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US4853226A Expired / Lapsed US ⏱️ 0.0 years remaining

Sustained-release particulate preparation and process for preparing the same

Assignee: Chugai Pharmaceutical Co Ltd
•
Filing: 1987-10-07
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Granted: 1989-08-01
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Expires: 2007-10-07
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Abstract

Abstract A sustained-release particulate preparation having a controlled releasing rate of a pharmacologically active agent contained therein in the living body, and a process for preparing the preparation are disclosed. The preparation comprises a polymeric compound which is capable of being degraded in the living body and which is compatible with living tissue, a pharmacologically active agent, and a natural high molecular weight compound of sugar origin or a derivative thereof. The preparation has fine and uniform particle size and can be administered subcutaneously or intramuscalarly for obtaining a long-lasting pharmacological activity.

Inventors

  • 👤 Minoru Machida
  • 👤 Masayuki Arakawa

Bibliographic Details

Application Number —
Jurisdiction US
Data Source google_patents
Last Synchronized 2026-10-30 23:01
CPC Classifications
A; A61; A61K; A61K9/00; A61K9/48; A61K9/14; A61K9/16; A61K9/1605; A61K9/1629; A61K9/1641; A61K9/1647; A61K9/1682; A61K9/1694

Claims Analysis

Total Claims: 7
Claim 1
Independent Claim 168 words
A sustained release particulate preparation consisting essentially of particles having a diameter not greater than 150 micrometers, prepared by a method which comprises the steps of: (a) combining an organic solution of a polymeric compound which is capable of being degraded in the living body and is compatible with living tissue, and an organic or organic/aqueous solution of a pharmacologically active agent, which pharmacologically active agent solution is capable of forming a solution, suspension or emulsion with said polymer solution and of forming a suspension in an aqueous solution; (b) combining the solution, suspension or emulsion of (a) with an aqueous solution of a natural high molecular weight compound selected from the group consisting of chitins and derivatives thereof, chitosans and derivatives thereof, hyaluronic acid and a salt thereof, soluble dextrans having a molecular weight of from about 10,000 to about 150,000 pectins, dextrins, having a molecular weight of from about 2,500 to about 150,000, and chondroitin sulfate and a salt thereof; and (c) recovering said particles therefrom.
Claim 2
Dependent Claim 168 words
A sustained release particulate preparation consisting essentially of particles having a diameter not greater than 150 micrometers, prepared by a method which comprises the steps of: (a) combining an organic solution of a polymeric compound which is capable of being degraded in the living body and is compatible with living tissue, and an organic or organic/aqueous solution of a pharmacologically active agent, which pharmacologically active agent solution is capable of forming a solution, suspension or emulsion with said polymer solution and of forming a suspension in an aqueous solution; (b) combining the solution, suspension or emulsion of (a) with an aqueous solution of a natural high molecular weight compound selected from the group consisting of chitins and derivatives thereof, chitosans and derivatives thereof, hyaluronic acid and a salt thereof, soluble dextrans having a molecular weight of from about 10,000 to about 150,000 pectins, dextrins, having a molecular weight of from about 2,500 to about 150,000, and chondroitin sulfate and a salt thereof; and (c) recovering said particles therefrom.
Claim 3
Dependent Claim 24 words
A sustained-release particulate preparation as claimed in claim 1, wherein said polymeric compound is polylactic acid, polyglycolic acid, polyhydroxybutyric acid or a copolymer thereof.
Claim 4
Dependent Claim 29 words
A sustained-release particulate preparation as claimed in claim 1, wherein the pharmacologically active agent-containing solution further comprises a surface active agent having a hydrophilic-lipophilic balance of 8 or less.
Claim 5
Dependent Claim 31 words
A sustained-release particulate preparation as claimed in claim 1, wherein said pharmacologically active agent is an organic compound, a protein or a peptide which is water-insoluble or difficulty soluble in water.
Claim 6
Independent Claim 168 words
A method of making a sustained release particulate-preparation consisting essentially of particles having a diameter not greater than 150 micrometers, which method comprises the steps of: (a) combining an organic solution of a polymeric compound which is capable of being degraded in the living body and is compatible with living tissue, and an organic or organic/aqueous solution of a pharmacologically active agent, which pharmacologically active agent solution is capable of forming a solution, suspension or emulsion with said polymer solution and of forming a suspension in an aqueous solution; (b) combining the solution, suspension or emulsion of (a) with an aqueous solution of a natural high molecular weight compound selected from the group consisting of chitins and derivatives thereof, chitosans and derivatives thereof, hyaluronic acid and a salt thereof, soluble dextrans having a molecular weight of from about 10,000 to about 150,000, pectins, dextrins, hyaving a molecular weight of from about 2,500 to about 150,000, and chondroitin sulfate and a salt thereof; and (c) recovering said particles therefrom.
Claim 7
Independent Claim 168 words
A method of making a sustained release particulate-preparation consisting essentially of particles having a diameter not greater than 150 micrometers, which method comprises the steps of: (a) combining an organic solution of a polymeric compound which is capable of being degraded in the living body and is compatible with living tissue, and an organic or organic/aqueous solution of a pharmacologically active agent, which pharmacologically active agent solution is capable of forming a solution, suspension or emulsion with said polymer solution and of forming a suspension in an aqueous solution; (b) combining the solution, suspension or emulsion of (a) with an aqueous solution of a natural high molecular weight compound selected from the group consisting of chitins and derivatives thereof, chitosans and derivatives thereof, hyaluronic acid and a salt thereof, soluble dextrans having a molecular weight of from about 10,000 to about 150,000, pectins, dextrins, hyaving a molecular weight of from about 2,500 to about 150,000, and chondroitin sulfate and a salt thereof; and (c) recovering said particles therefrom.

References Cited (Backward Citations)

US4451452A Cited
US4443497A Cited
JPS5933214A Cited
US4711782A Cited
US4745160A Cited
EP0169566B1 Cited
JPS6163613A Cited
JPS6165816A Cited
EP0215126A1 Cited
EP0220520A1 Cited

USPTO Annuity & Maintenance Windows

Annuity Stage Window Opens Payment Deadline Surcharge Period Until Estimated Fee Status
3.5 Years (Year 4) 1992-07-31 1993-01-30 1993-08-01 $2000.00 Window Closed / Lapsed
7.5 Years (Year 8) 1996-07-31 1997-01-30 1997-08-01 $3760.00 Window Closed / Lapsed
11.5 Years (Year 12) 2000-07-31 2001-01-30 2001-08-01 $7700.00 Window Closed / Lapsed

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