Drug – bio-affecting and body treating compositions – Preparations characterized by special physical form – Matrices
Patent
1997-10-02
1999-06-08
Page, Thurman K.
Drug, bio-affecting and body treating compositions
Preparations characterized by special physical form
Matrices
424464, 424469, 424470, 424486, 424487, 424489, 424490, 514964, 514965, A61K 926
Patent
active
059103221
DESCRIPTION:
BRIEF SUMMARY
This application claims benefit of U.K. application number 9416600.6 filed Aug. 17, 1994.
This invention relates to pharmaceutical formulations for oral administration, comprising an antibiotic and a .beta.-lactamase inhibitor.
Oral formulations of this type are known, but generally need to be administered three times daily. It is desirable to produce such a formulation in a delayed or sustained release form which may be suitable for less frequent administration. A particularly effective .beta.-lactamase inhibitor is the known compound clavulanic acid and its derivatives (hereinafter collectively termed "clavulanate" unless otherwise specifically identified), especially the potassium salt of clavulanic acid.
The invention therefore provides a pharmaceutical tablet formulation, comprising:
a matrix which comprises a .beta.-lactam antibiotic optionally in combination with a .beta.-lactamase inhibitor,
and dispersed within said matrix, granules in a delayed release form ("delayed release granules") which comprise a .beta.-lactam antibiotic optionally in combination with a .beta.-lactamase inhibitor, the overall tablet formulation including a .beta.-lactam antibiotic and a .beta.-lactamase inhibitor.
The matrix preferably includes a .beta.-lactamase inhibitor.
The granules may optionally also include a .beta.-lactamase inhibitor in combination with the .beta.-lactam antibiotic.
The matrix may also include dispersed within it granules ("rapid release granules"), in a form which release their content more rapidly than the delayed-release granules, which comprise a .beta.-lactam antibiotic, optionally in combination with a .beta.-lactamase inhibitor.
Preferred .beta.-lactam antibiotics are penicillins and cephalosporins, in particular amoxycillin, for example in the form of amoxycillin trihydrate. A preferred .beta.-lactamase inhibitor is clavulanate, particularly potassium clavulanate. In the matrix and those granules which contain a .beta.-lactamase inhibitor the ratio antibiotic:.beta.-lactamase inhibitor may vary independently between wide limits, in the case of amoxycillin:clavulanate for example varying between 1:1 to 30:1, for example amoxycillin:clavulanate between 1:1 to 12:1, e.g 2:1, 3:1, 4:1, 5:1, 6:1, 7:1 or 8:1 inclusive expressed as the equivalent weight ratios of the parent free acids. In the overall tablet formulation the ratio antibiotic:.beta.-lactamase inhibitor may also vary between similarly broad limits, for example between: 1 to 30:1, for example between: 1 to 12:1, e.g 2:1, 3:1, 4:1, 5:1, 6:1, 7:1 or 8:1 inclusive.
The matrix may suitably comprise a mixture of amoxycillin and potassium clavulanate in a ratio amoxycillin:clavulanate between 2:1 to 8:1, for example between 2:1 and 4:1 inclusive.
In one form of the tablet formulation of the invention, the tablet has a matrix which comprises amoxycillin and clavulanate, dispersed within which are delayed release granules which comprise amoxycillin and clavulanate. These granules may suitably comprise amoxycillin and potassium clavulanate in a ratio amoxycillin:clavulanate between 2:1 to 8:1 inclusive, for example around 4:1+10%.
In this first form of the tablet the overall distribution of the antibiotic and .beta.-lactamase inhibitor between the matrix:granules may independently suitably vary between 2.5:1 to 1:2.5. Suitably the distribution of matrix amoxycillin:granule amoxycillin is around 1:1.5+10%, and the distribution of matrix clavulanate:granule clavulanate is around 1.5:1+10%.
In a second form of the tablet formulation of the invention, the tablet has a matrix which comprises amoxycillin and clavulanate, dispersed within which are delayed release granules which comprise amoxycillin, and rapid release granules which comprise amoxycillin.
In this second form of the tablet the overall distribution of the amoxycillin between the matrix plus rapid release granules:delayed release granules may vary between 2.5:1 and 1:2.5. Suitably the distribution may be around 1:1.5+10%. Suitably the distribution of amoxycillin between rapid release gran
REFERENCES:
patent: 4173626 (1979-11-01), Demski et al.
patent: 4223006 (1980-09-01), Taskis
Grimmett Francis Walter
Hartnell Michael William
Rivett Ernest Lionel Gilbert
Kinzig Charles M.
Page Thurman K.
Seidleck Brian K.
SmithKline Beecham p.l.c.
Williams Janice E.
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