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Publication Number
US-12514822-B2
Publication Date
2026-01-06
Expiration Date
Abstract
The present invention relates to improved uses of glucagon-like peptide 1 (GLP-1) peptides in oral therapy.
Core Innovation
The disclosed invention relates to oral therapy for treating type 2 diabetes using a solid oral composition comprising semaglutide and sodium N-(8-(2-hydroxybenzoyl)amino)caprylate (SNAC). The semaglutide is present in an amount of 0.5–50 mg, and the composition is administered orally as a solid dosage form such as a tablet. The approach targets control of human pharmacokinetics, including human plasma half-life and dosing interval, to support long-plasma-half-life exposure.
A central feature is that the administration is configured such that the ratio between the plasma half-life in days in humans of the semaglutide and the dosing interval in days of the composition is more than 2:1, with further ratio ranges described. The disclosure further addresses reduced variability in plasma concentration to lower GLP-1–related side effects. The composition context includes an absorption/bioavailability enhancer and solid oral compositions, with SNAC used alongside semaglutide.
The disclosure also describes tablet-related excipients and optional coatings. Determination of relevant pharmacokinetic parameters and variability is described using methods including LC-MS and LOCI, and the disclosure includes background on peptide/derivative context for GLP-1 peptides and related chemistry.
Claims Coverage
The partial content provides one independent claim (clm-00001). Across the dependent claims listed, the main inventive features refine the oral composition and constrain the administration timing by a plasma half-life to dosing-interval ratio exceeding 2:1, with additional refinements for dosage form and subject population.
Oral semaglutide with SNAC for type 2 diabetes
Orally administering to a subject a composition comprising semaglutide and sodium N-(8-(2-hydroxybenzoyl)amino)caprylate (SNAC) for treating type 2 diabetes.
Semaglutide amount of 0.5–50 mg
The composition comprises 0.5–50 mg of semaglutide.
Plasma half-life to dosing-interval ratio greater than 2:1
The composition is administered such that the ratio between the plasma half-life in days in humans of semaglutide and the dosing interval in days is more than 2:1.
SNAC content as 50–90% (w/w)
The composition comprises SNAC as 50–90% (w/w) of the composition.
Tablet dosage form
The composition is provided as a tablet.
Semaglutide is the only GLP-1 peptide present
The composition uses semaglutide as the only GLP-1 peptide present.
SNAC dose level (100 mg)
The composition includes 100 mg of SNAC.
Treatment of subjects suffering from obesity
The method treats a subject who suffers from obesity.
Overall coverage centers on oral administration of a semaglutide/SNAC solid composition with a semaglutide amount set to 0.5–50 mg and an administration timing requirement defined by a human plasma half-life to dosing-interval ratio greater than 2:1, with dependent refinements specifying SNAC content, tablet format, semaglutide-only GLP-1 peptide content, an SNAC dose example, and a subject population narrowed to obesity.
Stated Advantages
Reduced variability in plasma concentration to lower GLP-1–related side effects.
Reduced %CV plasma exposure with repeated daily dosing in SNAC formulations versus single-dose or less frequent regimens.
Documented Applications
Medical indication: treating type 2 diabetes in a subject in need of such treatment.
Medical indication: treating subjects who suffer from obesity.
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