Patent application EP16173539A (EP), filed 2016-06-08
Publication number: EP3254674A1
Title: PHARMACEUTICAL COMPOSITIONS OF BETRIXABAN MALEATE
Abstract: The present invention relates to a solid dispersion comprising amorphous betrixaban maleate and a pharmaceutically acceptable carrier selected from the group consisting of organic polymers and silicon-based inorganic compounds, and to a process for preparing the same. It also relates to a pharmaceutical composition comprising said solid dispersion and one or more pharmaceutically acceptable excipients. The invention also concerns the use of said pharmaceutical compositions as a medicament, in particular for the prevention and the treatment of disease conditions characterized by undesired thrombosis.
IPC codes: A61K  31/    44            A I
A61K   9/    14            A I
A61P   7/    02            A I
Claims: number: 1
text: A solid dispersion comprising amorphous betrixaban maleate and a pharmaceutically acceptable carrier selected from the group consisting of organic polymers, silicon-based inorganic compounds and mixtures thereof.
number: 2
text: The solid dispersion according to claim 1, wherein in the adsorption-desorption isotherm of the pharmaceutically acceptable carrier, the mass difference Δm(desorption) at 75 % relative humidity and 25°C is greater than or equal to the mass difference Δm(adsorption) at 75 % relative humidity and 25°C, determined according to dynamic vapour sorption measurement.
number: 3
text: The solid dispersion according to claim 1 or 2, wherein the pharmaceutically acceptable carrier is an organic polymer.
number: 4
text: The solid dispersion according to claim 1 to 3, wherein the organic polymer is a hydrophilic organic polymer.
number: 5
text: The solid dispersion according to claim 1 or 4, wherein the organic polymer is a cellulose derivative selected from the group consisting of alkylcellulose, preferably methylcellulose, ethylcellulose, or propylcellulose; hydroxyalkylcellulose, preferably hydroxymethylcellulose, hydroxyethylcellulose, or hydroxypropyl cellulose; hydroxyalkyl alkylcellulose, preferably hydroxyethyl methylcellulose (HEMC), or hydroxypropyl methylcellulose (HPMC); carboxyalkyl cellulose, preferably carboxymethylcellulose (CMC), carboxymethyl hydroxyethylcellulose (CMHEC), hydroxyethyl carboxymethylcellulose (HECMC); sodium carboxymethylcellulose, cellulose acetate phthalate (CAP), hydroxypropyl methylcellulose acetate (HPMCA), hydroxypropyl methylcellulose phthalate (HPMCP), hydroxypropyl methylcellulose acetate succinate (HPMCAS), and a mixture of two or more thereof.
number: 6
text: The solid dispersion according to claims 1 to 5, wherein the organic polymer is hydroxypropyl methylcellulose.
number: 7
text: The solid dispersion according to claim 1 or 2, wherein the pharmaceutically acceptable carrier is a silicon-based inorganic compound.
number: 8
text: The solid dispersion according to claim 1, 2 or 7, wherein the silicon-based inorganic compound is selected from the group consisting of silica, silicates, and a combination of two or more thereof.
number: 9
text: The solid dispersion according to claim 1, 2, 7 or 8, wherein the silicon-based inorganic compound has a pH in the range of from 6.0 to 9.0, preferably in the range of from 6.3 to 8.5, more preferably in the range of from 6.6 to 8.0.
number: 10
text: The solid dispersion according to any of the preceding claims, wherein the weight ratio of betrixaban maleate and the pharmaceutically acceptable carrier is from 1:1 to 1:10.
number: 11
text: The solid dispersion according to any one of the preceding claims comprising at most 20%, preferably at most 10%, more preferably at most 5%, even more preferably at most 2% and most preferably at most 1% by weight of any crystalline form of betrixaban maleate.
number: 12
text: A pharmaceutical composition comprising a solid dispersion according to any one of the preceding claims and one or more pharmaceutically acceptable excipients.
number: 13
text: A process for the preparation of the solid dispersion of claims 1 to 11 comprising the steps of
number: 14
text: A solid dispersion according to claims 1 to 11 or a pharmaceutical composition according to claim 12 for use as a medicament.
number: 15
text: A solid dispersion according to claims 1 to 11 or a pharmaceutical composition according to claim 12 for use in the treatment of disease conditions characterized by undesired thrombosis.
Office action: search_report, dated 2017-12-13
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Final disposition: pending (2017-12-13)