US4769250A
Expired / Lapsed
US
⏱️ 0.0 years remaining
Antracycline antineoplastic agents encapsulated in phospholipid vesicle particles and methods for using same for tumor therapy
Assignee: Nexstar Pharmaceuticals Inc
•
Filing: 1987-10-26
•
Granted: 1988-09-06
•
Expires: 2007-10-26
Abstract
Abstract Formulations consisting of phospholipid bilayer membrane particles made from mixtures of anionic and neutral phospholipids encapsulating anthracycline anti-neoplastic agents, suspended in a low ionic strength aqueous phase, are described. In a preferred embodiment, the particles are in the form of vesicles which comprise daunorubicin, distearoyl phosphatidylglycerol and distearoyl phosphatidylcholine, the mol ratio of daunorubicin to distearoyl phosphatidylglycerol is at least about 1:1.25, and the suspending medium is an aqueous lactose solution containing a small amount of base.
Inventors
- 👤 Eric A. Forssen
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-10-23 13:32
CPC Classifications
A; A61; A61K; A61K9/00; A61K9/10; A61K31/00; A61K31/70; A61K9/127; A61K9/48; A61K9/50; A61P; A61P35/00; C; C07; C07H; C07H15/00; C07H15/20; C07H15/24; C07H15/252
Claims Analysis
Total Claims: 19
Claim 1
Independent Claim
45 words
A composition comprising an anthracycline anti-neoplastic agent encapsulated in phospholipid bilayer membrane particles consisting of anionic and neutral phospholipids, said particles being suspended in a low ionic strength aqueous phase, the mol ratio of anthracycline anti-neoplastic agent to anionic phospholipid being at least about 1:1.25.
Claim 2
Dependent Claim
45 words
A composition comprising an anthracycline anti-neoplastic agent encapsulated in phospholipid bilayer membrane particles consisting of anionic and neutral phospholipids, said particles being suspended in a low ionic strength aqueous phase, the mol ratio of anthracycline anti-neoplastic agent to anionic phospholipid being at least about 1:1.25.
Claim 3
Dependent Claim
20 words
A composition according to claim 1 wherein the low ionic strength aqueous phase contains a physiologically acceptable nonionic hydroxyl-containing compound.
Claim 4
Dependent Claim
13 words
A composition according to claim 2 wherein the hydroxyl-containing compound is a sugar.
Claim 5
Dependent Claim
12 words
A composition according to claim 3 wherein the sugar is a monosaccharide.
Claim 6
Dependent Claim
11 words
A composition according to claim 4 wherein the monosaccharide is dextrose.
Claim 7
Dependent Claim
12 words
A composition according to claim 3 wherein the sugar is a disaccharide.
Claim 8
Dependent Claim
11 words
A composition according to claim 6 wherein the disaccharide is lactose.
Claim 9
Dependent Claim
23 words
A composition according to claim 7 wherein the lactose is present as a 9-11% solution and the pH is about 6.0 to 8.0.
Claim 10
Dependent Claim
28 words
A composition according to claim 1 wherein the anionic phospholipid is a phosphatidylglycerol, phosphatidylserine, phosphatidylinositol or phosphatidic acid and the neutral phospholipid is a phosphatidyl choline or phosphatidylethanolamine.
Claim 11
Dependent Claim
11 words
A composition according to claim 9 wherein cholesterol is also present.
Claim 12
Dependent Claim
20 words
A composition according to claim 9 wherein the anionic phospholipid is distearoyl phosphatidylglycerol and the neutral phospholipid is distearoyl phosphatidylcholine.
Claim 13
Dependent Claim
24 words
A composition according to claim 11 wherein the anthracycline anti-neoplastic agent, distearoyl phosphatidylglycerol and distearoyl phosphatidyl choline are in the molar ratio of 1:1.5:7
Claim 14
Dependent Claim
25 words
A composition according to claim 10 wherein the anthracycline anti-neoplastic agent, distearoyl phosphatidylglycerol, distearoyl phosphatidyl choline and cholesterol ar in the molar ratio of 1:1.5:7:2.
Claim 15
Dependent Claim
24 words
A composition according to claim 10 wherein the anthracycline anti-neoplastic agent, distearoyl phosphatidylglycerol, distearoyl phosphatidylcholine and cholesterol are in the molar ratio of 1:4:5:6.
Claim 16
Dependent Claim
27 words
A composition according to any one of claims 1-14, inclusive, wherein the antracycline anti-neoplastic agent is selected from the group consisting of daunorubicin, doxorubicin and Aclacinomycin A.
Claim 17
Dependent Claim
13 words
A composition according to claim 15 wherein the anthracycline anti-neoplastic agent is daunorubicin.
Claim 18
Dependent Claim
27 words
A method for treating neoplastic tumors in a human body affected therewith comprising parenterally administering to said human body multiple doses of a composition of claim 15.
Claim 19
Dependent Claim
12 words
A method according to claim 17 wherein administration is by intraveneous injection.
References Cited (Backward Citations)
US4427649A
Cited
GB2002319A
Cited
US4356167A
Cited
US4411894A
Cited
US4310505A
Cited
US4331654A
Cited
US4427664A
Cited
US4474945A
Cited
US4619794A
Cited
US4438105A
Cited
WO1985000968A1
Cited
GB2146525A
Cited
USPTO Annuity & Maintenance Windows
| Annuity Stage | Window Opens | Payment Deadline | Surcharge Period Until | Estimated Fee | Status |
|---|---|---|---|---|---|
| 3.5 Years (Year 4) | 1991-09-06 | 1992-03-07 | 1992-09-06 | $2000.00 | Window Closed / Lapsed |
| 7.5 Years (Year 8) | 1995-09-06 | 1996-03-07 | 1996-09-06 | $3760.00 | Window Closed / Lapsed |
| 11.5 Years (Year 12) | 1999-09-06 | 2000-03-07 | 2000-09-06 | $7700.00 | Window Closed / Lapsed |