Methods and compositions for oral administration
Inventors
Assignees
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Publication Number
US-10010503-B2
Publication Date
2018-07-03
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 oral pharmaceutical compositions for treating diabetes that include a protein having a molecular weight of up to 100,000 Daltons. The protein is selected from interferon gamma, interferon alpha, growth hormone, erythropoietin, granulocyte colony stimulating factor (G-CSF), omentin, calcitonin, PTH and PYY. The composition further includes a protease inhibitor and a compound selected from N-(8-[2-hydroxybenzoyl] amino)caprylate (NAC), N-(10-[2-hydroxybenzoyl]amino)decanoate (NAD), a salt of said NAC or said NAD, and combinations thereof.
A key aspect is that the compound is in an effective amount to synergistically increase the bioavailability of the protein when administered orally. The combination with at least one protease inhibitor is described as protecting the orally administered protein from degradation in the gastrointestinal tract. The partial content further states that this combination unexpectedly and synergistically improves protein/insulin/Exenatide bioavailability and associated blood glucose and C-peptide outcomes.
The partial disclosure describes absorption enhancer/protease inhibitor combinations intended to inhibit stomach digestion. The protease inhibitor is described broadly to include serpin and trypsin inhibitors such as SBTI/aprotinin, as well as cysteine, threonine, aspartic and metalloprotease inhibitors, and related chelating agents such as EDTA/Na-EDTA and EGTA. Optional additional components described in the partial content include omega-3 fatty acids and digestion-inhibiting coatings such as enteric coatings, gelatin coatings, or microencapsulation.
Claims Coverage
The independent claim covers an orally administered pharmaceutical composition featuring three inventive elements: a specified protein (MW up to 100,000 Daltons), a protease inhibitor, and an NAC/NAD enhancer compound in an effective amount that synergistically increases protein bioavailability. The document also includes independent claim coverage for an oral method that administers the same composition framework to a subject in need.
Oral protein formulation with specified proteins up to 100,000 Daltons
A pharmaceutical composition for oral administration comprising a protein having a molecular weight of up to 100,000 Daltons, the protein being selected from interferon gamma, interferon alpha, growth hormone, erythropoietin, granulocyte colony stimulating factor (G-CSF), omentin, calcitonin, PTH and PYY.
Protease inhibitor plus NAC/NAD enhancer synergy for bioavailability
The composition comprises a protease inhibitor and a compound selected from N-(8-[2-hydroxybenzoyl] amino)caprylate (NAC), N-(10-[2-hydroxybenzoyl]amino)decanoate (NAD), a salt of said NAC or said NAD, and combinations thereof, the compound being in an effective amount to synergistically increase the bioavailability of said protein.
Oral administration method to a subject in need
A method administers orally to a subject in need a pharmaceutical composition comprising a protein having a molecular weight of up to 100,000 Daltons, together with a protease inhibitor and the compound selected from NAC, NAD, salts thereof, or combinations thereof, the compound being in an effective amount to synergistically increase the bioavailability of the protein.
Across the independent claim coverage, the core inventive concept is an orally administered formulation combining a specified protein (MW up to 100,000 Daltons), a protease inhibitor, and NAC/NAD (or salts) in an effective amount that synergistically increases protein bioavailability, with independent claim coverage also directed to oral administration of the same composition to a subject in need.
Stated Advantages
Synergistically increases the bioavailability of the protein.
Unexpectedly and synergistically increases protein/insulin/Exenatide bioavailability and improves blood glucose and C-peptide outcomes (as stated in the partial content).
Documented Applications
Use in treating diabetes, including oral formulations intended to improve protein/insulin/Exenatide outcomes.
Oral administration to a subject in need of the pharmaceutical composition (method context).
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