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US 2020/0046636 A1Published application
Oral cholestyramine formulation and use thereof
AssigneeAlbireo AB
InventorsPer-Göran Gillberg, Nils Ove Gustafsson, Nils-Olof Lindberg, Jessica Elversson
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Abstract
The invention relates to an oral formulation for targeted delivery of cholestyramine to the colon, comprising a plurality of cholestyramine pellets that are coated with a diffusion-controlled inner coating and an enteric outer coating. The invention also relates to the use of this formulation in the treatment of bile acid malabsorption.
Claims26
An oral dosage form comprising:
- a) a plurality of pellets, each pellet comprising at least 70% w/w cholestyramine and
- i. a combination of at least 6% w/w of a vinylpyrrolidone-based polymer and at least 2% w/w of an acrylate copolymer;
- or
- ii. a combination of at least 5% w/w of a vinvlpyrrolidone-based polymer and at least 3% w/w of an acrylate copolymer;
- or
- iii. 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;
- b) a diffusion-controlled inner coating surrounding each pellet;
- and
- c) an enteric outer coating;
- wherein the oral dosage form exhibits less than about 30% sequestration of cholic acid, chenodeoxycholic acid, and deoxycholic acid after 2 hours in small intestinal incubations (“SI-2”) as measured in a Simulator of the Human Intestinal Microbial Ecosystem (SHIME) model.
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Dependencies are inferred from the claim text.