Patent EP0219922A2 successfully refreshed from Google Patents.
EP0219922A2
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EP
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Anthracycline antineoplastic agents encapsulated in phospholipid micellular particles
Assignee: Nexstar Pharmaceuticals Inc
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Filing: 1986-03-04
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Granted: —
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Expires: 2006-03-04
Abstract
Abstract Anthracycline anti-neoplastic agents are formulated in phospholipid micellular particles. In a preferred embodiment, the particles are in the form of vesicles which comprise an anthracycline agent, preferably daunorubicin, distearyl phosphatidyl choline, distearyl phosphatidyl glycerol and cholesterol, preferably in a molar ratio of about 1:2:0:0 to about 1:4:20:20. The vesicles are suspended in a low ionic solution such as 5% dextrose at pH 7.4.
Inventors
- 👤 Eric Forssen
Bibliographic Details
Application Number
—
Jurisdiction
EP
Data Source
google_patents
Last Synchronized
2026-10-25 23:31
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: 22
Claim 1
Independent Claim
30 words
A composition comprising an anthracycline neoplastic agent encapsulated in phospholipid micellular particles consisting of anionic and neutral phospholipids and cholesterol, said particles suspended in a low ionic strength aqueous phase.
Claim 2
Dependent Claim
30 words
A composition comprising an anthracycline neoplastic agent encapsulated in phospholipid micellular particles consisting of anionic and neutral phospholipids and cholesterol, said particles suspended in a low ionic strength aqueous phase.
Claim 3
Dependent Claim
17 words
A composition according to Claim 1 wherein the low ionic strength aqueous phase contains a hydroxyl-containing compound.
Claim 4
Dependent Claim
14 words
A composition according to Claim 2 wherein the hydroxyl containing compound is a sugar.
Claim 5
Dependent Claim
13 words
A composition according to Claim 3 wherein the hydroxyl containing compound is dextrose.
Claim 6
Dependent Claim
17 words
A composition according to Claim 1 wherein the aqueous phase is a sugar solution containing 5% dextrose.
Claim 7
Dependent Claim
30 words
A composition according to any one of the proceeding claims wherein the phospholipid is at least one selected from phosphatidyl glycerol, phosphatidyl choline, phosphatidly serine, phosphatidic acid and phosphatidyl inositol.
Claim 8
Dependent Claim
17 words
A composition according to Claim 6 wherein the phospholipids are distearyl phosphatidyl glycerol and distearyl phosphatidyl choline.
Claim 9
Dependent Claim
27 words
The composition according to Claim 7 comprising the anthracycline agent, distearyl phosphatidyl glycerol, distearyl phosphatidyl choline and cholesterol in a molar ratio ranging from 1:2:0:0 to 1:4:20:20.
Claim 10
Dependent Claim
25 words
A composition according to Claim 8 wherein the anthyracycline agent, distearyl phosphatidyl glycerol, distearyl phosphatidyl choline and cholesterol are in the molar ration of 1:4:5:6.
Claim 11
Dependent Claim
25 words
A composition according to Claim 8 wherein the anthracycline agent, distearyl phosphatidyl glycerol, distearyl phosphatidyl choline and cholesterol are in the molar ration of 1:1:5:4:0.
Claim 12
Dependent Claim
24 words
A composition according to Claim 9 wherein the pH of the suspending solution is in the range of from about pH 4.0 to 8.0.
Claim 13
Dependent Claim
11 words
A composition according to Claim 11 wherein the pH is 7.4.
Claim 14
Dependent Claim
28 words
A composition according to any one of the preceding claims wherein the micellular particles are in the form of unilamellar vesicles about 45 to 55 nanometers in diameter.
Claim 15
Dependent Claim
22 words
A composition according to any one of the preceding claims wherein the anthracycline agent is daunorubicin, doxorubicin, N-Trifluoroacetyl doxorubicin-14-valerate and Aclacinomycin A.
Claim 16
Dependent Claim
17 words
A composition of according to any one of the preceding claim wherein the anthracycline agent is daunorubicin.
Claim 17
Dependent Claim
22 words
A composition accounting to any one of the preceding claims for use in a method of therapy practised on the human body.
Claim 18
Dependent Claim
30 words
A composition according to Claim 16 wherein the method is for treating neoplastic tumors in a human body by parenterally administering multiple doses of the composition into a human subject.
Claim 19
Dependent Claim
17 words
A composition to Claim 17 wherein the method is one wherein the administration is by intraveneous injection.
Claim 20
Independent Claim
38 words
A method of preparing a composition comprising an anthracycline neoplastic agent by encapsulating the neoplastic agent is phospholipid micellular particles consisting of anionic and neutral phospholipids and cholesterol, said particles suspended in a low ionic strength aqueous phase.
Claim 21
Independent Claim
38 words
A method of preparing a composition comprising an anthracycline neoplastic agent by encapsulating the neoplastic agent is phospholipid micellular particles consisting of anionic and neutral phospholipids and cholesterol, said particles suspended in a low ionic strength aqueous phase.
Claim 22
Dependent Claim
24 words
A method according to Claim 19 wherein the agent in the micellular particles are as defined in any one of Claims 2 - 15.
References Cited (Backward Citations)
No citation records indexed.
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