US20250242032
2025-07-31
Human necessities
A61K47/545
The patent application introduces a novel aggregate composed of a chalcogen heterocyclic compound and insulin, along with a method for preparing it. This aggregate can be processed into an oral insulin formulation aimed at reducing blood glucose levels in mammals, potentially benefiting diabetes treatment. The chalcogen heterocyclic compound provides protection for insulin against the physiological barriers encountered during oral uptake, ensuring stability within the gastrointestinal tract and facilitating entry into the circulatory system.
This invention pertains to biomedical technology, specifically focusing on diabetes treatment. Diabetes mellitus is a prevalent chronic disease affecting millions globally, characterized by high blood glucose levels that can lead to severe complications. Insulin is crucial for managing diabetes, but current delivery methods primarily involve injections, which can be painful and inconvenient. Therefore, developing a reliable and easy-to-administer oral insulin formulation is of significant clinical importance.
Oral administration of insulin faces several challenges due to physiological barriers: degradation by stomach acids and digestive enzymes, obstruction by mucoproteins in the gastrointestinal tract, and low absorption rates due to insulin's large molecular size. Existing methods to overcome these barriers often involve complex processes and additional additives that may compromise safety and increase costs. Thus, there is a pressing need for a simpler and more effective solution.
The invention proposes an aggregate formed by assembling a chalcogen heterocyclic compound with insulin. The chalcogen heterocyclic compound features a specific structure (Formula I) that includes a heterocyclic group containing chalcogen atoms (sulfur, selenium, tellurium), a linking group (L), and an interacting group (B) that binds with insulin. These components facilitate the formation of an aggregate through covalent or non-covalent interactions, enhancing insulin's bioavailability when administered orally.
This new approach aims to improve the pharmacokinetics and pharmacodynamics of orally ingested insulin by overcoming physiological barriers without the need for multiple additives. By simplifying the preparation process and enhancing bioavailability, this invention could significantly lower costs and increase the effectiveness of oral insulin formulations, potentially transforming diabetes management practices.