US5030457A
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US
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Bioerodible polymers useful for the controlled release of therapeutic agents
Assignee: PHARMACEUTICAL DELIVERY SYSTEMS Inc A CORP OF CALIFORNIA
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Filing: 1989-08-28
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Granted: 1991-07-09
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Expires: 2009-08-28
Abstract
Abstract Bioerodible ortho ester polymers useful for preparing soft form bioerodible pharmaceutical compositions such as ointments, creams, gels and the like are provided. A novel synthetic method for preparing the polymers is provided as well. Synthesis involves a one-step reaction between a monomeric ortho ester and a triol. The pharmaceutical compositions of the invention are useful for the controlled release of therapeutic agents, and may be administered for a variety of purposes, such as for the treatment of deep wounds, including burns, and for the treatment of periodontal disease.
Inventors
- 👤 Steve Y. W. Ng
- 👤 Jorge Heller
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-10-23 10:48
CPC Classifications
A; A61; A61K; A61K47/00; A61K47/30; A61K47/34; A61K9/00; A61K9/20; A61K9/2004; A61K9/2022; A61K9/2031; A61K9/204; C; C08; C08G; C08G65/00; C08G65/34
Claims Analysis
Total Claims: 29
Claim 1
Independent Claim
87 words
A method for preparing a bioerodible polymer comprising: reacting a monomeric ortho ester having the general formula ##STR14## wherein R is hydrogen or alkyl of 1 to 10 carbon atoms and R' is lower alkyl with a triol having the general formula ##STR15## wherein A is selected from alkylenes and cycloalkylenes of at least 5 carbon atoms, and oxyalkylenes and cyclooxyalkylenes of at least 5 carbons, to form without isolation of any intermediate species a nonrigid, bioerodible ortho ester polymer comprising mer units of the structure ##STR16##
Claim 2
Independent Claim
87 words
A method for preparing a bioerodible polymer comprising: reacting a monomeric ortho ester having the general formula ##STR14## wherein R is hydrogen or alkyl of 1 to 10 carbon atoms and R' is lower alkyl with a triol having the general formula ##STR15## wherein A is selected from alkylenes and cycloalkylenes of at least 5 carbon atoms, and oxyalkylenes and cyclooxyalkylenes of at least 5 carbons, to form without isolation of any intermediate species a nonrigid, bioerodible ortho ester polymer comprising mer units of the structure ##STR16##
Claim 3
Dependent Claim
12 words
The method of claim 1 wherein R is hydrogen or lower alkyl.
Claim 4
Dependent Claim
19 words
The method of claim 1 wherein A is an alkylene of from about 5 to about 20 carbon atoms.
Claim 5
Dependent Claim
19 words
The method of claim 1 wherein A is a cycloalkylene moiety of from about 5 to 20 carbon atoms.
Claim 6
Dependent Claim
20 words
The method of claim 1 wherein A is a cyclooxyalkylene moiety of from about 5 to about 20 carbon atoms.
Claim 7
Dependent Claim
12 words
The method of claim 5 wherein said triol is a sugar residue.
Claim 8
Dependent Claim
41 words
The method of claim 1 wherein A has the general formula: ##STR17## wherein x is 0 or 1, y is greater than or equal to 2, and the R"s are independently selected from the group consisting of hydrogen and lower alkyl.
Claim 9
Dependent Claim
18 words
The method of claim 7 wherein x is 0, y is 4 and the R"s are each hydrogen.
Claim 10
Dependent Claim
25 words
The method of claim 1 wherein the number of mer units in the final polymer is in the range of about 2 to about 1000.
Claim 11
Dependent Claim
40 words
A polymer containing repeating mer units of the structure ##STR18## wherein R is hydrogen or alkyl of 1 to 10 carbon atoms and A is selected from the group consisting of cycloalkylenes and cyclooxyalkylene of at least 5 carbon atoms.
Claim 12
Dependent Claim
40 words
A polymer containing repeating mer units of the structure ##STR18## wherein R is hydrogen or alkyl of 1 to 10 carbon atoms and A is selected from the group consisting of cycloalkylenes and cyclooxyalkylene of at least 5 carbon atoms.
Claim 13
Dependent Claim
11 words
The polymer of claim 10 wherein A is a pentafuranose ring.
Claim 14
Dependent Claim
14 words
The polymer of claim 10 having a molecular weight of at least about 5,000.
Claim 15
Dependent Claim
14 words
The polymer of claim 10 having a molecular weight of at least about 20,000.
Claim 16
Dependent Claim
14 words
The polymer of claim 10 having a molecular weight of at least about 50,000.
Claim 17
Dependent Claim
36 words
A bioerodible pharmaceutical composition comprising in the form of an ointment an effective therapeutic amount of a therapeutic agent dispersed in a carrier comprising the polymer of claim 10 in combination with a pharmaceutically acceptable carrier.
Claim 18
Dependent Claim
11 words
The composition of claim 15 further comprising an added acidic excipient.
Claim 19
Independent Claim
38 words
A method for treating deep wounds, comprising administering to an affected patient an effective amount of a composition of any one of claims 15, 16, or 20, in which the therapeutic agent is a deep wound treating agent.
Claim 20
Independent Claim
38 words
A method for treating periodontal disease, comprising administering to an affected patient an effective amount of a composition of any one of claims 15, 16, or 20 in which the therapeutic agent is a periodontal disease treating agent.
Claim 21
Dependent Claim
19 words
The composition of any one of claims 15, 16 or 20 wherein said therapeutic agent is an antibacterial agent.
Claim 22
Dependent Claim
18 words
The composition of any one of claims 15, 16 or 20 wherein said therapeutic agent is an antibiotic.
Claim 23
Dependent Claim
19 words
The composition of any one of claims 15, 16, or 20 wherein said therapeutic agent is a proteinaceous drug.
Claim 24
Dependent Claim
14 words
The composition of claim 21 wherein said proteinaceous drug is an epidermal growth factor.
Claim 25
Dependent Claim
13 words
The composition of claim 21 wherein said proteinaceous drug is a growth hormone.
Claim 26
Dependent Claim
11 words
The composition of claim 15 wherein said therapeutic agent is hydrocortisone.
Claim 27
Dependent Claim
15 words
The method of claim 17 wherein said deep wound treating agent is a proteinaceous drug.
Claim 28
Dependent Claim
112 words
A bioerodible pharmaceutical composition comprising, in the form of an ointment, an effective therapeutic amount of a therapeutic agent dispersed in a carrier comprising a polymer containing repeating mer units of the structure ##STR19## wherein R is hydrogen or alkyl of 1 to 10 carbon atoms and A is selected from the group consisting of cycloalkylenes of at least 5 carbon atoms, cyclooxyalkylenes of at least 5 carbon atoms, and alkylenes having the structure CH.increment..sub.2 --(CR".sub.2).sub.x --CR"--(CR".sub.2).sub.y --, wherein x is 0 or 1, y is greater than or equal to 3, and R"s are independently selected from the group consisting of hydrogen and lower alkyl, and a pharmaceutically acceptable acidic excipient.
Claim 29
Dependent Claim
112 words
A bioerodible pharmaceutical composition comprising, in the form of an ointment, an effective therapeutic amount of a therapeutic agent dispersed in a carrier comprising a polymer containing repeating mer units of the structure ##STR19## wherein R is hydrogen or alkyl of 1 to 10 carbon atoms and A is selected from the group consisting of cycloalkylenes of at least 5 carbon atoms, cyclooxyalkylenes of at least 5 carbon atoms, and alkylenes having the structure CH.increment..sub.2 --(CR".sub.2).sub.x --CR"--(CR".sub.2).sub.y --, wherein x is 0 or 1, y is greater than or equal to 3, and R"s are independently selected from the group consisting of hydrogen and lower alkyl, and a pharmaceutically acceptable acidic excipient.
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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) | 1994-07-08 | 1995-01-07 | 1995-07-09 | $2000.00 | Window Closed / Lapsed |
| 7.5 Years (Year 8) | 1998-07-08 | 1999-01-07 | 1999-07-09 | $3760.00 | Window Closed / Lapsed |
| 11.5 Years (Year 12) | 2002-07-08 | 2003-01-07 | 2003-07-09 | $7700.00 | Window Closed / Lapsed |