EP0025698A2
Expired / Lapsed
EP
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Controlled release formulations
Assignee: Eli Lilly and Co
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Filing: 1980-09-11
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Granted: —
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Expires: 2000-09-11
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 Henry Ludwig
- 👤 Earl Eugene Ose
Bibliographic Details
Application Number
—
Jurisdiction
EP
Data Source
google_patents
Last Synchronized
2026-10-28 18:42
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: 23
Claim 1
Independent Claim
127 words
A controlled release formulation capable of delivering an effective dose of an antimicrobial agent over a prolonged period of time and biodegradable into readily metabolized substances and normal active ingredient metabolic products, which formulation is useful in the prophylactic and therapeutic treatment of diseases caused by microorganisms in animals, which comprises about 5 to about 85 weight percent of an antimicrobial agent 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 weight average molecular weight of about 6000 to about 35000, and said formulation being in combination with suitable excipients and carriers therefor.
Claim 2
Dependent Claim
127 words
A controlled release formulation capable of delivering an effective dose of an antimicrobial agent over a prolonged period of time and biodegradable into readily metabolized substances and normal active ingredient metabolic products, which formulation is useful in the prophylactic and therapeutic treatment of diseases caused by microorganisms in animals, which comprises about 5 to about 85 weight percent of an antimicrobial agent 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 weight average molecular weight of about 6000 to about 35000, and said formulation being in combination with suitable excipients and carriers therefor.
Claim 3
Dependent Claim
51 words
The formulation of claim 1, wherein the copolymer 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 weight average molecular weight of about 15,000 to about 30,000.
Claim 4
Dependent Claim
22 words
The formulation of claim 1 or 2 wherein the antimicrobial agent is a penicillin, cephalosporin, tetracycline, sulfa drug, macrolide antibiotic, or aminoglycoside.
Claim 5
Dependent Claim
47 words
The formulation of claim 3 wherein the antimicrobial agent is chlortetracycline, tetracycline, oxytetracycline, doxycycline, ampicillin, benzylpeni- cillin, 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, 5-0-mycaminosyl tylonolide or sulfonamides.
Claim 6
Dependent Claim
45 words
The formulation of any one of claims 1 to 4 wherein the copolymer is derived from about 70 to about 80 weight percent lactic acid and about 30 to about 20 weight percent glycolic acid, having an inherent viscosity of about 0.13 to about 0.23.
Claim 7
Dependent Claim
24 words
The formulation of claim 5 wherein the antimicrobial agent is tetracycline, oxytetracycline, doxycycline, lincomycin, spiramycin, neomycin, erythromycin, tylosin, 3-methyl-7-α-methoxyimino-α-(2-amino- thiazol-4-yl)acetamido-3-cephem-4-carboxylic acid, or 3-(l-methyl-5,6-dioxo-l,3,4-triazin-2-yl)thiomethyl-7-a-methoxyimino-a-(2-aminothiazol-4-yl)acetamido-3-cephem-4-carboxylic acid.
Claim 8
Dependent Claim
53 words
The formulation of claim 1 comprising about 20 to about 75 weight percent of antimicrobial agent uniformly admixed with a copolymer derived from about 70 to about 80 weight percent lactic acid and about 30 to about 20 weight percent glycolic acid, said copolymer having a viscosity of about 0.13 to about 0.23.
Claim 9
Dependent Claim
19 words
The formulation of claim 7 wherein the antimicrobial agent is present in about 30 to about 60 weight percent.
Claim 10
Dependent Claim
14 words
The formulation of claim 6 or 8 wherein -the antimicrobial agent is doxycycline. -
Claim 11
Dependent Claim
13 words
The formulation of claim 6 or 8 wherein the antimicrobial agent is oxytetracycline.
Claim 12
Dependent Claim
20 words
The formulation of claim 6 or 8 wherein the antimicrobial agent is 3-methyl-7-a-methoxyimino-a-(2-aminothiazol-4-yl)acetamido-3-cephem-4-carboxylic acid, or 3-(1-methyl-5,6-dioxo-1,3,4-triazin-2-yl)thiomethyl-7-α-methoxyimino-α-(2-aminothiazol-4-yl)acetamido-3-cephem-4-carboxylic acid or their salts.
Claim 13
Dependent Claim
13 words
The formulation of claim 6 or 8 wherein the antimicrobial agent is lincomycin.
Claim 14
Dependent Claim
13 words
The formulation of claim 6 or 8 wherein the antimicrobial agent is spiramycin.
Claim 15
Dependent Claim
13 words
The formulation of claim 6 or 8 wherein the antimicrobial agent is erythromycin.
Claim 16
Dependent Claim
13 words
The formulation of claim 6 or 8 wherein the antimicrobial agent is neomycin.
Claim 17
Dependent Claim
16 words
The formulation of claim 6 or 8 wherein the antimicrobial agent is tylosin or 5-0-mycaminosyl tylonolide.
Claim 18
Dependent Claim
53 words
The formulation of claim 1, said formulation comprising about 30 to about 60 weight percent of tylosin admixed with from about 70 to about 40 weight percent of a copolymer derived from about 70 to about 80 weight percent of lactic acid and about 30 to about 20 weight percent of glycolic acid.
Claim 19
Dependent Claim
44 words
The formulation of claim 1 or 17, said formulation comprising about 40 weight percent-tylosin admixed with a copolymer derived from about 80 weight percent lactic acid and about 20 weight percent glycolic acid, said copolymer having a viscosity of about 0.18 to about 0.23.
Claim 20
Dependent Claim
46 words
The formulation of claim 1 or 17, said formulation comprising about 50 weight percent of tylosin admixed with a copolymer derived from about 80 weight percent lactic acid and about 20 weight percent glycolic acid, said copolymer having a viscosity of about 0.18 to about 0.23.
Claim 21
Dependent Claim
47 words
The formulation of claim 1 or 17, said formulation comprising of about 55 weight percent of tylosin admixed with a copolymer derived from about 80 weight percent lactic acid and about 20 weight percent glycolic acid, said copolymer having a viscosity of about 0.18 to about 0.23.
Claim 22
Dependent Claim
24 words
The formulation of claim 1 or 17 in the form of extruded glass-like rods having a diameter of about 2 to about 7 mm.
Claim 23
Dependent Claim
31 words
The formulation of claim 1 or 17 in the form of extruded glass-like rods being ground to uniformity and passed through a seive having mesh of about 60 to about 140.
References Cited (Backward Citations)
No citation records indexed.
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