US5504102A
Expired / Lapsed
US
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Stabilized pharmaceutical composition and stabilizing solvent
Assignee: Bristol Myers Squibb Co
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Filing: 1995-01-18
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Granted: 1996-04-02
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Expires: 2015-01-18
Abstract
Abstract A stabilized pharmaceutical composition containing paclitaxel, teniposide, camptothecin or other antineoplastic agent susceptible to degradation during storage is produced using a solvent system containing a low carboxylate anion content. The solvent system is a mixture of ethanol and a polyoxyethylated castor oil. The polyoxyethylated castor oil is treated with an acid or contacted with alumina to reduce the carboxylate anion content of the solvent. The low carboxylate anion content of the solvent provides extended shelf life and lower amounts of degradation by-products.
Inventors
- 👤 Shreeram N. Agharkar
- 👤 Uday S. Gogate
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-11-08 14:10
CPC Classifications
A; A61; A61K; A61K31/00; A61K31/33; A61K31/335; A61K31/337; A61K31/70; A61K31/395; A61K31/435; A61K31/47; A61K47/00; A61K47/02; A61K47/44; A61K9/00; A61K9/0012; A61K9/0019; A61P; A61P35/00
Claims Analysis
Total Claims: 24
Claim 1
Independent Claim
62 words
A stabilized composition comprising an antineoplastic compound selected from the group consisting of teniposide, paclitaxel, camptothecin and derivatives thereof; and a solvent capable of dispersing or solubilizing said antineoplastic compound comprising polyoxyethylated castor oil and sufficient acid to provide said solvent with a carboxylate anion content less than or equal to 0.6×10 -6 g equivalents of carboxylate anion per ml of solvent.
Claim 2
Dependent Claim
62 words
A stabilized composition comprising an antineoplastic compound selected from the group consisting of teniposide, paclitaxel, camptothecin and derivatives thereof; and a solvent capable of dispersing or solubilizing said antineoplastic compound comprising polyoxyethylated castor oil and sufficient acid to provide said solvent with a carboxylate anion content less than or equal to 0.6×10 -6 g equivalents of carboxylate anion per ml of solvent.
Claim 3
Dependent Claim
12 words
The composition of claim 1 wherein said solvent further comprises an alcohol.
Claim 4
Dependent Claim
20 words
The composition of claim 1 wherein said solvent is a mixture of ethyl alcohol, acid and said polyoxyethylated castor oil.
Claim 5
Dependent Claim
28 words
The composition of claim 1 wherein said polyoxyethylated castor oil is a condensation product of castor oil and 20-40 moles of ethylene oxide per mole of castor oil.
Claim 6
Dependent Claim
12 words
The composition of claim 1 wherein said acid is a mineral acid.
Claim 7
Dependent Claim
29 words
The composition of claim 1 wherein said acid is selected from the group consisting of HCl, HBr, HI, HF, H 2 SO 4 , HNO 3 and acetic acid.
Claim 8
Dependent Claim
31 words
The composition of claim 1 wherein said solvent contains a mineral acid in an amount to provide about 5.6×10 -6 to 8.4×10 -6 g of H + per ml of solvent.
Claim 9
Dependent Claim
11 words
The composition of claim 1 wherein said antineoplastic compound is teniposide.
Claim 10
Dependent Claim
11 words
The composition of claim 1 wherein said antineoplastic compound is camptothecin.
Claim 11
Independent Claim
64 words
A method of preparing a stabilized composition comprising preparing a solvent comprising a polyoxyethylated castor oil and sufficient acid to provide said solvent with a carboxylate anion content less than or equal to 0.6×10 -6 g equivalents of carboxylate anion per ml of solvents, and dispersing an antineoplastic compound selected from the group consisting of teniposide, paclitaxel, camptothecin and derivatives thereof in said solvent.
Claim 12
Independent Claim
64 words
A method of preparing a stabilized composition comprising preparing a solvent comprising a polyoxyethylated castor oil and sufficient acid to provide said solvent with a carboxylate anion content less than or equal to 0.6×10 -6 g equivalents of carboxylate anion per ml of solvents, and dispersing an antineoplastic compound selected from the group consisting of teniposide, paclitaxel, camptothecin and derivatives thereof in said solvent.
Claim 13
Dependent Claim
12 words
The method of claim 10 wherein said solvent further comprises an alcohol.
Claim 14
Dependent Claim
20 words
The method of claim 10 wherein said solvent is a mixture of ethyl alcohol, acid and said polyoxyethylated castor oil.
Claim 15
Dependent Claim
28 words
The method of claim 10 wherein said polyoxyethylated castor oil is a condensation product of castor oil, and 20-40 moles of ethylene oxide per mole of castor oil.
Claim 16
Dependent Claim
12 words
The method of claim 10 wherein said acid is a mineral acid.
Claim 17
Dependent Claim
29 words
The method of claim 10 wherein said acid is selected from the group consisting of HCl, HBr, HI, HF, H 2 SO 4 , HNO 3 and acetic acid.
Claim 18
Dependent Claim
31 words
The method of claim 10 wherein said solvent contains a mineral acid in an amount to provide about 5.6×10 -6 to 8.4×10 -6 g of H + per ml of solvent.
Claim 19
Dependent Claim
11 words
The method of claim 10 wherein said antineoplastic compound is teniposide.
Claim 20
Dependent Claim
11 words
The method of claim 10 wherein said antineoplastic compound is camptothecin.
Claim 21
Dependent Claim
47 words
A stabilized composition comprising paclitaxel and a solvent capable of dispersing or solubilizing said paclitaxel comprising polyoxyethylated castor oil and sufficient acid to provide said solvent with a carboxylate anion content less than or equal to 0.6×10 -6 g equivalents of carboxylate anion per ml of solvent.
Claim 22
Dependent Claim
47 words
A stabilized composition comprising paclitaxel and a solvent capable of dispersing or solubilizing said paclitaxel comprising polyoxyethylated castor oil and sufficient acid to provide said solvent with a carboxylate anion content less than or equal to 0.6×10 -6 g equivalents of carboxylate anion per ml of solvent.
Claim 23
Independent Claim
50 words
A method of preparing a stabilized composition comprising preparing a solvent comprising a polyoxyethylated castor oil and sufficient acid to provide said solvent with a carboxylate anion content less than or equal to 0.6×10 -6 g equivalents of carboxylate anion per ml of solvents, and dispersing paclitaxel in said solvent.
Claim 24
Independent Claim
50 words
A method of preparing a stabilized composition comprising preparing a solvent comprising a polyoxyethylated castor oil and sufficient acid to provide said solvent with a carboxylate anion content less than or equal to 0.6×10 -6 g equivalents of carboxylate anion per ml of solvents, and dispersing paclitaxel in said solvent.
References Cited (Backward Citations)
AU5196793A
Cited
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