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Publication Number
US-11504331-B2
Publication Date
2022-11-22
Expiration Date
Abstract
The present invention relates to a process to prepare solid pharmaceutical forms comprising a quantity of mesalazine comprised between 75 and 95%, i.e. between 1000 and 1600 mg of drug per dosage unit. Furthermore, the present invention relates to a granulate and/or tablets obtained/obtainable with the process according to the invention, preferably coated to allow the controlled release of the drug. Finally, the present invention relates to the use of the granulate and/or the tablets as a medicament, preferably for the treatment of chronic inflammatory pathologies that preferably affect the intestinal tract.
Core Innovation
The invention relates to a process for preparing a solid pharmaceutical formulation comprising from 70% to 95% by weight of mesalazine and/or a salt thereof and/or a derivative thereof, using a wet granulation based on a powder bed. A powder bed is prepared comprising mesalazine and/or a salt thereof and/or a derivative thereof and optionally at least one pharmacologically acceptable excipient, and an aqueous solution comprising from 10% to 20% of a binding agent is added to obtain a granulate characterized by a moisture content ranging from 20% to 40%.
The granulate is dried until reaching a moisture content lower than or equal to 3.0% and is then mixed with at least one disintegrating agent. Water is added to the granulate obtained from mixing until reaching a moisture content ranging from 3.0% to 3.5%, and the resulting granulate is compacted to form the solid pharmaceutical formulation.
The invention defines critical mesalazine powder properties using apparent density and packing density, together with particle size distribution parameters, and also specifies granulate properties using density and granulate particle size constraints. The resulting solid oral forms include tablet physical parameters such as friability, hardness, and disintegration, and optionally include gastro-resistant or modified-release/controlled release coatings for topical treatment of intestinal chronic inflammatory diseases.
Claims Coverage
Independent claim clm-00001 defines a wet-granulation, rewetting, and compaction process for a solid pharmaceutical formulation with 70% to 95% by weight mesalazine and/or a salt thereof and/or a derivative thereof, with moisture-content constraints across multiple steps. Four inventive features are identified across the independent claim structure.
Powder-bed preparation of high-mesalazine formulation for wet granulation
Preparing a powder bed comprising mesalazine and/or a salt thereof and/or a derivative thereof and optionally at least one pharmacologically acceptable excipient.
Aqueous binding-agent granulation at controlled granulate moisture
Adding an aqueous solution comprising from 10% to 20% of a binding agent to obtain a granulate characterized by a moisture content ranging from 20% to 40%.
Drying to low moisture and rewetting into a narrow moisture band
Drying the granulate until reaching a moisture content lower than or equal to 3.0%, mixing it with at least one disintegrating agent, and adding water until reaching a moisture content ranging from 3.0% to 3.5%.
Compaction of the rewetted granulate to form the solid pharmaceutical formulation
Compacting the granulate obtained after rewetting to form the solid pharmaceutical formulation.
The core inventive concept combines powder-bed formation with high mesalazine content, aqueous binding-agent granulation at defined moisture, drying to a moisture threshold followed by mixing with a disintegrating agent and controlled rewetting to a narrow moisture range, and compaction to obtain the final solid pharmaceutical formulation. The dependent claims further refine material choices, moisture and density constraints, particle-size constraints, tablet-forming parameters, and optional coating-related refinements.
Stated Advantages
Documented Applications
Topical treatment of intestinal chronic inflammatory diseases, including ulcerative colitis and Crohn’s disease.
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