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US3867538A Expired / Lapsed US ⏱️ 0.0 years remaining

Enzyme-resistant compositions containing penicillin in combination with 6-apa

Assignee: ER Squibb and Sons LLC
•
Filing: 1969-10-29
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Granted: 1975-02-18
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Expires: 1989-10-29
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Abstract

Abstract This invention has for its objects the provision of compositions of 6-APA with penicillins since it has been found that 6-APA protects penicillins from the action of Beta -lactamases produced by many organisms which destroy many types of penicillins. The 6-APA is provided in a ratio of 1 gram of 6-APA to 20 grams of a given penicillin up to 200 grams of 6-APA to one gram of penicillin. The penicillin is provided in standard dosages for the particular penicillin employed, and in the usual dosage forms. By penicillin is meant that any acyl derivative of 6-aminopenicillanic acid, including salts, esters and amides thereof. By 6-APA is meant 6-aminopenicillanic acid of which the salts, esters and amides thereof may also be employed.

Inventors

  • 👤 Richard Donovick

Bibliographic Details

Application Number —
Jurisdiction US
Data Source google_patents
Last Synchronized 2026-11-03 05:14
CPC Classifications
A; A61; A61K; A61K31/00; A61K31/33; A61K31/395; A61K31/41; A61K31/425; A61K31/429; A61K31/43

Claims Analysis

Total Claims: 12
Claim 1
Independent Claim 76 words
A METHOD OF PROTECTING PENICILLIN FROM THE ACTION OF MICROORGANISMS WHICH PRODUCE b-LACTAMASE ENZYMES WHICH DESTROY PENICILLIN WHICH COMPRISES ADMINISTERING A STANDARD DOSAGE FROM THE PENICILLIN TOOGETHER WITH AN AMOUNT OF FREE 6-AMINOPENICILLANIC ACID OR PHARMACEUTICALLY ACCEPTABLE SALTS, ESTERS AND AMIDES THEREOF, THE AMOUNT BEING EFFECTIVE TO PREVENT DESTRUCTION OF THE PENICILLIN BY B-LACTAMASE ENZYMES, THE AMOUNT OF PENICILLIN IN THE DOSAGE FORM BEING FROM ABOUT 0.01 TO ABOUT 1.5 GRAMS PER KILOGRAM OF BODY WEIGHT.
Claim 2
Independent Claim 76 words
A METHOD OF PROTECTING PENICILLIN FROM THE ACTION OF MICROORGANISMS WHICH PRODUCE b-LACTAMASE ENZYMES WHICH DESTROY PENICILLIN WHICH COMPRISES ADMINISTERING A STANDARD DOSAGE FROM THE PENICILLIN TOOGETHER WITH AN AMOUNT OF FREE 6-AMINOPENICILLANIC ACID OR PHARMACEUTICALLY ACCEPTABLE SALTS, ESTERS AND AMIDES THEREOF, THE AMOUNT BEING EFFECTIVE TO PREVENT DESTRUCTION OF THE PENICILLIN BY B-LACTAMASE ENZYMES, THE AMOUNT OF PENICILLIN IN THE DOSAGE FORM BEING FROM ABOUT 0.01 TO ABOUT 1.5 GRAMS PER KILOGRAM OF BODY WEIGHT.
Claim 3
Dependent Claim 13 words
A method according to claim 1 wherein the dosage form is a tablet.
Claim 4
Dependent Claim 13 words
A method according to claim 1 wherein the dosage form is a lozenge.
Claim 5
Dependent Claim 13 words
A method according to claim 1 wherein the dosage form is a solution.
Claim 6
Dependent Claim 13 words
A method according to claim 1 wherein the dosage form is a suspension.
Claim 7
Dependent Claim 78 words
A composition comprising a standard dosage form of penicillin together with an amount of free 6-aminopenicillanic acid, or pharmaceutically acceptable salts, esters or amides thereof wherein the esters or amides are formed by reaction of the carboxyl group of the acid, the amount of 6-aminopenicillanic acid in the composition being effective to prevent destruction of the penicillin by Beta -lactamase enzymes, the amount of 6-aminopenicillanic acid to penicillin in the dosage form being from about 1-20 to 200-1.
Claim 8
Dependent Claim 78 words
A composition comprising a standard dosage form of penicillin together with an amount of free 6-aminopenicillanic acid, or pharmaceutically acceptable salts, esters or amides thereof wherein the esters or amides are formed by reaction of the carboxyl group of the acid, the amount of 6-aminopenicillanic acid in the composition being effective to prevent destruction of the penicillin by Beta -lactamase enzymes, the amount of 6-aminopenicillanic acid to penicillin in the dosage form being from about 1-20 to 200-1.
Claim 9
Dependent Claim 17 words
A standard dosage form of penicillin according to claim 6 wherein the dosage form is a tablet.
Claim 10
Dependent Claim 17 words
A standard dosage form of penicillin according to claim 6 wherein the dosage form is a lozenge.
Claim 11
Dependent Claim 17 words
A standard dosage form of penicillin according to claim 6 wherein the dosage form is a solution.
Claim 12
Dependent Claim 17 words
A standard dosage form of penicillin according to claim 6 wherein the dosage form is a suspension.

References Cited (Backward Citations)

US3245983A Cited
US3035046A Cited
US3040032A Cited
US3157639A Cited
US3225033A Cited
US3035047A Cited

USPTO Annuity & Maintenance Windows

Annuity Stage Window Opens Payment Deadline Surcharge Period Until Estimated Fee Status
3.5 Years (Year 4) 1978-02-17 1978-08-19 1979-02-18 $2000.00 Window Closed / Lapsed
7.5 Years (Year 8) 1982-02-17 1982-08-19 1983-02-18 $3760.00 Window Closed / Lapsed
11.5 Years (Year 12) 1986-02-17 1986-08-19 1987-02-18 $7700.00 Window Closed / Lapsed

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