Cholestyramine pellets and methods for preparation thereof
AssigneeAlbireo AB
InventorsPer-Göran Gillberg, Nils Ove Gustafsson, Nils-Olof Lindberg, Jessica Elversson
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Abstract
The invention relates to small cholestyramine pellets that can be prepared by extrusion. The pellets have a high cholestyramine loading and are stable enough to be coated with one or more coating layers. The invention also relates to a process for the preparation of such pellets and to a multiparticulate drug delivery system comprising such pellets.
Claims18
A population of extruded and spheronized pellets, each extruded and spheronized pellet comprising at least 70% w/w cholestyramine and
- i. at least 7% w/w of a vinylpyrrolidone-based polymer;
- or
- ii. a combination of at least 6% w/w of a vinylpyrrolidone-based polymer and at least 2% w/w of an acrylate copolymer;
- or
- iii. a combination of at least 5% w/w of a vinylpyrrolidone-based polymer and at least 3% w/w of an acrylate copolymer;
- or
- iv. a combination of at least 6% w/w of a vinylpyrrolidone-based polymer, at least 1% w/w of an acrylate copolymer and at least 10% w/w microcrystalline cellulose;
- and wherein the vinylpyrrolidone-based polymer is selected from the group consisting of copovidone, povidone, and combinations thereof;
- wherein the pellets exhibits a friability of less than 2.1% as measured using the European Pharmacopoeia 8.0, test 2.9.7.
A process for the preparation of a population of extruded and spheronized pellets
- wherein each extruded and spheronized pellet comprises at least 70% w/w cholestyramine and
- i. at least 7% w/w of a vinylpyrrolidone-based polymer;
- or
- ii. a combination of at least 6% w/w of a vinylpyrrolidone-based polymer and at least 2% w/w of an acrylate copolymer;
- or
- iii. a combination of at least 5% w/w of a vinylpyrrolidone-based polymer and at least 3% w/w of an acrylate copolymer;
- or
- iv. a combination of at least 6% w/w of a vinylpyrrolidone-based polymer, at least 1% w/w of an acrylate copolymer and at least 10% w/w microcrystalline cellulose;
- and wherein the vinylpyrrolidone-based polymer is selected from the group consisting of copovidone, povidone, and combinations thereof;
- the process comprising the steps of:
- i) mixing the dry ingredients;
- ii) adding water, and optionally the acrylate copolymer, to obtain a wet mass;
- iii) extruding the wet mass;
- iv) spheronizing the extrudate;
- and
- v) drying the obtained extruded and spheronized pellets;
- wherein the pellets exhibit a friability of less than 2.1% as measured using the European Pharmacopoeia 8.0, test 2.9.7.
A formulation comprising a plurality of extruded and spheronized cholestyramine pellets, wherein each extruded and spheronized pellet comprises at least 70% w/w cholestyramine and
- i. at least 7% w/w of a vinylpyrrolidone-based polymer;
- or
- ii. a combination of at least 6% w/w of a vinylpyrrolidone-based polymer and at least 2% w/w of an acrylate copolymer;
- or
- iii. a combination of at least 5% w/w of a vinylpyrrolidone-based polymer and at least 3% w/w of an acrylate copolymer;
- or
- iv. a combination of at least 6% w/w of a vinylpyrrolidone-based polymer, at least 1% w/w of an acrylate copolymer and at least 10% w/w microcrystalline cellulose;
- and wherein the vinylpyrrolidone-based polymer is selected from the group consisting of copovidone, povidone, and combinations thereof;
- wherein the pellets exhibit a friability of less than 2.1% as measured using the European Pharmacopoeia 8.0, test 2.9.7.
A method for treating bile acid malabsorption or bile acid diarrhoea in a patient in need thereof, the method comprising administering to the patient a therapeutically effective amount of an oral formulation comprising:
- a plurality of extruded and spheronized pellets, each extruded and spheronized pellet comprising at least 70% w/w cholestyramine and
- i. at least 7% w/w of a vinylpyrrolidone-based polymer;
- or
- ii. a combination of at least 6% w/w of a vinylpyrrolidone-based polymer and at least 2% w/w of an acrylate copolymer;
- or
- iii. a combination of at least 5% w/w of a vinylpyrrolidone-based polymer and at least 3% w/w of an acrylate copolymer;
- or
- iv. a combination of at least 6% w/w of a vinylpyrrolidone-based polymer, at least 1% w/w of an acrylate copolymer and at least 10% w/w microcrystalline cellulose;
- and wherein the vinylpyrrolidone-based polymer is selected from the group consisting of copovidone, povidone, and combinations thereof;
- wherein the pellets exhibit a friability of less than 2.1% as measured using the European Pharmacopoeia 8.0, test 2.9.7.
Dependencies are inferred from the claim text.