Medicament formulation with a controlled release of an active agent
AssigneeBayer Aktiengesellscahft
InventorsHans-Martin Siefert, Patrick Bosché, Heino Stass, Stefan Kettelhoit, Tobias Laich
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Abstract
The invention relates to drug formulations which comprise 1-cyclopropyl-7-([S,S]-2,8-diazabicyclo[4.3.0]non-8-yl)-6-fluoro-1,4-dihydro-8-methoxy-4-oxo-3-quino-lonecarboxylic acid and/or pharmaceutically tolerable salts thereof and/or hydrates thereof as active compound which release the active compound they contain at a defined release rate.
Claims15
A diffusion-controlled pellet drug formulation having controlled release of an active compound, comprising:
- (a) 10-50% by weight of neutral pellet;
- (b) 10-85% by weight of a first coat covering said neutral pellet, said first coat comprising a mixture that is 70-99.5% by weight of the active compound, which is selected from 1-cyclopropyl-7-([S,S]-2,8-diazabicyclo[4.3.0]non-8-yl)-6-fluoro-1,4-dihydro-8-methoxy-4-oxo-3-quinolonecarboxylic acid and pharmaceutically tolerable salts and/or hydrates thereof, and 0.5%-30% by weight of a binder;
- and
- (c) 5-40% by weight of a diffusion coat covering said first coat, said diffusion coat comprising 40-90% by weight of a film former, 0-50% by weight of a pore former and 5-50% by weight of a plasticizer;
- wherein said drug formulation has an average release of active compound of between 80% in 2 hours and 80% in 16 hours and an initial release that is less than 60% of the active compound in the first hour of release.
A diffusion-controlled pellet drug formulation having controlled release of an active compound, comprising:
- (a) 50-95% by weight of a core, said core comprising 70-99.5% by weight of the active compound, selected from 1-cyclopropyl-7-([S,S]-2,8-diazabicyclo[4.3.0]non-8-yl)-6-fluoro-1,4-dihydro-8-methoxy-4-oxo-3-quinolonecarboxylic acid and pharmaceutically tolerable salts and/or hydrates thereof, and 0.5-30% by weight of a binder;
- and
- (b) 5-50% by weight of a diffusion coat covering said core, said diffusion coat comprising 40-90% by weight of a film former, 0-50% by weight of a pore former and 5-50% by weight of a plasticizer,
- wherein said drug formulation has an average release of active compound of between 80% in 2 hours and 80% in 16 hours and an initial release that is less than 60% of the active compound in the first hour of release.
A matrix system drug formulation having controlled release of an active compound, comprising:
- (a) 30-77.3% by weight of the active compound, selected from 1-cyclopropyl-7-([S,S]-2,8-diazabicyclo[4.3.0]non-8-yl)-6-fluoro-1,4-dihydro-8-methoxy-4-oxo-3-quinolonecarboxylic acid and pharmaceutically tolerable salts and/or hydrates thereof,
- (b) 20.9-50% by weight of a water-swellable polymer having a viscosity of at least 15 mPa.s (measured as a 2% strength aqueous solution at 20° C.);
- and
- (c) 0-50% by weight of pharmaceutically acceptable auxiliaries and carriers,
- wherein said drug formulation has an average release of active compound of between 80% in 2 hours and 80% in 16 hours and an initial release that is less than 60% of the active compound in the first hour of release.
Dependencies are inferred from the claim text.