Compositions of GLP-1 peptides and preparation thereof
Inventors
Vilhelmsen, Thomas Kvistgaard • Eliasen, Helle • Hansen, Tue
Assignees
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Publication Number
US-12594326-B2
Publication Date
2026-04-07
Expiration Date
Abstract
The invention relates to pharmaceutical compositions comprising a first type of granules and a second type of granules, wherein said first type of granules comprises a salt of N-(8-(2-hydroxybenzoyl)amino)caprylic acid and no GLP-1 peptide, and wherein said second type of granules comprises a GLP-1 peptide and no salt of N-(8-(2-hydroxybenzoyl)amino)caprylic acid, as well as the intermediate granules, processes for the preparation of the granules and compositions, and use thereof in medicine.
Core Innovation
The invention relates to oral pharmaceutical compositions for delivering GLP-1 peptides using a two-type granule design. A first type of granules comprises sodium N-(8-(2-hydroxybenzoyl)amino)caprylic acid (SNAC) without GLP-1, and a second type of granules comprises a GLP-1 peptide without SNAC. The design separates the SNAC component and the GLP-1 peptide into different granule types within the same pharmaceutical composition.
The composition includes a first type of granules and a second type of granules with defined amounts and formulation constraints. The first type of granules includes at least 70% (w/w) SNAC and less than 10% (w/w) of a lubricant, while the second type of granules includes semaglutide, at least 15% (w/w) of a filler, and less than 40% (w/w) of a binder. The disclosed granule approach supports oral delivery while maintaining the separation of SNAC and GLP-1 components.
The invention addresses oral administration of GLP-1 peptides by using SNAC granules in a configuration designed to promote dissolution-release behavior. Reported dissolution-release relationships indicate SNAC release simultaneous with or faster than the GLP-1 peptide as measured by Assay (I) at different pH values. The document further reports in vivo dog bioavailability data associated with the granule design and uses Assay (II) to quantify bioavailability.
Claims Coverage
The partial content includes one independent claim that defines a two-type granule pharmaceutical composition for oral delivery of semaglutide with defined SNAC, lubricant, filler, and binder amounts. The dependent claims further specify particular excipient materials and constrain which granule type contains which actives, for a total of six inventive features.
Two-type granule pharmaceutical composition with separated SNAC and semaglutide
A pharmaceutical composition comprising a first type and a second type of granules, wherein the first type comprises at least 70% (w/w) sodium N-(8-(2-hydroxybenzoyl)amino)caprylic acid (SNAC) and less than 10% (w/w) of a lubricant, and wherein the second type comprises semaglutide, at least 15% (w/w) of a filler, and less than 40% (w/w) of a binder.
Specific lubricant in SNAC granules
The pharmaceutical composition where the lubricant is magnesium stearate.
Specific filler in semaglutide granules
The pharmaceutical composition where the filler is microcrystalline cellulose.
Specific binder in semaglutide granules
The pharmaceutical composition where the binder is povidone.
Semaglutide excluded from the first granule type
The pharmaceutical composition where the first type of granules excludes semaglutide.
SNAC excluded from the second granule type
The pharmaceutical composition where the second type of granules does not include SNAC.
Overall, claim coverage centers on a two-type granule pharmaceutical composition that separates SNAC and semaglutide into different granule types, with quantitative constraints for SNAC and lubricant in the first granules and semaglutide, filler, and binder in the second granules. Dependent claims narrow the formulation by specifying magnesium stearate, microcrystalline cellulose, and povidone as particular excipient components and by explicitly excluding semaglutide from the SNAC-containing granules and excluding SNAC from the semaglutide-containing granules.
Stated Advantages
Documented Applications
No documented applications found
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