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EP0142085A2 Expired / Lapsed EP ⏱️ 0.0 years remaining

Method of preparing microspheres for intravascular delivery

Assignee: Individual
•
Filing: 1984-10-26
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Granted: —
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Expires: 2004-10-26
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Abstract

Abstract @ The field of this invention is the encapsulation of therapeutic or diagnostic substances in minute capsules or spheres from which the substances are slowly released over a prescribed period of time. The general processes for preparing such capsules or spheres include coacervation or a related process by means of which liquid droplets can be encapsulated, and solid phase entrapment in which the watersoluble agent is dispersed in a solid matrix material. The method of this invention can be classified as an improved procedure for matrix encapsulation or entrapment.

Inventors

  • 👤 Benjamin Mosier

Bibliographic Details

Application Number —
Jurisdiction EP
Data Source google_patents
Last Synchronized 2026-10-30 09:50
CPC Classifications
B; B01; B01J; B01J13/00; B01J13/02; B01J13/06; B01J13/12; B01J13/125; A; A61; A61K; A61K9/00; A61K9/14; A61K9/16; A61K9/1605; A61K9/1617; A61K9/1682; A61K9/1694

Claims Analysis

Total Claims: 11
Claim 1
Independent Claim 155 words
The method of preparing microspheres containing therapeutic or diagnostic agents, comprising: (a) preparing a solution by dissolving said agent and a non-toxic matrix material in a first organic solvent in which they are mutually soluble, said matrix material being heat-liquifiable and having a congealing temperature above 100°F, said first organic solvent having a dielectric constant above 15; (b) dispersing the prepared solution in a second organic solvent to form an emulsion containing dispersed droplets of said solution in said second solvent as the continuous phase, said second organic solvent having a dielectric constant below 5, and being present in at least as great a volume as said solution; (c) removing substantially all of both of said solvents from said dispersion while maintaining said droplets at a temperature substantially below the congealing temperature of said matrix material to produce solid microspheres comprising said matrix material with said water-soluble agent distributed therein; and (d) recovering said microspheres.
Claim 2
Independent Claim 155 words
The method of preparing microspheres containing therapeutic or diagnostic agents, comprising: (a) preparing a solution by dissolving said agent and a non-toxic matrix material in a first organic solvent in which they are mutually soluble, said matrix material being heat-liquifiable and having a congealing temperature above 100°F, said first organic solvent having a dielectric constant above 15; (b) dispersing the prepared solution in a second organic solvent to form an emulsion containing dispersed droplets of said solution in said second solvent as the continuous phase, said second organic solvent having a dielectric constant below 5, and being present in at least as great a volume as said solution; (c) removing substantially all of both of said solvents from said dispersion while maintaining said droplets at a temperature substantially below the congealing temperature of said matrix material to produce solid microspheres comprising said matrix material with said water-soluble agent distributed therein; and (d) recovering said microspheres.
Claim 3
Dependent Claim 40 words
The method of claim 1 in which said matrix material is composed primarily of fatty acid glycerides in which the glycerides contain from 1 to 3 fatty acid groups ard the fatty acid groups contains from 12 to 22 carbons.
Claim 4
Dependent Claim 30 words
The method of claim 1 in which said matrix material is composed primarily of fatty acid monoglycerides in which the fatty acid groups contain predominately from 12 to 18 carbons.
Claim 5
Dependent Claim 33 words
The method of claim 1 in which said matrix material is composed primarily of propylene glycol monoesters of fatty acids in which the fatty acid groups contain predominately from 12 to 18 carbons.
Claim 6
Dependent Claim 21 words
The method of claim 1 in which said first solvent has a dielectric content in the range from 20 to 40.
Claim 7
Dependent Claim 21 words
The method of claim 1 in which said second solvent has a dielectric constant in the range from 1 to 3.
Claim 8
Dependent Claim 28 words
The method of claim 1 in which said second solvent is present in the volume ratio of from 2 to 4 parts per part of said prepared solution.
Claim 9
Dependent Claim 46 words
8 . The method of claim 1 in which said dispersion is at a temperature in the range of 0 to 50°F when the removal of said solvents is begun, and said droplets are maintained at a temperature below 50°F while said solvents are being removed.
Claim 10
Dependent Claim 50 words
The method of claim 1 in which said prepared solution is formed at a temperature of from 60 to 90°F, said second solvent is at a temperature below 50°F when said dispersion is prepared, and said droplets are maintained at a temperature below 50°F while said solvents are being removed.
Claim 11
Dependent Claim 49 words
The method of claim 1 in which the first step in removing said solvents is the separation of said droplets from most of said second solvent by mechanical separation, and in which the rest of said second solvent and said first solvent are removed by evaporation under reduced pressure.

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