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US5573781A
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Methods and compositions for the treatment of a host with a cellular proliferative disease
Assignee: Intarcia Therapeutics Inc
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Filing: 1994-12-29
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Granted: 1996-11-12
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Expires: 2014-12-29
Abstract
Abstract Methods and compositions are provided for the treatment of a host with a cellular proliferative disease, particularly a neoplasia. In the subject methods, a pharmaceutically acceptable, substantially anhydrous, injectable semi-solid composition which acts as a depot for a cytostatic agent, is administered to a lesion of the disease, particularly intralesionally. The subject compositions comprise a water immiscible, fatty acid ester matrix and a cytostatic agent.
Inventors
- 👤 Dennis M. Brown
- 👤 Richard E. Jones
- 👤 Richard Maskiewicz
- 👤 Shawnya K. Michaels
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-10-31 23:21
CPC Classifications
A; A61; A61K; A61K9/00; A61K9/0012; A61K9/0019; A61K33/00; A61K33/24; A61K33/243; A61K47/00; A61K47/06; A61K47/08; A61K47/10; A61K47/44; A61P; A61P3/00; A61P3/06; A61P35/00; A61P43/00
Claims Analysis
Total Claims: 45
Claim 1
Independent Claim
63 words
A pharmaceutically acceptable, substantially anhydrous, intralesionally injectable, semi-solid cytostatic composition to act as a depot in the treatment of a host with a cellular proliferative disease susceptible to a cytostatic agent, said composition comprising: (a) a carrier composition comprising a water immiscible, fatty acid ester matrix; and (b) said cytostatic agent in an amount to slow the growth of said cellular proliferative disease.
Claim 2
Dependent Claim
63 words
A pharmaceutically acceptable, substantially anhydrous, intralesionally injectable, semi-solid cytostatic composition to act as a depot in the treatment of a host with a cellular proliferative disease susceptible to a cytostatic agent, said composition comprising: (a) a carrier composition comprising a water immiscible, fatty acid ester matrix; and (b) said cytostatic agent in an amount to slow the growth of said cellular proliferative disease.
Claim 3
Dependent Claim
14 words
The composition according to claim 1, wherein said fatty acid ester matrix comprises glycerides.
Claim 4
Dependent Claim
39 words
The composition according to claim 2, wherein said fatty acid ester matrix is a naturally occurring vegetable oil, a hydrogenated naturally occurring vegetable oil or mixture of hydrogenated naturally occurring vegetable oils, or a thickened naturally occurring vegetable oil.
Claim 5
Dependent Claim
19 words
The composition according to claim 3, wherein said cytostatic agent is present in from about 0.5 to 50 mg/ml.
Claim 6
Dependent Claim
26 words
The composition according to claim 1, wherein said carrier composition further comprises at least 10(v/v) % of an alkanol of from 2 to 3 carbon atoms.
Claim 7
Dependent Claim
91 words
A pharmaceutically acceptable, substantially anhydrous, intralesionally injectable semi-solid cytostatic composition to act as a depot in the treatment of a host with a cellular proliferative disease susceptible to a cytostatic agent, said composition comprising: (a) a carrier composition consisting of: a water immiscible, fatty acid ester matrix, wherein said fatty acid ester matrix is from 5 to 100 weight % of said carrier composition; and an alkanol of from 2 to 3 carbon atoms: and (b) said cytostatic agent in an amount to slow the growth of said cellular proliferative disease.
Claim 8
Dependent Claim
91 words
A pharmaceutically acceptable, substantially anhydrous, intralesionally injectable semi-solid cytostatic composition to act as a depot in the treatment of a host with a cellular proliferative disease susceptible to a cytostatic agent, said composition comprising: (a) a carrier composition consisting of: a water immiscible, fatty acid ester matrix, wherein said fatty acid ester matrix is from 5 to 100 weight % of said carrier composition; and an alkanol of from 2 to 3 carbon atoms: and (b) said cytostatic agent in an amount to slow the growth of said cellular proliferative disease.
Claim 9
Dependent Claim
22 words
The composition according to claim 6, wherein said alkanol is ethanol and is present in from about 30 to 95 (v/v) %.
Claim 10
Dependent Claim
39 words
The composition according to claim 6, wherein said fatty acid ester matrix is a naturally occurring vegetable oil, a hydrogenated naturally occurring vegetable oil or mixture of hydrogenated naturally occurring vegetable oils, or a thickened naturally occurring vegetable oil.
Claim 11
Dependent Claim
31 words
The composition according to claim 6, wherein said fatty acid ester matrix is a thickened naturally occurring vegetable oil comprising from about 0.5 to 40 (w/v) % of a thickening agent.
Claim 12
Dependent Claim
14 words
The composition according to claim 6, wherein said composition further comprises an effector agent.
Claim 13
Dependent Claim
28 words
The composition according to claim 10, wherein said effector agent is a vasoconstrictor agent and is epinephrine, eoinephrine borate or ephedrine in from about 0.1 to 2.5 mg/ml.
Claim 14
Dependent Claim
125 words
A pharmaceutically acceptable, substantially anhydrous, injectable, semi-solid cytostatic composition to act as a depot in the treatment of a host with a cellular proliferative disease susceptible to a cytostatic agent, having a viscosity in the range of about 5,000 to 50,000 cps at low shear, said composition comprising: a carrier composition consisting of: a water immiscible, fatty acid ester matrix comprising at least one physiologically acceptable vegetable oil, wherein said fatty acid ester matrix is at least 2 and not more than about 30 weight % of said composition; and ethanol in up to 98 v/v % of said composition; and said cytostatic agent in an amount to slow the growth of said cellular proliferative disease in the range of about 0.5 to 50 mg/ml.
Claim 15
Dependent Claim
125 words
A pharmaceutically acceptable, substantially anhydrous, injectable, semi-solid cytostatic composition to act as a depot in the treatment of a host with a cellular proliferative disease susceptible to a cytostatic agent, having a viscosity in the range of about 5,000 to 50,000 cps at low shear, said composition comprising: a carrier composition consisting of: a water immiscible, fatty acid ester matrix comprising at least one physiologically acceptable vegetable oil, wherein said fatty acid ester matrix is at least 2 and not more than about 30 weight % of said composition; and ethanol in up to 98 v/v % of said composition; and said cytostatic agent in an amount to slow the growth of said cellular proliferative disease in the range of about 0.5 to 50 mg/ml.
Claim 16
Dependent Claim
25 words
The composition according to claim 12, wherein said physiologically acceptable vegetable oil is selected from the group consisting of peanut, cottonseed, soybean, and sesame oils.
Claim 17
Dependent Claim
61 words
The composition according to claim 12, wherein said fatty acid ester matrix is at least 10 (w/v) % of said carrier composition and further comprises a thickening agent selected from the group consisting of triglyceride fatty acids or fatty acid salts of at least 8 carbon atoms, cetyl/stearyl alcohol, wax esters, guar gum, methyl cellulose, hydroxypropyl cellulose and polyethylene glycol 4000.
Claim 18
Dependent Claim
28 words
The composition according to claim 12, wherein said cytostatic agent is selected from the group consisting of paclitaxel, mechlorethamine, ionomycin, etoposide, 5-fluorouracil, cantharidin, camptothecin, mitomycin, cisplatin and doxorubicin.
Claim 19
Dependent Claim
19 words
The composition according to claim 12, wherein said composition further comprises epinephrine in from about 0.1 to 2.5 mg/ml.
Claim 20
Dependent Claim
124 words
A pharmaceutically acceptable, substantially anhydrous, injectable, semi-solid cytostatic composition to act as a depot in the treatment of a host with a cellular proliferative disease susceptible to a cytostatic agent, having a viscosity in the range of about 5,000 to 50,000 cps at low shear, said composition comprising: a carrier composition comprising: a water immiscible, fatty acid ester matrix comprising at least one physiologically acceptable vegetable oil, wherein said fatty acid ester matrix is at least 2 and not more than about 95 weight % of said composition; and ethanol in up to 90 v/v % of said composition; and said cytostatic agent in an amount to slow the growth of said cellular proliferative disease in the range of about 0.5 to 50 mg/ml.
Claim 21
Dependent Claim
124 words
A pharmaceutically acceptable, substantially anhydrous, injectable, semi-solid cytostatic composition to act as a depot in the treatment of a host with a cellular proliferative disease susceptible to a cytostatic agent, having a viscosity in the range of about 5,000 to 50,000 cps at low shear, said composition comprising: a carrier composition comprising: a water immiscible, fatty acid ester matrix comprising at least one physiologically acceptable vegetable oil, wherein said fatty acid ester matrix is at least 2 and not more than about 95 weight % of said composition; and ethanol in up to 90 v/v % of said composition; and said cytostatic agent in an amount to slow the growth of said cellular proliferative disease in the range of about 0.5 to 50 mg/ml.
Claim 22
Dependent Claim
47 words
A composition according to claim 17, wherein said cytostatic agent has a solubility in water under standard temperature and pressure of less than about 0.1% w/v, said cytostatic composition has less than about 1 weight % water, and further comprises 0.1 to 2.5 mg/ml of a vasoconstrictor.
Claim 23
Dependent Claim
58 words
A pharmaceutically acceptable, substantially anhydrous cytostatic composition to act as a depot in the treatment of a host with a cellular proliferative disease susceptible to a cytostatic agent, said composition comprising: a water immiscible alkanol of from 4 to 8 carbon atoms; and said cytostatic agent in an amount to slow the growth of said cellular proliferative disease.
Claim 24
Dependent Claim
58 words
A pharmaceutically acceptable, substantially anhydrous cytostatic composition to act as a depot in the treatment of a host with a cellular proliferative disease susceptible to a cytostatic agent, said composition comprising: a water immiscible alkanol of from 4 to 8 carbon atoms; and said cytostatic agent in an amount to slow the growth of said cellular proliferative disease.
Claim 25
Dependent Claim
20 words
The composition according to claim 19, wherein said alkanol is selected from the group consisting of butanol, hexanol and octanol.
Claim 26
Dependent Claim
12 words
The composition according to claim 20, wherein said cytostatic agent is paclitaxel.
Claim 27
Independent Claim
68 words
A method for treating a host with a cellular proliferative disease susceptible to a cytostatic agent, said method comprising administering at the site of a lesion of said cellular proliferative disease a pharmaceutically acceptable, substantially anhydrous, injectable, semi-solid cytostatic composition comprising a carrier composition comprising a water immiscible, fatty acid ester matrix; and said cytostatic agent in an amount to slow the growth of said cellular proliferative disease.
Claim 28
Independent Claim
68 words
A method for treating a host with a cellular proliferative disease susceptible to a cytostatic agent, said method comprising administering at the site of a lesion of said cellular proliferative disease a pharmaceutically acceptable, substantially anhydrous, injectable, semi-solid cytostatic composition comprising a carrier composition comprising a water immiscible, fatty acid ester matrix; and said cytostatic agent in an amount to slow the growth of said cellular proliferative disease.
Claim 29
Dependent Claim
14 words
The method according to claim 22, wherein said fatty acid ester matrix comprises glycerides.
Claim 30
Dependent Claim
39 words
The method according to claim 23, wherein said fatty acid ester matrix is a naturally occurring vegetable oil, a hydrogenated naturally occurring vegetable oil or mixture of hydrogenated naturally occurring vegetable oils, or a thickened naturally occurring vegetable oil.
Claim 31
Dependent Claim
19 words
The method according to claim 24, wherein said cytostatic agent is present in from about 0.5 to 50 mg/ml.
Claim 32
Dependent Claim
26 words
The method according to claim 23, wherein said carrier composition further comprises at least 10(v/v) % of an alkanol of from 2 to 3 carbon atoms.
Claim 33
Independent Claim
115 words
A method for treating a host with a cellular proliferative disease susceptible to a cytostatic agent, said method comprising administering at the site of a lesion of said cellular proliferative disease a pharmaceutically acceptable, substantially anhydrous, injectable, semi-solid cytostatic composition comprising a carrier composition consisting of: a water immiscible, fatty acid ester matrix, wherein said fatty acid ester matrix is present in said composition in an amount from 10 to 90 weight %, and an alkanol selected from the group consisting of ethanol and isopropanol, wherein said alkanol is present in an amount from 10 to 90 v/v %; and said cytostatic agent in an amount to slow the growth of said cellular proliferative disease.
Claim 34
Independent Claim
115 words
A method for treating a host with a cellular proliferative disease susceptible to a cytostatic agent, said method comprising administering at the site of a lesion of said cellular proliferative disease a pharmaceutically acceptable, substantially anhydrous, injectable, semi-solid cytostatic composition comprising a carrier composition consisting of: a water immiscible, fatty acid ester matrix, wherein said fatty acid ester matrix is present in said composition in an amount from 10 to 90 weight %, and an alkanol selected from the group consisting of ethanol and isopropanol, wherein said alkanol is present in an amount from 10 to 90 v/v %; and said cytostatic agent in an amount to slow the growth of said cellular proliferative disease.
Claim 35
Dependent Claim
22 words
The method according to claim 27, wherein said method further comprises administration of a vasoconstrictor agent at the site of said lesion.
Claim 36
Dependent Claim
19 words
The method according to claim 28, wherein said vasoconstrictor agent is administered prior to administration of said cytostatic composition.
Claim 37
Dependent Claim
16 words
The method according to claim 29 wherein said vasoconstrictor is administered concurrently with said cytostatic composition.
Claim 38
Independent Claim
62 words
A method of treating a host with a cellular proliferative disease susceptible to a cytostatic agent, said method comprising administering at the site of a lesion of said cellular proliferative disease a composition comprising a water immiscible alkanol of from 4 to 8 carbon atoms and a said cytostatic agent in an amount to slow the growth of said cellular proliferative disease.
Claim 39
Independent Claim
62 words
A method of treating a host with a cellular proliferative disease susceptible to a cytostatic agent, said method comprising administering at the site of a lesion of said cellular proliferative disease a composition comprising a water immiscible alkanol of from 4 to 8 carbon atoms and a said cytostatic agent in an amount to slow the growth of said cellular proliferative disease.
Claim 40
Dependent Claim
28 words
The method according to claim 31, wherein said water immiscible alkanol is selected from the group consisting of butanol, hexanol and octanol and said cytostatic agent is paclitaxel.
Claim 41
Independent Claim
65 words
A method for treating a host with a neoplastic disease susceptible to a cytostatic agent, said method comprising administering at the site of a lesion of said neoplastic disease a pharmaceutically acceptable, substantially anhydrous, injectable, semi-solid cytostatic composition comprising a carrier composition comprising a water immiscible, fatty acid ester matrix; and said cytostatic agent in an amount to slow the growth of said neoplastic disease.
Claim 42
Independent Claim
65 words
A method for treating a host with a neoplastic disease susceptible to a cytostatic agent, said method comprising administering at the site of a lesion of said neoplastic disease a pharmaceutically acceptable, substantially anhydrous, injectable, semi-solid cytostatic composition comprising a carrier composition comprising a water immiscible, fatty acid ester matrix; and said cytostatic agent in an amount to slow the growth of said neoplastic disease.
Claim 43
Dependent Claim
14 words
The method according to claim 33, wherein said fatty acid ester matrix comprises glycerides.
Claim 44
Dependent Claim
27 words
The method according to claim 34, wherein said carrier composition further comprises at least 10 (v/v) % of an alkanol of from 2 to 3 carbon atoms.
Claim 45
Dependent Claim
19 words
The method according to claim 33, wherein said cytostatic agent is present in from about 0.5 to 50 mg/ml.
References Cited (Backward Citations)
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