Pharmaceutical formulations of a Bruton's tyrosine kinase inhibitor
Inventors
Chong, Ching W. • Kuehl, Robert • Tan, Heow • ATLURI, Harisha
Assignees
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Publication Number
US-10828259-B2
Publication Date
2020-11-10
Expiration Date
Abstract
Described herein are pharmaceutical formulations of Bruton's tyrosine kinase (Btk) inhibitor 1-((R)-3-(4-amino-3-(4-phenoxyphenyl)-1H-pyrazolo[3,4-d]pyrimidin-1-yl)piperidin-1-yl)prop-2-en-1-one. Also disclosed are methods of using the Btk inhibitor, alone or in combination with other therapeutic agents, for the treatment of autoimmune diseases or conditions, heteroimmune diseases or conditions, cancer, including lymphoma, and inflammatory diseases or conditions.
Core Innovation
The invention relates to a solid tablet formulation comprising ibrutinib and pharmaceutically acceptable excipients, wherein the ibrutinib is a compound having the structure of Compound 1. The formulation includes about 60% w/w to about 75% w/w of the ibrutinib and excipients selected from diluents, disintegrating agents, binders, colloidal silicon dioxide, and magnesium stearate.
The formulation specifies excipient classes and selected representatives, including diluents such as lactose, sucrose, dextrose, dextrates, maltodextrin, mannitol, xylitol, sorbitol, cyclodextrins, calcium phosphate, calcium sulfate, starches, modified starches, cellulose, microcrystalline cellulose, microcellulose, and talc. It further specifies disintegrating agents such as croscarmellose, croscarmellose sodium, and other listed options, and binders such as hydroxypropyl cellulose and polyvinylpyrrolidone.
A particular aspect of the invention provides solid tablet formulations with intragranular and extragranular excipients, where intragranular excipients comprise microcrystalline cellulose and polyvinylpyrrolidone and extragranular excipients comprise croscarmellose sodium, colloidal silicon dioxide, and magnesium stearate. The disclosed embodiments address high-load oral tablet formulations of ibrutinib, including the stated high ibrutinib loading range and defined excipient sets.
Claims Coverage
The independent claims are 1, 10, and 24. Across these claims, the inventive coverage centers on high ibrutinib loading in a solid tablet, specified excipient categories and representative excipients, quantitative excipient amount ranges, and a specific intragranular/extragranular excipient separation with defined excipient sets.
High-load ibrutinib solid tablet with defined excipient categories
A solid tablet formulation comprising ibrutinib (Compound 1) with about 60% w/w to about 75% w/w ibrutinib, where the excipients comprise one or more diluents from a defined group, one or more disintegrating agents from a defined group, one or more binders selected from hydroxypropyl cellulose and polyvinylpyrrolidone, and additionally colloidal silicon dioxide and magnesium stearate.
Defined high-load ranges paired with quantitative excipient amount ranges
A solid tablet formulation comprising ibrutinib (Compound 1) with about 60% w/w to about 75% w/w ibrutinib, where the excipients comprise microcrystalline cellulose, croscarmellose sodium, crospovidone, polyvinylpyrrolidone, sodium lauryl sulfate, colloidal silicon dioxide, and magnesium stearate, each present in specified weight-percent ranges.
Intragranular/extragranular excipient split with defined intragranular and extragranular sets
A solid tablet formulation comprising ibrutinib (Compound 1) with about 60% w/w to about 75% w/w of the ibrutinib, wherein the excipients comprise intragranular and extragranular excipients, the intragranular excipients comprise microcrystalline cellulose and polyvinylpyrrolidone, and the extragranular excipients comprise croscarmellose sodium, colloidal silicon dioxide, and magnesium stearate.
The claim set covers high-load ibrutinib tablets based on the Compound 1 structure, with excipients selected from specified categories and representatives, quantitative excipient amount constraints, and a defined intragranular/extragranular excipient arrangement.
Stated Advantages
Not explicitly described in patent.
Documented Applications
Not explicitly described in patent.
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