US4148871A
Expired / Lapsed
US
⏱️ 0.0 years remaining
Sustained subdermal delivery ofdrugs using poly(ε-caprolactone) and its copolymers
Assignee: RTI International
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Filing: 1977-10-11
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Granted: 1979-04-10
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Expires: 1997-10-11
Abstract
Abstract Compositions containing either poly(ε-caprolactone) or copolymers of ε-caprolactone with other lactones, together with a drug, when subdermally implanted in the body, provide a slow sustained release of the drug. The polymers may be designed to biodegrade during or subsequent to the depletion of the drug.
Inventors
- 👤 Colin G. Pitt
- 👤 Anton E. Schindler
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-10-23 06:54
CPC Classifications
A; A61; A61K; A61K9/00; A61K9/0012; A61K9/0019; A61K9/0024
Claims Analysis
Total Claims: 17
Claim 1
Independent Claim
192 words
A subdermally implantable pharmaceutical composition comprising (a) a surgically implantable device in the form of a macrocapsule having a hollow cavity and being composed of a polymer or copolymer having repeating units of the formula ##STR5## wherein R' and R" are lower alkylene groups of up to six carbon atoms; n and are 0 or 1; and R'" and R"" are either hydrogen or a lower alkyl group of from 1 to about 6 carbon atoms; at least 5% of the polymer or copolymer being formed of the repeating unit ##STR6## derived from ε-hydroxy caproic acid, where m= 0, n=1, R' = (CH 2 ) 4 , and R'" and R"" = H, and (b) a drug contained within the hollow cavity of said device; said device, comprosed of said polymer or copolymer, having a sufficiently high permeability to the drug to enable it to be used in said macrocapsule form for subdermal implantation, being capable of holding a high drug content which can be released in an effective amount at a sustained constant rate for a long time, and which is capable of biodegrading after the drug supply has become depleted.
Claim 2
Dependent Claim
192 words
A subdermally implantable pharmaceutical composition comprising (a) a surgically implantable device in the form of a macrocapsule having a hollow cavity and being composed of a polymer or copolymer having repeating units of the formula ##STR5## wherein R' and R" are lower alkylene groups of up to six carbon atoms; n and are 0 or 1; and R'" and R"" are either hydrogen or a lower alkyl group of from 1 to about 6 carbon atoms; at least 5% of the polymer or copolymer being formed of the repeating unit ##STR6## derived from ε-hydroxy caproic acid, where m= 0, n=1, R' = (CH 2 ) 4 , and R'" and R"" = H, and (b) a drug contained within the hollow cavity of said device; said device, comprosed of said polymer or copolymer, having a sufficiently high permeability to the drug to enable it to be used in said macrocapsule form for subdermal implantation, being capable of holding a high drug content which can be released in an effective amount at a sustained constant rate for a long time, and which is capable of biodegrading after the drug supply has become depleted.
Claim 3
Dependent Claim
28 words
The pharmaceutical composition of claim 1, wherein said polymer comprises poly(ε -caprolactone) with a molecular weight corresponding to an intrinsic viscosity of greater than 1 dl/g in benzene.
Claim 4
Dependent Claim
25 words
The composition of claim 1 in which the device and the drug are present in the composition in the ratio of 10% to 90% respectively.
Claim 5
Dependent Claim
15 words
The pharmaceutical composition of claim 1 in which the drug is a steroidal contraceptive agent.
Claim 6
Dependent Claim
15 words
The pharmaceutical composition of claim 1 in which the drug is a non-steroidal contraceptive agent.
Claim 7
Dependent Claim
13 words
The pharmaceutical composition of claim 1 in which the drug is a narcotic.
Claim 8
Dependent Claim
14 words
The pharmaceutical composition of claim 1 in which the drug is a narcotic antagonist.
Claim 9
Dependent Claim
14 words
The pharmaceutical composition of claim 1 in which the drug is a hormonal agent.
Claim 10
Dependent Claim
14 words
The pharmaceutical composition of claim 1 in which the drug is an anti-neoplastic agent.
Claim 11
Dependent Claim
25 words
The composition of claim 1 in which the drug release can be sustained for a period of time of up to at least one year.
Claim 12
Dependent Claim
15 words
The pharmaceutical composition of claim 1 in which the polymer is a homopolymer of ε-caprolactone.
Claim 13
Dependent Claim
36 words
The pharmaceutical composition of claim 1 in which the copolymer consists of ε-caprolactone as the principal monomer and the co-monomer is a member selected from the group consisting of glycolide, dilactide, pivalolactone, valerolactone, ε-heptalactone, and ε-decalactone.
Claim 14
Dependent Claim
24 words
The pharmaceutical composition of claim 1 in which the drug, contained within the cavity of the device, is present as a solid micronized powder.
Claim 15
Dependent Claim
33 words
The pharmaceutical composition of claim 1 in which the drug, contained within the cavity of the device, is present as a solid micronized powder mixed with a suitable solvent, diluent, or dispersing agent.
Claim 16
Dependent Claim
103 words
A surgically implantable pharmaceutical composition comprising an intimate mixture of a drug and a polymer or copolymer having repeating units of the formula ##STR7## wherein R' and R" are lower alkylene groups of up to mix carbon atoms; n and m are 0 or 1; and R'" and R"" are either hydrogen or a lower alkyl group of from 1 to about 6 carbon atoms; at least 5% of the polymer or copolymer being formed of the repeating unit ##STR8## derived from ε-hydroxy caproic acid, where m= 0, n= 1, R' = (CH 2 ) 4 , and R'" and R"" = H.
Claim 17
Dependent Claim
103 words
A surgically implantable pharmaceutical composition comprising an intimate mixture of a drug and a polymer or copolymer having repeating units of the formula ##STR7## wherein R' and R" are lower alkylene groups of up to mix carbon atoms; n and m are 0 or 1; and R'" and R"" are either hydrogen or a lower alkyl group of from 1 to about 6 carbon atoms; at least 5% of the polymer or copolymer being formed of the repeating unit ##STR8## derived from ε-hydroxy caproic acid, where m= 0, n= 1, R' = (CH 2 ) 4 , and R'" and R"" = H.
References Cited (Backward Citations)
USPTO Annuity & Maintenance Windows
| Annuity Stage | Window Opens | Payment Deadline | Surcharge Period Until | Estimated Fee | Status |
|---|---|---|---|---|---|
| 3.5 Years (Year 4) | 1982-04-09 | 1982-10-09 | 1983-04-10 | $2000.00 | Window Closed / Lapsed |
| 7.5 Years (Year 8) | 1986-04-09 | 1986-10-09 | 1987-04-10 | $3760.00 | Window Closed / Lapsed |
| 11.5 Years (Year 12) | 1990-04-09 | 1990-10-09 | 1991-04-10 | $7700.00 | Window Closed / Lapsed |