting of acetone, a halogenated hydrocarbon, an aromatic hydrocarbon. a halogenated aromatic hydracarbon, a cyclic ether, an alcohol and water and dissolving a biocompatible and biodegradable wall forming material in said solvent; (b) dispersing said solvent containing said anti-inflammatory agent and wall forming material in a continuous phase processing medium of water, toluene, xylene, a synthetic oil or a natural oil; (c) evaporating a portion of said solvent from said dispersion of step (b), thereby forming microparticles containing said anti-inflammatory agent in the suspension; and (d) extracting the remainder of the solvent from said microparticles.
Claim 3
Dependent Claim 33 words
The composition of claim 1, wherein the polymeric matrix material of said microparticles is poly-d, 1-lactic acid, polyglycolic acid, copolymers of mixed d,1-lactic acid and glycolic acid, copolyoxalates, polycaprolactone, or poly (lactic acid-caprolactone).
Claim 4
Dependent Claim 25 words
The composition of claim 1, wherein said microparticles are loaded with 1 to 75 wt. % of said anti-inflammatory agent based on said polymeric matrix.
Claim 5
Dependent Claim 16 words
The composition of claim 1, wherein said microparticles range in size from 1 to 200 microns.
Claim 6
Dependent Claim 15 words
The composition of claim 1, wherein said microparticles are formulated in a liquid injectable vehicle.
Claim 7
Dependent Claim 30 words
A method of treating inflammation comprising: administering microparticles of claim 1 containing a pharmaceutically effective amount of an anti-inflammatory compound in a biocompatible and biodegradable matrix material to a subject.
Claim 8
Dependent Claim 27 words
The method of claim 6, wherein said microparticles are formed of a matrix of polymeric d,1-lactic acid, glycolic acid, copolymers thereof, copolyoxalates, polycaprolactone or poly (lactic acid-caprolactone).
Claim 9
Dependent Claim 21 words
The method of claim 6, wherein from microgram to milligram quantities of said corticosteroid are administered per day to a subject.
Claim 10
Dependent Claim 23 words
The method of claim 6, wherein said microparticles are administered by injection into the area of the inflammed joints of an affected subject.
Claim 11
Dependent Claim 17 words
The method of claim 6, wherein said injectable microparticles are formulated as microparticles in a liquid vehicle.
Claim 12
Dependent Claim 13 words
The method of claim 10, wherein said liquid vehicle is physiological saline solution.
Claim 13
Dependent Claim 13 words
The method of claim 6, wherein said micro-particles are administered by intra-muscular injection.

References Cited (Backward Citations)

US4066747A Cited
US4196188A Cited
US4328204A Cited
US4374121A Cited
US4267173A Cited
US4389330A Cited

USPTO Annuity & Maintenance Windows

Annuity Stage Window Opens Payment Deadline Surcharge Period Until Estimated Fee Status
3.5 Years (Year 4) 1988-07-22 1989-01-21 1989-07-23 $2000.00 Window Closed / Lapsed
7.5 Years (Year 8) 1992-07-22 1993-01-21 1993-07-23 $3760.00 Window Closed / Lapsed
11.5 Years (Year 12) 1996-07-22 1997-01-21 1997-07-23 $7700.00 Window Closed / Lapsed

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