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US4797282A
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Drug depot containing cytostatics
Assignee: Merck Patent GmbH
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Filing: 1986-04-18
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Granted: 1989-01-10
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Expires: 2006-04-18
Abstract
Abstract A drug depot, which can be implanted in the body, for the controlled, delayed release of cytostatics, comprises a synthetic material based on polyacrylates and/or polymethacrylates containing a cytostatic and at least one amino acid. The depot can be used in a particularly advantageous manner for the local control of tumors.
Inventors
- 👤 Helmut Wahlig
- 👤 Elvira Dingeldein
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-10-24 03:40
CPC Classifications
A; A61; A61K; A61K9/00; A61K9/0012; A61K9/0019; A61K9/0024; A61K9/20; A61K9/2004; A61K9/2013; A61K9/2022; A61K9/2027; A61L; A61L24/00; A61L24/001; A61L24/0015; A61L24/04; A61L24/06; A61L2300/00; A61L2300/40; A61L2300/404; A61L2300/406; A61L2300/416
Claims Analysis
Total Claims: 23
Claim 1
Independent Claim
54 words
A drug depot composition comprising a base of a polyacrylate or polymethacrylate, an amount of an amino acid effective to control the release of the drug from the composition and an effective amount of a cytostatic agent, wherein the amino acid is in the form of particles of a size less than 125 μm.
Claim 2
Dependent Claim
54 words
A drug depot composition comprising a base of a polyacrylate or polymethacrylate, an amount of an amino acid effective to control the release of the drug from the composition and an effective amount of a cytostatic agent, wherein the amino acid is in the form of particles of a size less than 125 μm.
Claim 3
Dependent Claim
14 words
A drug depot composition of claim 1 comprising 1-15% b.w of an amino acid.
Claim 4
Dependent Claim
13 words
A composition according to claim 1, further comprising an antibiotic or antiseptic agent.
Claim 5
Dependent Claim
15 words
A composition according to claim 1, wherein the cytostatic agent is adriamycin, 5-fluorouracil or methotrexate.
Claim 6
Dependent Claim
12 words
A composition according to claim 4, wherein the cytostatic agent is methotrexate.
Claim 7
Dependent Claim
18 words
A composition according to claim 1, wherein the cytostatic agent is present in an amount of 0.1-4% b.w.
Claim 8
Dependent Claim
17 words
A composition according to claim 1, wherein the cytostatic agent is present in amount of 0.2-2% b.w.
Claim 9
Dependent Claim
23 words
A composition according to claim 1, wherein the amino acid is a monobasic natural amino acid having a molecular weight of about 75-200.
Claim 10
Dependent Claim
18 words
A composition according to claim 8, wherein the amino acid is glycine, alanine, histidine, leucine, threonine or arginine.
Claim 11
Dependent Claim
12 words
A composition according to claim 4, wherein the amino acid is arginine.
Claim 12
Dependent Claim
15 words
A composition according to claim 1, wherein the amino acid is a monomeric amino acid.
Claim 13
Dependent Claim
26 words
A composition according to claim 1, wherein the amino acid particles are rod-shaped and at least 95% have a nominal diameter of less than 50 μm.
Claim 14
Dependent Claim
14 words
A composition of claim 1, wherein the amino acid particles are freeze dried particles.
Claim 15
Dependent Claim
14 words
A composition of claim 9, wherein the amino acid particles are freeze dried particles.
Claim 16
Dependent Claim
72 words
A kit for the preparation of a drug depot, having as components a polyacrylate or polymethacrylate base comprising an effective amount of a cytostatic agent, and at least one of a polymer of an acrylic or methacrylic ester, an amino acid, an acrylic or methacrylic ester monomer, or a polymerization catalyst, whereby the components may be combined to form a bone cement or a component for the preparation of a bone cement.
Claim 17
Dependent Claim
72 words
A kit for the preparation of a drug depot, having as components a polyacrylate or polymethacrylate base comprising an effective amount of a cytostatic agent, and at least one of a polymer of an acrylic or methacrylic ester, an amino acid, an acrylic or methacrylic ester monomer, or a polymerization catalyst, whereby the components may be combined to form a bone cement or a component for the preparation of a bone cement.
Claim 18
Dependent Claim
35 words
A kit according to claim 15, comprising an effective amount of a cytostatic agent, a polymer of an acrylic or methacrylic ester, an amino acid, an acrylic or mthacrylic ester monomer, and a polymerization catalyst.
Claim 19
Dependent Claim
13 words
A kit according to claim 16, further comprising an antibiotic or antiseptic agent.
Claim 20
Dependent Claim
15 words
A kit according to claim 16, wherein the cytostatic agent is adriamycin, 5-fluorouracil or methotrexate.
Claim 21
Dependent Claim
24 words
A composition according to claim 14, wherein the amino acid is a monobasic natural amino acid having a molecular weight of about 75-200 .
Claim 22
Dependent Claim
34 words
A method of achieving a depot effect in the administration of a cytostatic agent to a patient comprising administering said agent to the patient in the form of a drug depot of claim 1.
Claim 23
Dependent Claim
27 words
A method for locally treating a tumor in a patient comprising implanting in the patient a drug depot of claim 1 at the locus of the tumor.
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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) | 1992-01-10 | 1992-07-11 | 1993-01-10 | $2000.00 | Window Closed / Lapsed |
| 7.5 Years (Year 8) | 1996-01-10 | 1996-07-11 | 1997-01-10 | $3760.00 | Window Closed / Lapsed |
| 11.5 Years (Year 12) | 2000-01-10 | 2000-07-11 | 2001-01-10 | $7700.00 | Window Closed / Lapsed |