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US 2020/0046635 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 colon release 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 extruded and spheronized pellets, each extruded and spheronized pellet comprising 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
- b) a coating surrounding each extruded and spheronized pellet, wherein the coating is capable of targeting release of the cholestyramine in the colon;
- 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 the Simulator of the Human Intestinal Microbial Ecosystem (SHIME) model.
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Dependencies are inferred from the claim text.