Formulations of 3-(6-(1-(2,2-difluorobenzo[d][1,3]dioxol-5-yl) cyclopropanecarboxamido)-3-methylpyridin-2-yl)benzoic acid
Inventors
Assignees
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Publication Number
US-12508231-B2
Publication Date
2025-12-30
Expiration Date
Abstract
A pharmaceutical composition comprising Compound 1, (3-(6-(1-(2,2-difluorobenzo[d][1,3]dioxol-5-yl) cyclopropanecarboxamido)-3-methylpyridin-2-yl)benzoic acid), and at least one excipient selected from: a filler, a disintegrant, a surfactant, a binder, and a lubricant, the composition being suitable for oral administration to a patient in need thereof to treat a CFTR mediated disease such as Cystic Fibrosis. Processes of preparing pharmaceutical compositions comprising Compound 1 are also disclosed.
Core Innovation
The disclosure concerns an oral tablet comprising Compound 1 Form I and a continuous process for preparing the tablet using continuous twin-screw wet granulation. The formulation comprises Compound 1 Form I with specified excipient categories including microcrystalline cellulose, croscarmellose sodium, sodium lauryl sulfate, polyvinylpyrrolidone, and magnesium stearate within defined composition ranges, followed by optional tablet coating. [procedural detail omitted for safety]
The continuous twin-screw granulation process utilizes a granulation fluid containing both a surfactant and a binder to improve wettability and enable controlled processing. The disclosure details solid-form characterization across different loss-on-drying levels, tablet dissolution profiles, hardness, and friability targets. The resulting tablet composition is directed to treating cystic fibrosis and other CFTR-mediated disorders, including combination use with CFTR modulators.
Claims Coverage
The claim coverage includes three inventive features directed to an independent claim for preparing a tablet containing Compound 1 Form I.
Continuous tablet preparation
The independent claim provides a continuous twin-screw granulation process for preparing a tablet comprising Compound 1 Form I. [procedural detail omitted for safety]
Specified tablet composition
The tablet comprises Compound 1 Form I with microcrystalline cellulose as filler, croscarmellose sodium as disintegrant, sodium lauryl sulfate as surfactant, polyvinylpyrrolidone as binder, and magnesium stearate as lubricant within specified composition ranges.
Optional tablet coating
The claimed process provides for optionally coating the prepared tablet.
The independent claim combines continuous twin-screw granulation with defined tablet composition requirements and optional coating to cover preparation of a tablet comprising Compound 1 Form I, while dependent claims further address solid-form characterization, tablet performance, and treatment of cystic fibrosis in patients having a ΔF508 CFTR mutation.
Stated Advantages
The continuous twin-screw granulation process utilizing granulation fluid containing both a surfactant and a binder improves wettability, enables controlled processing, and supports product quality.
Documented Applications
Treatment of cystic fibrosis and other CFTR-mediated disorders, including treatment of patients with specified CFTR mutation status such as a ΔF508 CFTR mutation.
Combination therapy with CFTR modulators, including ivacaftor, and other adjunct therapies.
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