Method for prophylaxis and/or treatment of thromboembolism
AssigneeAstraZeneca AB
InventorsSigbrit Forsman, Christer Karlsson, Magnus Karlsson
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Abstract
A new oral IR formulation in solid form for a low molecular weight thrombin inhibitor having pH dependant dissolution, characterized in that the formulation comprises a filler or a combination of fillers having disintegrant properties in an amount higher than 35% W/W of the formulation.
Claims12
An oral immediate release formulation in solid form of a low molecular weight peptide-based thrombin inhibitor having pH dependent solubility c h a r a c t e r i z e d in that the formulation comprises a filler or a combination of fillers having disintegrant properties in an amount higher than 35% w/w of the formulation, selected from the group consisting of a cellulose per se and a starch per se.
An oral formulation according to any of the preceding claims, characterized in that the thrombin inhibitor is having a particle size of less than 300 μm, preferably less than 150 μm and a preferred mean particle size less than 80 μm.
An oral formulation according to claims any of the preceding claims c ha r a c t e r i z e d in that it comprises a combination of microcrystalline cellulose and mannitol.
An oral formulation according to any of the preceding claims wherein the thrombin inhibitor is glycine, N-[1-cyclohexyl-2-[2-[[[[4-[(hydroxyimino)aminomethyl]-phenyl]methyl]amino]carbonyl]-1-azetidinyl]-2-oxoethyl]-, ethyl ester, [S-(R*, S*)]-).
An oral formulation according to any of the preceding claims for use in therapy.
Use of a filler selected from the group consisting of a cellulose derivative, and a starch derivative, optionally a sugar, a disintegrant, a binder and/or a lubricant in the preparation of an oral immediate release formulation containing a low molecular weight peptide-based thrombin inhibitor having pH dependent solubility.
Dependencies are inferred from the claim text.