Patent ID: 11872229
Assignee: PRINCIPIA BIOPHARMA INC.
Field: Pharmaceuticals (Chemistry)
Classification: CPC A | IPC A

Claim 0:
1. A modified release solid oral dosage form comprising:
(a) a core composition comprising a (E) isomer, a (Z) isomer, a mixture of (E) and (Z) isomers of (R)-2-[3-[4-amino-3-(2-fluoro-4-phenoxy-phenyl)pyrazolo[3,4-d]pyrimidin-1-yl]piperidine-1-carbonyl]-4-methyl-4-[4-(oxetan-3-yl)piperazin-1-yl]pent-2-enenitrile, (S)-2-[3-[4-amino-3-(2-fluoro-4-phenoxy-phenyl)pyrazolo[3,4-d]pyrimidin-1-yl]piperidine-1-carbonyl]-4-methyl-4-[4-(oxetan-3-yl)piperazin-1-yl]pent-2-enenitrile, or a mixture of (R) and (S) isomers of 2-[3-[4-amino-3-(2-fluoro-4-phenoxy-phenyl)pyrazolo[3,4-d]pyrimidin-1-yl]piperidine-1-carbonyl]-4-methyl-4-[4-(oxetan-3-yl)piperazin-1-yl]pent-2-enenitrile (Compound I) having the structure:, where *C is a stereochemical center, or a pharmaceutically acceptable salt thereof;
wherein the core composition comprises by weight:
about 6% to about 20% of Compound (I) or a pharmaceutically acceptable salt thereof;
about 34% to about 72% of microcrystalline cellulose;
about 5% to about 25% mannitol;
about 0% to about 20% of hydroxypropyl methyl cellulose;
about 0.5% to about 1.5% of crosslinked homopolymer of N-vinyl-2-pyrrolidone; and
about 0.5% to about 1.5% of sodium stearyl fumarate;
(b) a sub-coating layer coating the core composition, the sub-coating layer comprising a polyvinyl alcohol and/or a hydroxypropyl methyl cellulose; and
(c) an enteric coating layer encapsulating the sub-coating layer and the core composition, the enteric coating layer comprising at least one polymer selected from an acrylic/methacrylic/ethacrylic acid homopolymer and copolymers thereof, a cellulose derivative, and a polyvinylpyrrolidone.