US4975280A
Expired / Lapsed
US
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Bioerodable sustained release implants
Assignee: Ethyl Corp
•
Filing: 1989-01-23
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Granted: 1990-12-04
•
Expires: 2009-01-23
Abstract
Abstract A device for controlled release of one or more pharmacologically active substances within an animal which comprises (i) a body of a bioerodable solid state poly(amino acid ester) phosphazene polymer, and (ii) at least one pharmacologically active substance physically incorporated within said body. The device may comprise an implantable body in which the poly(amino acid ester)phosphazene polymer is a matrix within which such pharmacologically active substance is dispersed. Alternatively, the polymer may constitute a coating or container within which such pharmacologically active substance is physically encased--i.e., the polymer surrounds the active agent as in a capsule or in a microencapsulated form. Results of in vivo experiments using implants of poly[bis((ethyl glycino)phosphazene] containing 25% ethidium are described.
Inventors
- 👤 Etienne Schacht
- 👤 Jan Crommen
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-10-23 15:24
CPC Classifications
A; A61; A61K; A61K9/00; A61K9/0012; A61K9/0019; A61K9/0024; A61K9/20; A61K9/2004; A61K9/2022; A61K9/2031; A61K9/2045
Claims Analysis
Total Claims: 64
Claim 1
Independent Claim
187 words
A device for controlled release of one or more pharmacologically active substances within an animal which comprises (i) a bioerodable solid state poly(amino acid ester)phosphazene polymer represented by the general formula [N--P(R--L).sub.2x (R"--OR').sub.2y ].sub.n wherein R is the residue of an alpha-amino acid, R' is a hydrocarbyl group, R" is the residue of an alpha-amino acid, n is from about 50 to about 25,000, and x is a number averaging from 0.05 to 1.00 per repeating unit and y is a number averaging from 0.95 to 0.00 per repeating unit so that per repeating unit the sum of x and y is 1, and wherein L is R 1 OR 2 , OCH(R 3 )COOR 4 , or OR 5 in which R 1 is the residue of an alpha-amino acid, R 2 , R 4 , and R 5 are hydrocarbyl groups, and R 3 is a hydrogen atom or a hydrocarbyl group; and (ii) at least one pharmacologically active substance physically incorporated within said polymer, said pharmacologically active substance comprising a trypanocide, antibiotic/antibacterial, antiparasitic, non-steroidal antiinflammatory, growth permittant, steroid hormone, growth hormone, or estrus synchronizer.
Claim 2
Independent Claim
187 words
A device for controlled release of one or more pharmacologically active substances within an animal which comprises (i) a bioerodable solid state poly(amino acid ester)phosphazene polymer represented by the general formula [N--P(R--L).sub.2x (R"--OR').sub.2y ].sub.n wherein R is the residue of an alpha-amino acid, R' is a hydrocarbyl group, R" is the residue of an alpha-amino acid, n is from about 50 to about 25,000, and x is a number averaging from 0.05 to 1.00 per repeating unit and y is a number averaging from 0.95 to 0.00 per repeating unit so that per repeating unit the sum of x and y is 1, and wherein L is R 1 OR 2 , OCH(R 3 )COOR 4 , or OR 5 in which R 1 is the residue of an alpha-amino acid, R 2 , R 4 , and R 5 are hydrocarbyl groups, and R 3 is a hydrogen atom or a hydrocarbyl group; and (ii) at least one pharmacologically active substance physically incorporated within said polymer, said pharmacologically active substance comprising a trypanocide, antibiotic/antibacterial, antiparasitic, non-steroidal antiinflammatory, growth permittant, steroid hormone, growth hormone, or estrus synchronizer.
Claim 3
Dependent Claim
22 words
A device of claim 1 wherein said bierodable solid state polymer is a matrix within which such pharmacologically active substance is dispersed.
Claim 4
Dependent Claim
25 words
A device of claim 1 wherein said bioerodable solid state polymer is a coating or container within which such pharmacologically active substance is physically incorporated.
Claim 5
Dependent Claim
13 words
A device of claim 1 wherein the pharmacologically active substance is a trypanocide.
Claim 6
Dependent Claim
12 words
A device of claim 1 wherein the pharmacologically active substance is ethidium.
Claim 7
Dependent Claim
11 words
A device of claim 1 wherein said polymer is poly[bis(ethyl glycino)phosphazene].
Claim 8
Dependent Claim
18 words
A device of claim 1 wherein said polymer is poly[bis(ethyl glycino)phosphazene] and the pharmacologically active substance is ethidium.
Claim 9
Dependent Claim
19 words
A device of claim 1 wherein said polymer is a matrix of poly[bis(ethyl glycino)phosphazene] within which ethidium is dispersed.
Claim 10
Independent Claim
179 words
A device for controlled release of one or more pharmacologically active substances within a living body which comprises (i) a bioerodable solid state poly(amino acid ester)phosphazene polymer of the general formula [N═P(R--L).sub.2x (GlyOR').sub.2y ].sub.n wherein R is the residue of an alpha-amino acid, R' is a hydrocarbyl group, n is from about 50 to about 25,000, and x is a number averaging from 0.05 to 0.95 per repeating unit and y is a number averaging from 0.95 to 0.05 per repeating unit so that per repeating unit the sum of x and y is 1, and wherein L is R 1 OR 2 , OCH(R 3 )COOR 4 , or OR 5 in which R 1 is the residue of an alpha-amino acid, R 2 , R 4 , and R 5 are hydrocarbyl groups, and R 3 is a hydrogen atom or a hydrocarbyl group; and (ii) at least one pharmacologically active substance physically incorporated in said polymer, said pharmacologically active substance comprising a trypanocide, antibiotic/antibacterial, antiparasitic, non-steroidal antiinflammatory, growth permittant, steroid hormone, growth hormone, or estrus synchronizer.
Claim 11
Independent Claim
179 words
A device for controlled release of one or more pharmacologically active substances within a living body which comprises (i) a bioerodable solid state poly(amino acid ester)phosphazene polymer of the general formula [N═P(R--L).sub.2x (GlyOR').sub.2y ].sub.n wherein R is the residue of an alpha-amino acid, R' is a hydrocarbyl group, n is from about 50 to about 25,000, and x is a number averaging from 0.05 to 0.95 per repeating unit and y is a number averaging from 0.95 to 0.05 per repeating unit so that per repeating unit the sum of x and y is 1, and wherein L is R 1 OR 2 , OCH(R 3 )COOR 4 , or OR 5 in which R 1 is the residue of an alpha-amino acid, R 2 , R 4 , and R 5 are hydrocarbyl groups, and R 3 is a hydrogen atom or a hydrocarbyl group; and (ii) at least one pharmacologically active substance physically incorporated in said polymer, said pharmacologically active substance comprising a trypanocide, antibiotic/antibacterial, antiparasitic, non-steroidal antiinflammatory, growth permittant, steroid hormone, growth hormone, or estrus synchronizer.
Claim 12
Dependent Claim
15 words
A device of claim 9 wherein L is R 1 OR 2 as therein defined.
Claim 13
Dependent Claim
13 words
A device of claim 10 wherein R and R 1 are both Gly.
Claim 14
Dependent Claim
14 words
A device of claim 10 wherein R is Gly and R 1 is Ala.
Claim 15
Dependent Claim
14 words
A device of claim 10 wherein R is Gly and R 1 is Leu.
Claim 16
Dependent Claim
14 words
A device of claim 10 wherein R is Gly and R 1 is PHe.
Claim 17
Dependent Claim
15 words
A device of claim 10 wherein R' and R 2 are both lower alkyl groups.
Claim 18
Dependent Claim
14 words
A device of claim 10 wherein R' and R 2 are both ethyl groups.
Claim 19
Dependent Claim
23 words
A device of claim 10 wherein R and R 1 are both Gly and R' and R 2 are both lower alkyl groups.
Claim 20
Dependent Claim
22 words
A device of claim 10 wherein R and R 1 are both Gly and R' and R 2 are both ethyl groups.
Claim 21
Dependent Claim
23 words
A device of claim 18 wherein x is about 0.3 and y is about 0.7 as determined by 360 MHz 1 H--NMR spectroscopy.
Claim 22
Dependent Claim
24 words
A device of claim 10 wherein R is Gly and R 1 is Ala and R' and R 2 are both lower alkyl groups.
Claim 23
Dependent Claim
23 words
A device of claim 10 wherein R is Gly and R 1 is Ala and R' and R 2 are both ethyl groups.
Claim 24
Dependent Claim
23 words
A device of claim 21 wherein x is about 0.85-0.9 and y is about 0.15-0.1 as determined by 350 MHZ 1 H--NMR spectroscopy.
Claim 25
Dependent Claim
24 words
A device of claim 10 wherein R is Gly and R 1 is Leu and R' and R 2 are both lower alkyl groups.
Claim 26
Dependent Claim
23 words
A device of claim 10 wherein R is Gly and R 1 is Leu and R' and R 2 are both ethyl groups.
Claim 27
Dependent Claim
23 words
A device of claim 24 wherein x is about 0.85-0.9 and y is about 0.15-0.1 as determined by 360 MHz 1 H--NMR spectroscopy.
Claim 28
Dependent Claim
24 words
A device of claim 10 wherein R is Gly and R 1 is Phe and R' and R 2 are both lower alkyl groups.
Claim 29
Dependent Claim
23 words
A device of claim 10 wherein R is Gly and R 1 is Phe and R' and R 2 are both ethyl groups.
Claim 30
Dependent Claim
23 words
A device of claim 27 wherein x is about 0.75-0.8 and y is about 0.25-0.2 as determined by 360 MHZ 1 H--NMR spectroscopy.
Claim 31
Dependent Claim
15 words
A device of claim 9 wherein L is OCH(R 3 )COOR 4 as therein defined.
Claim 32
Dependent Claim
9 words
A device of claim 29 wherein R is Gly.
Claim 33
Dependent Claim
11 words
A device of claim 29 wherein R 3 is lower alkyl.
Claim 34
Dependent Claim
10 words
A device of claim 29 wherein R 3 is methyl.
Claim 35
Dependent Claim
15 words
A device of claim 29 wherein R' and R 4 are both lower alkyl groups.
Claim 36
Dependent Claim
14 words
A device of claim 29 wherein R' and R 4 are both ethyl groups.
Claim 37
Dependent Claim
19 words
A device of claim 29 wherein R is Gly and R' and R 4 are both lower alkyl groups.
Claim 38
Dependent Claim
18 words
A device of claim 29 wherein R is Gly and R' and R 4 are both ethyl groups.
Claim 39
Dependent Claim
15 words
A device of claim 29 wherein R is Gly and R 3 is lower alkyl.
Claim 40
Dependent Claim
14 words
A device of claim 29 wherein R is Gly and R 3 is methyl.
Claim 41
Dependent Claim
20 words
A device of claim 29 wherein R is Gly and R', R 3 and R 4 are lower alkyl groups.
Claim 42
Dependent Claim
22 words
A device of claim 29 wherein R is Gly, R 3 is methyl, and R' and R 4 are lower alkyl groups.
Claim 43
Dependent Claim
22 words
A device of claim 29 wherein R is Gly, R 3 is methyl, and R' and R 4 are both ethyl groups.
Claim 44
Dependent Claim
23 words
A device of claim 41 wherein x is about 0.10-0.50 and y is about 0.90-0.50 as determined by 360 MHz 1 H--NMR spectroscopy.
Claim 45
Dependent Claim
13 words
A device of claim 9 wherein L is OR 5 as therein defined.
Claim 46
Dependent Claim
9 words
A device of claim 43 wherein R is Gly.
Claim 47
Dependent Claim
9 words
A device of claim 43 wherein R is Leu.
Claim 48
Dependent Claim
9 words
A device of claim 43 wherein R is Phe.
Claim 49
Dependent Claim
15 words
A device of claim 43 wherein R' and R 5 are both lower alkyl groups.
Claim 50
Dependent Claim
14 words
A device of claim 43 wherein R' and R 5 are both ethyl groups.
Claim 51
Dependent Claim
19 words
A device of claim 43 wherein R is Gly and R' and R 5 are both lower alkyl groups.
Claim 52
Dependent Claim
18 words
A device of claim 43 wherein R is Gly and R' and R 5 are both ethyl groups.
Claim 53
Dependent Claim
19 words
A device of claim 43 wherein R is Leu and R' and R 5 are both lower alkyl groups.
Claim 54
Dependent Claim
18 words
A device of claim 43 wherein R is Leu and R' and R 5 are both ethyl groups.
Claim 55
Dependent Claim
19 words
A device of claim 43 wherein R is Phe and R' and R 5 are both lower alkyl groups.
Claim 56
Dependent Claim
18 words
A device of claim 43 wherein R is Phe and R' and R 5 are both ethyl groups.
Claim 57
Dependent Claim
26 words
A device of claim 43 wherein R is Leu, x is about 0.45 and y is about 0.55 as determined by 360 MHz 1 H--NMR spectroscopy.
Claim 58
Dependent Claim
26 words
A device of claim 43 wherein R is Phe, x is about 0.75 and y is about 0.25 as determined by 360 MHz 1 H--NMR spectroscopy.
Claim 59
Dependent Claim
34 words
A device of claim 43 wherein R is Leu; R' and R 5 are both ethyl; and x is about 0.45 and y is about 0.55 as determined by 360 MHz 1 H--NMR spectroscopy.
Claim 60
Dependent Claim
34 words
A device of claim 43 wherein R is Phe; R' and R 5 are both ethyl; and x is about 0.45 and y is about 0.55 as determined by 360 MHz 1 H--NMR spectroscopy.
Claim 61
Dependent Claim
12 words
A device of claim 9 in the form of a body implant.
Claim 62
Dependent Claim
13 words
A device of claim 9 wherein the pharmacologically active substance is a trypanocide.
Claim 63
Dependent Claim
10 words
A device of claim 60 wherein the trypanocide is ethidium.
Claim 64
Dependent Claim
19 words
A device of claim 9 wherein the the polymer is poly[bis(ethylglycino)phosphazene] and the pharmacologically active substance is a trypanocide.
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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) | 1993-12-03 | 1994-06-04 | 1994-12-04 | $2000.00 | Window Closed / Lapsed |
| 7.5 Years (Year 8) | 1997-12-03 | 1998-06-04 | 1998-12-04 | $3760.00 | Window Closed / Lapsed |
| 11.5 Years (Year 12) | 2001-12-03 | 2002-06-04 | 2002-12-04 | $7700.00 | Window Closed / Lapsed |