Galenic composition for low bioavailability medicaments
AssigneeHoffmann-La Roche Inc.
InventorsMartin Kuentz, Dieter Roethlisberger
Life of this patent
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Abstract
A pharmaceutical composition for oral administration of an active compound having a bioavailability of 20% or less. The composition comprises, based on its total weight, from 0.01% to about 15% (w/w) of said active compound molecularly dissolved in the composition, from 30 to 80% (w/w) of an edible lipid matrix and from 1 to 20% (w/w) of an edible emulsifier, the ratio between the dose weight of the active compound and its solubility in the composition being equal to or greater than 0.6 ml. The high percentage of fat (30-80%) enables a considerable increase the amount of the drug that is molecularly dispersed in the dosage form, thus allowing a significant reduction in the number of unit doses that must be taken daily-by patients.
Claims27
A pharmaceutical composition for orally administering an active compound having a bioavailability of 20% or less, which comprises, based on the total weight of the composition, from about 0.01% to about 15% (w/w) of an active compound molecularly dissolved in the composition, from about 30% to about 80% (w/w) of an edible lipid matrix, and from about 1% to about 20% (w/w) of an edible emulsifier, the ratio between the dose weight of the active compound and its solubility in the composition being equal to or greater than 0.6 ml and which comprises a chewable unit dosage form resembling a piece of chocolate.
A process for preparing a pharmaceutical composition comprising a chewable unit dosage form resembling a piece of chocolate, which process comprises:
- (i) selecting an active compound showing a bioavailability of 20% or less, an edible lipid matrix, and an edible emulsifier;
- and
- (ii) mixing, based on the total weight of the composition, from about 0.01% to about 15% (w/w) of an active compound showing a bioavailability of 20% or less, from about 30% to about 80% (w/w) of an edible lipid matrix, and from 1% to about 20%(w/w) of an edible emulsifier, so that the ratio between the dose weight of the active compound and its solubility in the composition is equal to or greater than 0.6 ml.
Dependencies are inferred from the claim text.