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US4766046A Expired / Lapsed US ⏱️ 0.0 years remaining

Stabilized liposome/amphotericin composition and method

Assignee: Liposome Technology Inc
•
Filing: 1985-09-27
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Granted: 1988-08-23
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Expires: 2005-09-27
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Abstract

Abstract A dehydrated liposome/amphotericin B composition which, upon addition of an aqueous medium, forms a suspension of liposomes (a) having a predetermined size distribution in size range less than about 1 micron, and (b) containing at least about 1 mole percent amphotericin B. The composition is prepared by forming a suspension of heterogeneous size amphotericin B liposomes in an aqueous solution containing at least about 0.5% of a membrane-stabilizing agent. The suspension is sized--for example, by extrusion through a small-pore polycarbonate membrane--to produce liposomes having the selected size distribution, and dehydrated.

Inventors

  • 👤 Robert Abra
  • 👤 Francis C. Szoka

Bibliographic Details

Application Number —
Jurisdiction US
Data Source google_patents
Last Synchronized 2026-10-27 20:50
CPC Classifications
A; A61; A61K; A61K9/00; A61K9/10; A61K9/127; A61K9/1277; A61K31/00; A61K31/70; A61K31/7042; A61K31/7048; Y; Y10; Y10S; Y10S436/00; Y10S436/829

Claims Analysis

Total Claims: 5
Claim 1
Independent Claim 149 words
A method of administering liposomes containing between about 3 to 7 mole percent amphotericin B and having, after a storage period, a selected liposome size distribution in a size range between about 0.2 to 0.5 micron, comprising preparing a suspension of heterogeneously sized liposomes containing between about 3 to 7 mole percent amphotericin B in the lipid phase, and, in the aqueous phase, at least about 0.5% w/v of a membrane-stabilizing agent, reducing the size heterogeneity of the liposome suspension to achieve said selected liposome size distribution, lyophilizing the liposome suspension before the size distribution of the liposomes changes substantially, after such storage period, adding an aqueous medium to the lyophilized suspension, said adding being effective to produce a reconstituted suspension of liposomes in which the size distribution achieved by said reducing is substantially preserved, and administering the reconstituted liposomes before the size distribution of the liposomes changes substantially.
Claim 2
Independent Claim 149 words
A method of administering liposomes containing between about 3 to 7 mole percent amphotericin B and having, after a storage period, a selected liposome size distribution in a size range between about 0.2 to 0.5 micron, comprising preparing a suspension of heterogeneously sized liposomes containing between about 3 to 7 mole percent amphotericin B in the lipid phase, and, in the aqueous phase, at least about 0.5% w/v of a membrane-stabilizing agent, reducing the size heterogeneity of the liposome suspension to achieve said selected liposome size distribution, lyophilizing the liposome suspension before the size distribution of the liposomes changes substantially, after such storage period, adding an aqueous medium to the lyophilized suspension, said adding being effective to produce a reconstituted suspension of liposomes in which the size distribution achieved by said reducing is substantially preserved, and administering the reconstituted liposomes before the size distribution of the liposomes changes substantially.
Claim 3
Dependent Claim 27 words
The method of claim 1, wherein the liposomes have a lipid composition which includes about 50-80 mole percent unsaturated phospholipids, and between about 20-50 mole percent cholesterol.
Claim 4
Dependent Claim 59 words
The method of claim 1, wherein the membrane-stabilizing agent includes at least about 0.5% w/v of an agent selected from the group consisting of glucose, mannitol, trehalose, sucrose, and lactose, when the amphotericin B concentration is less than about 4 mole percent, and about 0.5% w/v maltodextrin, when the amphotericin B concentration is greater than about 6 mole percent.
Claim 5
Dependent Claim 26 words
The method of claim 3, wherein the liposomes contain between about 6-7 mole percent amphoteracin B, and the membrane stabilizing agent includes about 0.5% w/v maltodextrin.

References Cited (Backward Citations)

GB2013609A Cited
US4529561A Cited
US4411894A Cited

USPTO Annuity & Maintenance Windows

Annuity Stage Window Opens Payment Deadline Surcharge Period Until Estimated Fee Status
3.5 Years (Year 4) 1991-08-23 1992-02-22 1992-08-23 $2000.00 Window Closed / Lapsed
7.5 Years (Year 8) 1995-08-23 1996-02-22 1996-08-23 $3760.00 Window Closed / Lapsed
11.5 Years (Year 12) 1999-08-23 2000-02-22 2000-08-23 $7700.00 Window Closed / Lapsed

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