US4525339A
Expired / Lapsed
US
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Enteric coated oral dosage form
Assignee: Hoffmann La Roche Inc
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Filing: 1982-10-15
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Granted: 1985-06-25
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Expires: 2002-10-15
Abstract
Abstract There is presented a method, in the form of a dosage formulation, for transforming substantially orally inactive beta -lactam antibiotics or their pharmaceutically acceptable salts or the esters, ethers, or hydrates of said antibiotics or their salts into orally active compounds by combination of the chosen beta -lactam antibiotic with an enhancer comprising an aliphatic, preferably a C2 to C18, straight- or branched-chain, saturated or unsaturated, fatty acid or an aliphatic, preferably a C2 to C12, straight- or branched-chain, saturated or unsaturated, fatty acid mono-, di- or triglyceride or mixtures thereof, partial or total esters of propylene glycol, polyethylene glycol and carbohydrates of C2 to C12 fatty acids, as well as the pharmaceutically acceptable esters and ethers of said glycerides. The antibiotic and enhancer mixture may be administered orally as a solid dosage form with the beta -lactam antibiotic above or, optionally, with the enhancer protected by an enteric coating.
Inventors
- 👤 Charanjit Behl
- 👤 George Beskid
- 👤 Navnit Shah
- 👤 Jacques Tossounian
- 👤 Joel Unowsky
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-10-29 19:10
CPC Classifications
A; A61; A61K; A61K31/00; A61K31/33; A61K31/335; A61K31/35; A61K47/00; A61K47/06; A61K47/08; A61K47/14; A61K31/395; A61K31/40; A61K31/41; A61K31/425; A61K31/429; A61K31/43; A61K31/54; A61K31/542; A61K31/545; A61K9/00; A61K9/48; A61K9/4891
Claims Analysis
Total Claims: 19
Claim 1
Independent Claim
78 words
An orally administered enteric coated pharmaceutical composition which consists essentially of from about 50 to 500 mg of beta-lactam antibiotic distributed in at least about 33% by weight of an enhancer consisting of a C 2 to C 12 glyceride mixture of at least one glyceride selected from the group consisting essentially of monoglycerides, diglycerides and triglycerids of fatty acids of C 2 to C 12 chain length and mixtures thereof and adjuvants suitable for oral enteric administration.
Claim 2
Dependent Claim
78 words
An orally administered enteric coated pharmaceutical composition which consists essentially of from about 50 to 500 mg of beta-lactam antibiotic distributed in at least about 33% by weight of an enhancer consisting of a C 2 to C 12 glyceride mixture of at least one glyceride selected from the group consisting essentially of monoglycerides, diglycerides and triglycerids of fatty acids of C 2 to C 12 chain length and mixtures thereof and adjuvants suitable for oral enteric administration.
Claim 3
Dependent Claim
21 words
The composition of claim 1, wherein the glyceride or mixture of glycerides is of C 8 to C 12 fatty acids.
Claim 4
Dependent Claim
21 words
The composition of claim 2, wherein the glyceride mixture is between about 33° to about 98% by weight of the composition.
Claim 5
Dependent Claim
17 words
The composition of claim 3, wherein the glyceride mixture is about 89% by weight of the composition.
Claim 6
Independent Claim
99 words
A method of beta-lactam antibiotic treatment which comprises orally administering to a warm blooded animal a readily absorbable enteric coated pharmaceutical composition which consists essentially of from about 50 to 500 mg of a beta-lactam antibiotic distributed in at least about 33% by weight of an enhancer consisting of an absorption enhancing amount of a C 2 to C 12 glyceride mixture of at least one glyceride selected from the group consisting essentially of monoglycerides diglycerides and triglycerids of fatty acids of C 2 to C 12 chain length and mixtures thereof and adjuvants suitable for oral enteric administration.
Claim 7
Independent Claim
99 words
A method of beta-lactam antibiotic treatment which comprises orally administering to a warm blooded animal a readily absorbable enteric coated pharmaceutical composition which consists essentially of from about 50 to 500 mg of a beta-lactam antibiotic distributed in at least about 33% by weight of an enhancer consisting of an absorption enhancing amount of a C 2 to C 12 glyceride mixture of at least one glyceride selected from the group consisting essentially of monoglycerides diglycerides and triglycerids of fatty acids of C 2 to C 12 chain length and mixtures thereof and adjuvants suitable for oral enteric administration.
Claim 8
Dependent Claim
21 words
The composition of claim 5, wherein the glyceride or mixture of glyceride is of C 8 to C 12 fatty acids.
Claim 9
Dependent Claim
21 words
The composition of claim 6, wherein the glyceride mixture is between about 33% to about 98% by weight of the composition.
Claim 10
Dependent Claim
17 words
The composition of claim 7, wherein the glyceride mixture is about 89% by weight of the composition.
Claim 11
Dependent Claim
17 words
The composition of claim 1 wherein the dosage form is an enteric coated capsule, microcapsule or beadlet.
Claim 12
Dependent Claim
12 words
The composition of claim 1 wherein the dosage form is a tablet.
Claim 13
Dependent Claim
50 words
An absorbable pharmaceutical composition which comprises a therapeutically effective amount of ceftriaxone distributed in a vehicle comprising an absorption enhancing amount of a C 8 to C 10 mixture of mono- and diglycerides wherein the monoglyceride content may be about 70% or about 90% respectivley, said composition being enterally administered.
Claim 14
Dependent Claim
50 words
An absorbable pharmaceutical composition which comprises a therapeutically effective amount of ceftriaxone distributed in a vehicle comprising an absorption enhancing amount of a C 8 to C 10 mixture of mono- and diglycerides wherein the monoglyceride content may be about 70% or about 90% respectivley, said composition being enterally administered.
Claim 15
Dependent Claim
17 words
The method of claim 5 wherein the dosage form is an enteric coated capsule, microcapsule or beadlet.
Claim 16
Dependent Claim
14 words
The method of claim 5 wherein the dosage form is an enteric coated tablet.
Claim 17
Independent Claim
82 words
A method of β-lactam antibiotic treatment which comprises orally administering to a human being a readily absorbable enteric coated pharmaceutical composition which comprises a therapeutically effective amount of a β-lactam distributed in a C 8 to C 10 mixture of mono- or diglycerides wherein the monoglyceride is present as about 70% or about 90% of the mixture in an enteric coated entity selected from an enteric coated capsule or tablet or a capsule having enterically coated microencapsulated ceftriaxone in said glyceride mixture.
Claim 18
Independent Claim
82 words
A method of β-lactam antibiotic treatment which comprises orally administering to a human being a readily absorbable enteric coated pharmaceutical composition which comprises a therapeutically effective amount of a β-lactam distributed in a C 8 to C 10 mixture of mono- or diglycerides wherein the monoglyceride is present as about 70% or about 90% of the mixture in an enteric coated entity selected from an enteric coated capsule or tablet or a capsule having enterically coated microencapsulated ceftriaxone in said glyceride mixture.
Claim 19
Dependent Claim
34 words
The composition of claim 9 wherein the vehicle is a C 8 to C 10 mixture of mono- or diglycerides wherein the monoglyceride is present as about 70% or about 90% of the mixture.
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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) | 1988-06-24 | 1988-12-24 | 1989-06-25 | $2000.00 | Window Closed / Lapsed |
| 7.5 Years (Year 8) | 1992-06-24 | 1992-12-24 | 1993-06-25 | $3760.00 | Window Closed / Lapsed |
| 11.5 Years (Year 12) | 1996-06-24 | 1996-12-24 | 1997-06-25 | $7700.00 | Window Closed / Lapsed |