Patent US5733888A successfully refreshed from Google Patents.
US5733888A
Expired / Lapsed
US
⏱️ 0.0 years remaining
Injectable composition
Assignee: Mayne Pharma USA Inc
•
Filing: 1996-01-31
•
Granted: 1998-03-31
•
Expires: 2016-01-31
Abstract
Abstract A pharmaceutical formulation of taxol and polyethoxylated castor oil is disclosed to be relatively acidified to a pH of less than 8.1 and preferably within a pH range of 5 to 7, inclusively, by an acidifying agent. Ethanol is optionally included in the formulation which is adapted for use in a body for the treatment of cancer. A formulation method is disclosed and includes the step of mixing an acid with a carrier material, such as polyethoxylated castor oil, to form a carrier solution after which taxol is added in an amount such that the resulting pH is less than 8.1 and preferably in a pH range of 5 to 7. Ethanol may optionally be slurried with the taxol before mixing with the carrier solution. A variety of acidifying agents, a preferred one being anhydrous citric acid, are described.
Inventors
- 👤 David Carver
- 👤 Timothy Prout
- 👤 Hernita Ewald
- 👤 Robyn Elliott
- 👤 Paul Handreck
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-11-08 14:28
CPC Classifications
A; A61; A61K; A61K9/00; A61K9/0012; A61K9/0019; A61K31/00; A61K31/33; A61K31/335; A61K31/337; A61K47/00; A61K47/06; A61K47/08; A61K47/10; A61K47/12; A61K47/14; A61K47/44
Claims Analysis
Total Claims: 51
Claim 1
Independent Claim
44 words
In a pharmaceutical formulation adapted for use in treating cancer comprising taxol and polyethoxylated castor oil, the improvement comprising an acidifying agent added to said pharmaceutical formulation in a proportion such that said composition has a resulting pH less than or equal to 7.0.
Claim 2
Dependent Claim
44 words
In a pharmaceutical formulation adapted for use in treating cancer comprising taxol and polyethoxylated castor oil, the improvement comprising an acidifying agent added to said pharmaceutical formulation in a proportion such that said composition has a resulting pH less than or equal to 7.0.
Claim 3
Independent Claim
57 words
A method of formulating a taxol solution for injection in which the taxol does not readily degrade, comprising the following steps: mixing acid with a carrier material to form a first carrier solution; and mixing taxol with the first carrier solution to form a taxol solution whereby the taxol in the taxol solution does not readily degrade.
Claim 4
Independent Claim
57 words
A method of formulating a taxol solution for injection in which the taxol does not readily degrade, comprising the following steps: mixing acid with a carrier material to form a first carrier solution; and mixing taxol with the first carrier solution to form a taxol solution whereby the taxol in the taxol solution does not readily degrade.
Claim 5
Dependent Claim
12 words
A method according to claim 2 wherein said acid is acetic acid.
Claim 6
Dependent Claim
12 words
A method according to claim 2 wherein said acid is citric acid.
Claim 7
Dependent Claim
14 words
A method according to claim 2 wherein said carrier material is polyethoxylated castor oil.
Claim 8
Dependent Claim
24 words
A method according to claim 2 including the step of slurrying said taxol in alcohol before mixing said taxol with the first carrier solution.
Claim 9
Dependent Claim
45 words
A pharmaceutical taxol composition comprising: taxol; polyethoxylated castor oil; and anhydrous citric acid in sufficient amounts to improve the stability of the taxol such that at least 95% of the taxol potency is retained when the composition is stored at 40° C. for 7 days.
Claim 10
Dependent Claim
45 words
A pharmaceutical taxol composition comprising: taxol; polyethoxylated castor oil; and anhydrous citric acid in sufficient amounts to improve the stability of the taxol such that at least 95% of the taxol potency is retained when the composition is stored at 40° C. for 7 days.
Claim 11
Dependent Claim
19 words
A pharmaceutical formulation according to claim 1 wherein said composition has a pH of between 5 and 7, inclusively.
Claim 12
Dependent Claim
13 words
A pharmaceutical formulation according to claim 1 including ethanol as a constituent thereof.
Claim 13
Dependent Claim
19 words
A pharmaceutical formulation according to claim 9 wherein said composition has a pH of between 5 and 7, inclusively.
Claim 14
Dependent Claim
19 words
A method according to claim 2 wherein said taxol solution has a pH of between 5 and 7, inclusively.
Claim 15
Independent Claim
43 words
A method for improving the stability of a pharmaceutical taxol solution over an extended period, comprising the steps of: providing a formulation comprising taxol, a pharmaceutically-acceptable carrier, and an acidifying agent; and storing said formulation in a container for at least 7 days.
Claim 16
Independent Claim
43 words
A method for improving the stability of a pharmaceutical taxol solution over an extended period, comprising the steps of: providing a formulation comprising taxol, a pharmaceutically-acceptable carrier, and an acidifying agent; and storing said formulation in a container for at least 7 days.
Claim 17
Dependent Claim
12 words
The method of claim 12, wherein said carrier is polyethoxylated castor oil.
Claim 18
Dependent Claim
10 words
The method of claim 13, wherein said formulation is anhydrous.
Claim 19
Dependent Claim
13 words
The method of claim 12, wherein said acidifying agent is a mineral acid.
Claim 20
Dependent Claim
13 words
The method of claim 12, wherein said acidifying agent is an organic acid.
Claim 21
Dependent Claim
12 words
The method of claim 12, wherein said acidifying agent is citric acid.
Claim 22
Dependent Claim
12 words
The method of claim 12, wherein said acidifying agent is acetic acid.
Claim 23
Dependent Claim
11 words
The method of claim 17, wherein said citric acid is anhydrous.
Claim 24
Dependent Claim
11 words
The method of claim 4, wherein said citric acid is anhydrous.
Claim 25
Dependent Claim
19 words
The method of claim 2, wherein said taxol solution has an apparent pH of between 5 and 7, inclusively.
Claim 26
Dependent Claim
35 words
In an anhydrous pharmaceutical formulation comprising taxol and polyethoxylated castor oil, the improvement comprising an acidifying agent mixed in a proportion such that said pharmaceutical formulation has a resulting pH of about 7 or less.
Claim 27
Dependent Claim
35 words
In an anhydrous pharmaceutical formulation comprising taxol and polyethoxylated castor oil, the improvement comprising an acidifying agent mixed in a proportion such that said pharmaceutical formulation has a resulting pH of about 7 or less.
Claim 28
Dependent Claim
17 words
The improved pharmaceutical formulation of claim 22, wherein the apparent pH from about 7 to about 5.
Claim 29
Dependent Claim
15 words
The improved pharmaceutical formulation of claim 22, wherein said acidifying agent is a mineral acid.
Claim 30
Dependent Claim
15 words
The improved pharmaceutical formulation of claim 22, wherein said acidifying agent is an organic acid.
Claim 31
Dependent Claim
14 words
The improved pharmaceutical formulation of claim 22, wherein said acidifying agent is acetic acid.
Claim 32
Dependent Claim
14 words
The improved pharmaceutical formulation of claim 22, wherein said acidifying agent is citric acid.
Claim 33
Dependent Claim
13 words
The improved pharmaceutical formulation of claim 27, wherein said citric acid is anhydrous.
Claim 34
Dependent Claim
42 words
An article of manufacture comprising a container and a pharmaceutical formulation contained therein, said pharmaceutical formulation comprising a pharmaceutically-acceptable carrier, taxol, and an acidifying agent mixed in proportion such that said pharmaceutical formulation has a resulting pH of about 7 or less.
Claim 35
Dependent Claim
42 words
An article of manufacture comprising a container and a pharmaceutical formulation contained therein, said pharmaceutical formulation comprising a pharmaceutically-acceptable carrier, taxol, and an acidifying agent mixed in proportion such that said pharmaceutical formulation has a resulting pH of about 7 or less.
Claim 36
Dependent Claim
18 words
The article of manufacture of claim 29 further comprising instructions for administering said pharmaceutical formulation to a patient.
Claim 37
Dependent Claim
15 words
The article of manufacture of claim 30, wherein said acidifying agent is a mineral acid.
Claim 38
Dependent Claim
15 words
The article of manufacture of claim 30, wherein said acidifying agent is an organic acid.
Claim 39
Dependent Claim
14 words
The article of manufacture of claim 30, wherein said acidifying agent is acetic acid.
Claim 40
Dependent Claim
14 words
The article of manufacture of claim 30, wherein said acidifying agent is citric acid.
Claim 41
Dependent Claim
13 words
The article of manufacture of claim 34, wherein said citric acid is anhydrous.
Claim 42
Dependent Claim
15 words
The article of manufacture of claim 30, wherein said pharmaceutically-acceptable carrier is polyethoxylated castor oil.
Claim 43
Dependent Claim
15 words
The improved pharmaceutical formulation of claim 1, wherein said acidifying agent is a mineral acid.
Claim 44
Dependent Claim
15 words
The improved pharmaceutical formulation of claim 1, wherein said acidifying agent is an organic acid.
Claim 45
Dependent Claim
14 words
The improved pharmaceutical formulation of claim 1, wherein said acidifying agent is acetic acid.
Claim 46
Dependent Claim
14 words
The improved pharmaceutical formulation of claim 1, wherein said acidifying agent is citric acid.
Claim 47
Dependent Claim
13 words
The improved pharmaceutic formulation of claim 40, wherein said citric acid is anhydrous.
Claim 48
Dependent Claim
12 words
The method of claim 2, wherein said acid is a mineral acid.
Claim 49
Dependent Claim
12 words
The method of claim 2, wherein said acid is an organic acid.
Claim 50
Dependent Claim
44 words
A pharmaceutical taxol composition comprising: taxol; polyethoxylated castor oil; and acetic acid in sufficient amounts to improve the stability of the taxol such that at least 95% of the taxol potency is retained when the composition is stored at 40° C. for 7 days.
Claim 51
Dependent Claim
44 words
A pharmaceutical taxol composition comprising: taxol; polyethoxylated castor oil; and acetic acid in sufficient amounts to improve the stability of the taxol such that at least 95% of the taxol potency is retained when the composition is stored at 40° C. for 7 days.
References Cited (Backward Citations)
US4814470A
Cited
US4942184A
Cited
US5157049A
Cited
US4960790A
Cited
US5254580A
Cited
US5504102A
Cited
USPTO Annuity & Maintenance Windows
| Annuity Stage | Window Opens | Payment Deadline | Surcharge Period Until | Estimated Fee | Status |
|---|---|---|---|---|---|
| 3.5 Years (Year 4) | 2001-03-30 | 2001-09-29 | 2002-03-31 | $2000.00 | Window Closed / Lapsed |
| 7.5 Years (Year 8) | 2005-03-30 | 2005-09-29 | 2006-03-31 | $3760.00 | Window Closed / Lapsed |
| 11.5 Years (Year 12) | 2009-03-30 | 2009-09-29 | 2010-03-31 | $7700.00 | Window Closed / Lapsed |