US4293539A
Expired / Lapsed
US
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Controlled release formulations and method of treatment
Assignee: Eli Lilly and Co
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Filing: 1979-09-12
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Granted: 1981-10-06
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Expires: 1999-09-12
Abstract
Abstract Controlled release formulations useful in the prolonged treatment and control of microbial infections in animals are comprised of a microbial agent intimately dispersed throughout a copolymer derived from lactic acid and glycolic acid. A method for providing protection to animals for extended periods of time following a single administration is provided.
Inventors
- 👤 Nelson H. Ludwig
- 👤 Earl E. Ose
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-10-23 17:07
CPC Classifications
C; C08; C08G; C08G63/00; C08G63/02; C08G63/06; C08G63/08; A; A61; A61K; A61K9/00; A61K9/14; A61K9/16; A61K9/1605; A61K9/1629; A61K9/1641; A61K9/1647
Claims Analysis
Total Claims: 49
Claim 1
Independent Claim
103 words
A controlled release formulation capable of delivering an effective dose of active ingredient over a prolonged period of time and biodegradable into readily metabolized substances and normal active ingredient metabolic products comprising about 5 to about 85 percent by weight of active ingredient intimately dispersed throughout a copolymer derived from about 60 to about 95 weight percent lactic acid and about 40 to about 5 weight percent glycolic acid, said copolymer having an inherent viscosity of about 0.08 to about 0.30 when measured in chloroform, a molecular weight of about 6000 to about 35000, and said copolymer being substantially free of polymerization catalyst.
Claim 2
Dependent Claim
103 words
A controlled release formulation capable of delivering an effective dose of active ingredient over a prolonged period of time and biodegradable into readily metabolized substances and normal active ingredient metabolic products comprising about 5 to about 85 percent by weight of active ingredient intimately dispersed throughout a copolymer derived from about 60 to about 95 weight percent lactic acid and about 40 to about 5 weight percent glycolic acid, said copolymer having an inherent viscosity of about 0.08 to about 0.30 when measured in chloroform, a molecular weight of about 6000 to about 35000, and said copolymer being substantially free of polymerization catalyst.
Claim 3
Dependent Claim
29 words
The formulation of claim 1 wherein the active ingredient is an antimicrobial agent and the formulation is useful in the prophylactic and therapeutic treatment of diseases caused by microorganisms.
Claim 4
Dependent Claim
50 words
The formulation of claim 2 wherein the copolymer utilized is derived from about 60 to about 90 percent lactic acid and about 40 to about 10 percent glycolic acid, said copolymer having a viscosity of about 0.10 to about 0.25 and a molecular weight of about 15,000 to about 30,000.
Claim 5
Dependent Claim
29 words
The formulation of claim 3 wherein the active ingredient is an antimicrobial agent selected from the group consisting of the penicillins, cephalosporins, tetracyclines, sulfa drugs, macrolide antibiotics, and aminoglycosides.
Claim 6
Dependent Claim
49 words
The formulation of claim 3 wherein the active ingredient is an antibacterial agent selected from chlortetracycline, tetracycline, oxytetracycline, doxycycline, ampicillin, benzylpenicillin, penicillin V, cephalosporins, cloxicillin, streptomycin, lincomycin, novobiocin, neomycin, spiramycin, erythromycin, colistin, nalidixic acid, salinomycin, nigericin, kanamycin, kitsamycin, gentamycin, tobramycin, apramycin, furaltadone, vancomycin, thiostrepton, ristocetin, soimycin, tylosin or sulfonamides.
Claim 7
Dependent Claim
39 words
The formulation of claim 5 wherein the copolymer matrix is derived from about 70 to about 80 percent lactic acid and about 30 to about 20 percent glycolic acid, having an inherent viscosity of about 0.13 to about 0.23.
Claim 8
Dependent Claim
27 words
The formulation of claim 6 wherein the active ingredient is selected from the group consisting of tetracycline, oxytetracycline, doxycycline, lincomycin, spiramycin, neomycin, erythromycin, tylosin, and 3-methyl-7-α-methoxyimino-α-(2-aminothiazol-4-yl)acetamido-3-cephem-4-carboxylic acid.
Claim 9
Dependent Claim
54 words
The formulation of claim 7 comprising about 20 to about 75 percent by weight of active ingredient uniformly admixed with a copolymer matrix derived from about 70 to about 80 weight percent lactic acid and about 30 to about 20 percent glycolic acid, said copolymer having a viscosity of about 0.13 to about 0.23.
Claim 10
Dependent Claim
20 words
The formulation of claim 8 wherein the active ingredient is present in about 30 to about 60 percent by weight.
Claim 11
Dependent Claim
11 words
The formulation of claim 9 wherein the active ingredient is doxycycline.
Claim 12
Dependent Claim
11 words
The formulation of claim 9 wherein the active ingredient is oxytetracycline.
Claim 13
Dependent Claim
12 words
The formulation of claim 9 wherein the active ingredient is 3-methyl-7-α-methoxyimino-α-(2-aminothiazol-4-yl)acetamido-3-cephem-4-carboxylic acid.
Claim 14
Dependent Claim
11 words
The formulation of claim 9 wherein the active ingredient is lincomycin.
Claim 15
Dependent Claim
11 words
The formulation of claim 9 wherein the active ingredient is spiramycin.
Claim 16
Dependent Claim
11 words
The formulation of claim 9 wherein the active ingredient is erythromycin.
Claim 17
Dependent Claim
11 words
The formulation of claim 9 wherein the active ingredient is neomycin.
Claim 18
Dependent Claim
11 words
The formulation of claim 9 wherein the active ingredient is tylosin.
Claim 19
Dependent Claim
57 words
The formulation of claim 17, said formulation comprising about 30 to about 60 percent by weight of tylosin admixed with from about 70 to about 40 percent by weight of a copolymer derived from about 70 to about 80 percent by weight of lactic acid and about 30 to about 20 percent by weight of glycolic acid.
Claim 20
Dependent Claim
41 words
The formulation of claim 17, said formulation comprised of about 40 percent tylosin admixed with a copolymer derived from about 80 percent lactic acid and about 20 percent glycolic acid, said copolymer having a viscosity of about 0.18 to about 0.23.
Claim 21
Dependent Claim
42 words
The formulation of claim 17, said formulation comprised of about 50 percent by weight of tylosin admixed with a copolymer derived from about 80 percent lactic acid and about 20 percent glycolic acid having a viscosity of about 0.18 to about 0.23.
Claim 22
Dependent Claim
42 words
The formulation of claim 17, said formulation comprised of about 55 percent by weight of tylosin admixed with a copolymer derived from about 80 percent lactic acid and about 20 percent glycolic acid having a viscosity of about 0.18 to about 0.23.
Claim 23
Dependent Claim
22 words
The formulation of claim 17 in the form of extruded glass-like rods having a diameter of about 2 to about 7 mm.
Claim 24
Dependent Claim
29 words
The formulation of claim 17 in the form of extruded glass-like rods being ground to uniformity and passed through a sieve having mesh of about 60 to about 140.
Claim 25
Dependent Claim
19 words
A method of treating microbial infections in animals comprising administering an effective amount of a formulation of claim 1.
Claim 26
Dependent Claim
19 words
A method of treating microbial infections in animals comprising administering an effective amount of the formulation of claim 5.
Claim 27
Dependent Claim
26 words
A method of treating animals suffering from a microbial infection and in need of treatment comprising administering an effective amount of the formulation of claim 7.
Claim 28
Dependent Claim
26 words
A method of treating animals suffering from a microbial infection and in need of treatment comprising administering an effective amount of the formulation of claim 9.
Claim 29
Dependent Claim
26 words
A method of treating animals suffering from a microbial infection and in need of treatment comprising administering an effective amount of the formulation of claim 18.
Claim 30
Dependent Claim
11 words
The method of claim 28 wherein the microbial infection is pneumonia.
Claim 31
Dependent Claim
12 words
The method of claim 29 wherein the host is a young calf.
Claim 32
Dependent Claim
29 words
A method of treating a young calf suffering from pneumonia and in need of treatment comprising administering to said calf an effective amount of the formulation of claim 18.
Claim 33
Dependent Claim
22 words
The method of claim 31 wherein the formulation is in the form of an extruded glass-like rod and administered by subcutaneous implantation.
Claim 34
Dependent Claim
25 words
The method of claim 31 wherein the formulation is in the form of a uniformly ground extruded glass-like rod suspended in a suitable pharmaceutical vehicle.
Claim 35
Dependent Claim
13 words
The method of claim 33 wherein the formulation is administered by subcutaneous injection.
Claim 36
Dependent Claim
24 words
A method for the prophylactic treatment of microbial infections in animals comprising the administration of an effective amount of the formulation of claim 1.
Claim 37
Dependent Claim
24 words
A method for the prophylactic treatment of microbial infections in animals comprising the administration of an effective amount of the formulation of claim 7.
Claim 38
Dependent Claim
24 words
A method for the prophylactic treatment of microbial infections in animals comprising the administration of an effective amount of the formulation of claim 18.
Claim 39
Dependent Claim
14 words
The method of treatment of claim 37 wherein the host animal is a ruminant.
Claim 40
Dependent Claim
12 words
The method of claim 38 wherein the animal is a young calf.
Claim 41
Dependent Claim
13 words
The method of claim 39 wherein the microbial infection being treated is pneumonia.
Claim 42
Dependent Claim
11 words
The method of claim 37 wherein the host animal is swine.
Claim 43
Dependent Claim
13 words
The method of claim 41 wherein the animal treated is a young pig.
Claim 44
Dependent Claim
14 words
The method of claim 42 wherein the animal treated is a new born pig.
Claim 45
Dependent Claim
12 words
The method of claim 41 wherein the disease guarded against is pneumonia.
Claim 46
Dependent Claim
13 words
The method of claim 43 wherein the disease guarded against is mycoplasmal pneumonia.
Claim 47
Dependent Claim
12 words
The method of claim 37 wherein the host animal is a chicken.
Claim 48
Dependent Claim
12 words
The method of claim 46 wherein the disease guarded against is pneumonia.
Claim 49
Dependent Claim
14 words
The method of claim 37 wherein the disease guarded against is chronic respiratory disease.
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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) | 1984-10-05 | 1985-04-06 | 1985-10-06 | $2000.00 | Window Closed / Lapsed |
| 7.5 Years (Year 8) | 1988-10-05 | 1989-04-06 | 1989-10-06 | $3760.00 | Window Closed / Lapsed |
| 11.5 Years (Year 12) | 1992-10-05 | 1993-04-06 | 1993-10-06 | $7700.00 | Window Closed / Lapsed |