US5415869A
Expired / Lapsed
US
⏱️ 0.0 years remaining
Taxol formulation
Assignee: Research Foundation of the State University of New York
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Filing: 1993-11-12
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Granted: 1995-05-16
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Expires: 2013-11-12
Abstract
Abstract The present invention relates to a pharmaceutical composition for use in treatment of cancer patients. The composition includes at least one taxane present in a pharmaceutical effective amount and a mixture of one or more negatively charged phospholipids and one or more zwitterion (i.e. uncharged) phospholipids. This mixture entraps the at least one taxane in what is believed to be a liposome. The mixture contains a ratio of negatively charged phospholipids to zwitterion phospholipids of 1:9 to 7:3. The taxol is present in an amount of 1.5-8.0 mole percent taxane. The composition is in the form of particles having a size of 0.025 to 10 microns with substantially no taxane crystals.
Inventors
- 👤 Robert M. Straubinger
- 👤 Amarnath Sharma
- 👤 Eric Mayhew
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-10-26 22:24
CPC Classifications
A; A61; A61K; A61K31/00; A61K31/70; A61K31/33; A61K31/335; A61K9/00; A61K9/10; A61K9/127; A61P; A61P35/00
Claims Analysis
Total Claims: 27
Claim 1
Independent Claim
88 words
A pharmaceutical composition for use in treatment of cancer comprising: at least one taxane present in said composition in a pharmaceutically effective amount of 1.5-8.0 mol % and a mixture of one or more negatively charged phospholipids and one or more zwitterion phospholipids in a respective ratio of 1:9 to 3:7, wherein said mixture entraps said at least one taxane and said composition is in the form of particles having a size of 0.025 to 10 microns with a substantial absence of taxane crystal formation in said composition.
Claim 2
Dependent Claim
88 words
A pharmaceutical composition for use in treatment of cancer comprising: at least one taxane present in said composition in a pharmaceutically effective amount of 1.5-8.0 mol % and a mixture of one or more negatively charged phospholipids and one or more zwitterion phospholipids in a respective ratio of 1:9 to 3:7, wherein said mixture entraps said at least one taxane and said composition is in the form of particles having a size of 0.025 to 10 microns with a substantial absence of taxane crystal formation in said composition.
Claim 3
Dependent Claim
59 words
A pharmaceutical composition according claim 1, wherein the negatively charged phospholipid is selected from the group consisting of phosphatidyl inositol, phosphatidyl serine, phosphatidyl glycerol, phosphaphatic acid, diphosphatidyl glycerol, poly(ethylene glycol)-phosphatidyl ethanolamine, dimyristoylphosphatidyl glycerol, dioleoylphosphatidyl glycerol, dilauryloylphosphatidyl glycerol, dipalmitotylphosphatidyl glycerol, distearyloylphosphatidyl glycerol, dimyristoyl phosphatic acid, dipalmitoyl phosphatic acid, dimyristoyl phosphitadyl serine, dipalmitoyl phosphatidyl serine, brain phosphatidyl serine, and mixtures thereof.
Claim 4
Dependent Claim
66 words
A pharmaceutical composition according to claim 1, wherein the zwitterion phospholipid is selected from the group consisting of phosphatidyl choline, phosphatidyl ethanolamine, sphingomyelin, lecithin, lysolecithin, lysophatidylethanolamine, cerebrosides, dimyristoylphosphatidyl choline, dipalmitotylphosphatidyl choline, distearyloylphosphatidyl choline, dielaidoylphosphatidyl choline, dioleoylphosphatidyl choline, dilauryloylphosphatidyl choline, 1-myristoyl-2-palmitoyl phosphatidyl choline, 1-palmitoyl-2-myristoyl phosphatidyl choline, 1-palmitoyl-2-stearoyl phosphatidyl choline, 1-stearoyl-2-palmitoyl phosphatidyl choline, dimyristoyl phosphatidyl ethanolamine, dipalmitoyl phosphatidyl ethanolamine, brain sphingomyelin, dipalmitoyl sphingomyelin, distearoyl sphingomyelin, and mixtures thereof.
Claim 5
Dependent Claim
22 words
A pharmaceutical composition according to claim 1, wherein the negatively charged phospholipid is phosphatidyl glycerol and the zwitterion phospholipid is phosphatidyl choline.
Claim 6
Dependent Claim
17 words
A pharmaceutical composition according to claim 1, wherein said composition contains 1.5-3.3 mol % of said taxane.
Claim 7
Dependent Claim
31 words
A pharmaceutical composition according to claim 1, wherein said taxane is selected from the group consisting of taxol, 7-epitaxol, 7-acetyl taxol, 10-desacetyltaxol, 10-desacetyl-7-epitaxol, 7-xylosyltaxol, 10-desacetyl-7-glutaryltaxol, 7-N,N-dimethylglycyltaxol, 7-L-alanyltaxol, taxotere, and mixtures thereof.
Claim 8
Dependent Claim
11 words
A pharmaceutical composition according to claim 1 further comprising: a sterol.
Claim 9
Dependent Claim
30 words
A pharmaceutical composition according to claim 7, wherein said sterol is selected from the group consisting of cholesterol, cholesterol derivatives, vitamin D, phytosterols, steroid hormones, cholesteryl esters, and mixtures thereof.
Claim 10
Dependent Claim
19 words
A pharmaceutical composition according to claim 7, wherein said composition contains 0.01 to 50 mol % of said sterol.
Claim 11
Dependent Claim
15 words
A pharmaceutical composition according to claim 1, wherein said composition is in dry, lyophilized form.
Claim 12
Dependent Claim
14 words
A pharmaceutical composition according to claim 1, wherein said composition is a liquid suspension.
Claim 13
Dependent Claim
23 words
A method of treating cancer patients comprising: administering to a cancer patient said pharmaceutical composition according to claim 1 in an effective amount.
Claim 14
Dependent Claim
91 words
A pharmaceutical composition for use in treatment of cancer comprising: at least one taxane present in said composition in a pharmaceutically effective amount of 1.5-8.0 mol % and a mixture of one or more negatively charged phospholipids and one or more zwitterion phospholipids in a respective ratio of 1:9 to 3:7, wherein said mixture forms liposomes which entrap said at least one taxane and said composition is in the form of particles having a size of 0.025 to 10 microns with a substantial absence of taxane crystal formation in said composition.
Claim 15
Dependent Claim
91 words
A pharmaceutical composition for use in treatment of cancer comprising: at least one taxane present in said composition in a pharmaceutically effective amount of 1.5-8.0 mol % and a mixture of one or more negatively charged phospholipids and one or more zwitterion phospholipids in a respective ratio of 1:9 to 3:7, wherein said mixture forms liposomes which entrap said at least one taxane and said composition is in the form of particles having a size of 0.025 to 10 microns with a substantial absence of taxane crystal formation in said composition.
Claim 16
Dependent Claim
59 words
A pharmaceutical composition according claim 13, wherein the negatively charged phospholipid is selected from the group consisting of phosphatidyl inositol, phosphatidyl serine, phosphatidyl glycerol, phosphaphatic acid, diphosphatidyl glycerol, poly(ethylene glycol)-phosphatidyl ethanolamine, dimyristoylphosphatidyl glycerol, dioleoylphosphatidyl glycerol, dilauryloylphosphatidyl glycerol, dipalmitotylphosphatidyl glycerol, distearyloylphosphatidyl glycerol, dimyristoyl phosphatic acid, dipalmitoyl phosphatic acid, dimyristoyl phosphitadyl serine, dipalmitoyl phosphatidyl serine, brain phosphatidyl serine, and mixtures thereof.
Claim 17
Dependent Claim
66 words
A pharmaceutical composition according to claim 13, wherein the zwitterion phospholipid is selected from the group consisting of phosphatidyl choline, phosphatidyl ethanolamine, sphingomyelin, lecithin, lysolecithin, lysophatidylethanolamine, cerebrosides, dimyristoylphosphatidyl choline, dipalmitotylphosphatidyl choline, distearyloylphosphatidyl choline, dielaidoylphosphatidyl choline, dioleoylphosphatidyl choline, dilauryloylphosphatidyl choline, 1-myristoyl-2-palmitoyl phosphatidyl choline, 1-palmitoyl-2-myristoyl phosphatidyl choline, 1-palmitoyl-2-stearoyl phosphatidyl choline, 1-stearoyl-2-palmitoyl phosphatidyl choline, dimyristoyl phosphatidyl ethanolamine, dipalmitoyl phosphatidyl ethanolamine, brain sphingomyelin, dipalmitoyl sphingomyelin, distearoyl sphingomyelin, and mixtures thereof.
Claim 18
Dependent Claim
32 words
A pharmaceutical composition according to claim 13, wherein said taxane is selected from the group consisting of taxol, 7-epitaxol, 7-acetyl taxol, 10-desacetyltaxol, 10-desacetyl-7-epitaxol, 7-xylosyltaxol, 10-desacetyl-7-sylosyltaxol, 7-glutaryltaxol, 7-N,N-dimethylglycycltaxol, 7-L-alanyltaxol, taxotere, and mixtures thereof.
Claim 19
Dependent Claim
24 words
A pharmaceutical composition according to claim 13, wherein said composition is in the form of particles having a size of 1 to 5 microns.
Claim 20
Dependent Claim
23 words
A method of treating cancer patients comprising: administering to a cancer patient said pharmaceutical composition according to claim 13 in an effective amount.
Claim 21
Dependent Claim
85 words
A pharmaceutical composition in particulate form for use in treatment of cancer comprising: at least one taxane present in said composition in a pharmaceutically effective amount of 1.5-8.0 mol % and a mixture of one or more negatively charged phospholipids and one or more zwitterion phospholipids in a respective molar ratio of 1:9 to 3:7, wherein said mixture entraps said at least one taxane within particles having a size of 1 to 5 microns with a substantial absence of taxane crystal formation in said composition.
Claim 22
Dependent Claim
85 words
A pharmaceutical composition in particulate form for use in treatment of cancer comprising: at least one taxane present in said composition in a pharmaceutically effective amount of 1.5-8.0 mol % and a mixture of one or more negatively charged phospholipids and one or more zwitterion phospholipids in a respective molar ratio of 1:9 to 3:7, wherein said mixture entraps said at least one taxane within particles having a size of 1 to 5 microns with a substantial absence of taxane crystal formation in said composition.
Claim 23
Dependent Claim
59 words
A pharmaceutical composition according claim 19, wherein the negatively charged phospholipid is selected from the group consisting of phosphatidyl inositol, phosphatidyl serine, phosphatidyl glycerol, phosphaphatic acid, diphosphatidyl glycerol, poly(ethylene glycol)-phosphatidyl ethanolamine, dimyristoylphosphatidyl glycerol, dioleoylphosphatidyl glycerol, dilauryloylphosphatidyl glycerol, dipalmitotylphosphatidyl glycerol, distearyloylphosphatidyl glycerol, dimyristoyl phosphatic acid, dipalmitoyl phosphatic acid, dimyristoyl phosphitadyl serine, dipalmitoyl phosphatidyl serine, brain phosphatidyl serine, and mixtures thereof.
Claim 24
Dependent Claim
66 words
A pharmaceutical composition according to claim 19, wherein the zwitterion phospholipid is selected from the group consisting of phosphatidyl choline, phosphatidyl ethanolamine, sphingomyelin, lecithin, lysolecithin, lysophatidylethanolamine, cerebrosides, dimyristoylphosphatidyl choline, dipalmitotylphosphatidyl choline, distearyloylphosphatidyl choline, dielaidoylphosphatidyl choline, dioleoylphosphatidyl choline, dilauryloylphosphatidyl choline, 1-myristoyl-2-palmitoyl phosphatidyl choline, 1-palmitoyl-2-myristoyl phosphatidyl choline, 1-palmitoyl-2-stearoyl phosphatidyl choline, 1-stearoyl-2-palmitoyl phosphatidyl choline, dimyristoyl phosphatidyl ethanolamine, dipalmitoyl phosphatidyl ethanolamine, brain sphingomyelin, dipalmitoyl sphingomyelin, distearoyl sphingomyelin, and mixtures thereof.
Claim 25
Dependent Claim
32 words
A pharmaceutical composition according to claim 19, wherein said taxane is selected from the group consisting of taxol, 7-epitaxol, 7-acetyl taxol, 10-desacetyltaxol, 10-desacetyl-7-epitaxol, 7-xylosyltaxol, 10-desacetyl-7-sylosyltaxol, 7-glutaryltaxol, 7-N,N-dimethylglycytaxol, 7-L-alanyltaxol, taxotere, and mixtures thereof.
Claim 26
Dependent Claim
11 words
A pharmaceutical composition according to claim 19 further comprising: a sterol.
Claim 27
Dependent Claim
23 words
A method of treating cancer patients comprising: administering to a cancer patient said pharmaceutical composition according to claim 19 in an effective amount.
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USPTO Annuity & Maintenance Windows
| Annuity Stage | Window Opens | Payment Deadline | Surcharge Period Until | Estimated Fee | Status |
|---|---|---|---|---|---|
| 3.5 Years (Year 4) | 1998-05-15 | 1998-11-14 | 1999-05-16 | $2000.00 | Window Closed / Lapsed |
| 7.5 Years (Year 8) | 2002-05-15 | 2002-11-14 | 2003-05-16 | $3760.00 | Window Closed / Lapsed |
| 11.5 Years (Year 12) | 2006-05-15 | 2006-11-14 | 2007-05-16 | $7700.00 | Window Closed / Lapsed |