Methods and compositions for oral administration
Inventors
Assignees
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Publication Number
US-11246827-B2
Publication Date
2022-02-15
Expiration Date
Abstract
This invention provides compositions comprising a protein, an absorption enhancer, a protease inhibitor, method for treating diabetes mellitus, comprising administering same, and methods for oral administration of a protein with an enzymatic activity, comprising orally administering same.
Core Innovation
The invention relates to a pharmaceutical composition for oral administration as a solid composition comprising a protein having a molecular weight of up to 150,000 Daltons, wherein the protein is a GLP-2 or a GLP-2 analogue. The composition further comprises a protease inhibitor, and a compound selected from NAC, NAD, a salt of NAC or NAD, or a combination thereof. The amount of the selected compound is in a range of from 70% to 99.4% by weight, and the protease inhibitor is a serpin.
The invention also relates to the synergy between the serpin protease inhibitor and the selected compound, acting in synergy in increasing a bioavailability of the GLP-2 or GLP-2 analogue protein after oral administration. The background of the described subject matter focuses on protecting proteins from degradation and enhancing intestinal absorption for oral delivery.
In additional embodiments described, the protease inhibitor is a serpin such as a trypsin inhibitor, including embodiments featuring specific serpin/trypsin inhibitors such as SBTI and aprotinin. The described composition may include additional optional components such as omega-3 fatty acid and EDTA/Na-EDTA, and may further include digestion-inhibiting coatings or encapsulation, including enteric/gastro-resistant gelatin coatings and microencapsulation, together with sustained-release regimens.
Claims Coverage
The provided independent claim contains 4 core inventive elements: (i) an oral solid composition comprising a GLP-2 or a GLP-2 analogue protein, (ii) a serpin protease inhibitor, (iii) a selected compound (NAC/NAD and/or salts) with a defined weight-range, and (iv) the serpin and compound acting in synergy to increase bioavailability.
Oral solid composition with a GLP-2 protein
A pharmaceutical composition for oral administration that is a solid composition comprising a protein having a molecular weight of up to 150,000 Daltons, the protein being a GLP-2 or a GLP-2 analogue.
Serpin protease inhibitor
The composition further comprises a protease inhibitor, wherein the protease inhibitor is a serpin.
NAC/NAD or salts at a defined weight range
The composition further comprises a compound selected from NAC, NAD, a salt of said NAC or said NAD, or a combination thereof, wherein an amount of said compound is in a range of from 70% to 99.4% by weight.
Synergistic bioavailability increase by protease inhibitor and compound
The protease inhibitor and the compound act in synergy in increasing a bioavailability of said protein.
Overall, the claim coverage centers on an orally administered solid composition containing a GLP-2 or GLP-2 analogue protein, a serpin protease inhibitor, and NAC/NAD (or salts) at a specified weight-range, with a functional limitation that the serpin and compound act synergistically to increase bioavailability. Dependent claims refine specific serpin options, NAC/NAD salt forms, and gastric/intestinal protection via specified coatings, and further narrow solid dosage form and protein form (recombinant).
Stated Advantages
Increases a bioavailability of the GLP-2 or GLP-2 analogue protein.
Documented Applications
Oral delivery use for treating diabetes, including reductions of blood glucose levels and C-peptide levels in human subjects [procedural detail omitted for safety].
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