Solid compositions comprising a GLP-1 agonist and a salt of N-(8-(2-hydroxybenzoyl)amino)caprylic acid
Inventors
Pedersen, Betty Lomstein • Nissen, Birgitte
Assignees
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Publication Number
US-12396953-B2
Publication Date
2025-08-26
Expiration Date
Abstract
The invention relates to pharmaceutical compositions comprising a peptide, such as a GLP-1 peptide and a salt of N-(8-(2-hydroxybenzoyl)amino)caprylic acid. The invention further relates to processes for the preparation of such compositions, and their use in medicine.
Core Innovation
The invention relates to oral solid pharmaceutical compositions comprising semaglutide and sodium N-(8-(2-hydroxybenzoyl)amino)caprylic acid (SNAC) as a delivery/absorption enhancer, with magnesium stearate as an excipient. SNAC is present at very high weight fraction, specifically constituting at least 95% (w/w) of the excipients of the composition, and the composition specifies a quantitative relationship between magnesium stearate and SNAC.
The compositions optionally include a small amount of lubricant, and are described as oral solid dosage forms such as tablet, capsule, or sachet. Multiple GLP-1 agonists are identified, including semaglutide and specific diacylated GLP-1 analogs, including GLP-1 analogue B and GLP-1 analogue C.
A stated performance aim is fast release and increased early dose-corrected exposure, with dissolution and pharmacokinetic outcomes described using measurements such as AUC 0-30 min in beagle dogs. Example formulations are described with observed dissolution and PK improvements versus reference formulations using more conventional excipient systems.
Claims Coverage
The document provides one independent composition claim and additional independent method-use claims that rely on administering the defined pharmaceutical composition. The independent claims focus on quantitative composition constraints and on medical uses.
Semaglutide-SNAC high-excipient formulation with defined magnesium stearate level
A pharmaceutical composition comprising semaglutide, sodium N-(8-(2-hydroxybenzoyl)amino)caprylic acid (SNAC), and magnesium stearate, wherein semaglutide is in an amount of 0.2 to 100 mg, wherein the pharmaceutical composition comprises 2-5 mg of the magnesium stearate per 100 mg of the SNAC, and wherein the SNAC constitutes at least 95% (w/w) of the excipients of the composition.
Treating type 2 diabetes by administering the semaglutide-SNAC formulation
A method for treating type 2 diabetes by administering the pharmaceutical composition of the composition claim to a subject in need.
Reducing body weight by administering the semaglutide-SNAC formulation
A method for reducing a subject's body weight by administering a pharmaceutical composition according to the composition claim.
Overall, the claim coverage centers on a semaglutide formulation with SNAC as the dominant excipient (at least 95% w/w) together with a specified magnesium stearate amount relative to SNAC, and on administering that composition for type 2 diabetes treatment and for reducing body weight.
Stated Advantages
Fast release.
Increased early dose-corrected exposure (e.g., AUC 0-30 min) in beagle dogs.
Improved dissolution and PK performance compared with reference formulations using more conventional excipients.
Documented Applications
Medical treatment of type 2 diabetes by administering the pharmaceutical composition to a subject in need.
Reduction of a subject's body weight by administering the pharmaceutical composition.
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