Formulations for poorly permeable active pharmaceutical ingredients
AssigneeSolvay Phamaceuticals GmbH
InventorsJan P. Moschwitzer, Aldo V. Ket, Heike Dinter-Heidorn
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Abstract
The present invention relates to a pharmaceutical oral dosage form containing a poorly permeable active pharmaceutical ingredient and at least one permeability improving substance, wherein the permeability improving substance is thermostably embedded in a water-soluble matrix of a water soluble carrier, and to thermostable formulations which can be used to improve bioavailability.
Claims16
A thermostable solid composition comprising at least one permeability improving substance embedded in a water soluble matrix, wherein the sum of the amount of said permeability improving substance or mixture of permeability improving substances and said water soluble matrix is at least 80% w/w of the total dry material in the composition, with the proviso that said thermostable solid composition does not contain an active pharmaceutical ingredient.
A process of preparing a thermostable solid composition comprising at least one permeability improving substance embedded in a water soluble matrix, said process comprising:
- a) dissolving or dispersing at least one permeability improving substance in water to form a mixture;
- b) dissolving water soluble matrix forming material in the mixture obtained in a) or adding a solution of water soluble matrix forming material in water to the mixture obtained in a);
- c) optionally adding one or more auxiliary materials to the mixture obtained in a) or b);
- and
- d) drying the mixture obtained in b) or c);
- wherein the sum of the amount of said permeability improving substance or mixture of permeability improving substances and said water soluble matrix is at least 80% w/w of the total dry material of the composition.
A process of preparing a thermostable solid composition comprising at least one permeability improving substance embedded in a water soluble matrix, said process comprising:
- a) dissolving or dispersing water soluble matrix forming material in water to form a mixture;
- b) dissolving or dispersing at least one permeability improving substance in the mixture obtained in a), or adding a solution or dispersion of the at least one permeability improving substance in water to the mixture obtained in a);
- c) optionally adding one or more auxiliary materials to the mixture obtained in a or b);
- and
- d) drying the mixture obtained in b or c);
- wherein the sum of the amount of said permeability improving substance or mixture of permeability improving substances and said water soluble matrix is at least 80% w/w of the total dry material of the composition.
Dependencies are inferred from the claim text.