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Methods And Compositions For Oral Administration Of Proteins

A composition and protein technology, applied in the direction of peptide/protein composition, drug combination, drug delivery, etc., can solve the problems of fat hyperplasia, lipodystrophy, atrophy, etc.

Pending Publication Date: 2015-08-26
ENTERA BIO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Known side effects such as lipodystrophy, lipoatrophy, lipohypertrophy, and occasional hypoglycemia at the injection site
In addition, subcutaneously administered insulin typically does not provide the fine-grained, sustained metabolic regulation normally provided by insulin secreted by the pancreas into the liver via the direct portal vein

Method used

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  • Methods And Compositions For Oral Administration Of Proteins
  • Methods And Compositions For Oral Administration Of Proteins

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0124] implement Example 1: Oral formulations of insulin, SNAC, and protease inhibitors

[0125] Material and experimental methods

[0126] preparation

[0127] Prepare the following preparations: (1) containing 6mg insulin, 250mg SNAC, 125mg SBTI, (2) containing 6mg insulin, 250mg SNAC, 2.5mg aprotinin, 125mg SBTI, (3) containing 6mg insulin, 250mg SNAC, 2.5mg aprotinin Peptide, 125mg SBTI, (4) with 6mg insulin, 250mg SNAC. The formulations were stored in the refrigerator (4°C) prior to dosing.

[0128] result

[0129] In a subsequent experiment, the formulations described in the "Formulations" section were orally administered to 3 healthy human subjects. like figure 1 As shown, blood glucose levels were significantly lower and more stable in human subjects treated with formulations (1) and (3). These results indicate that formulations comprising a combination of protease inhibitors and SNAC are superior to formulations comprising SNAC alone. Specifically, the co...

Embodiment 2

[0132] Example 2: Optimization of Omega-3 Fatty Acid Sources

[0133] Various omega-3 fatty acids or sources of omega-3 fatty acids, such as those listed above in this specification, were compared for their ability to protect insulin following oral administration in the methods and compositions of the invention. Insulin tablets or capsules were formulated as described in the previous examples, except that the insulin was dissolved in an alternative source instead of fish oil. The most effective source of omega-3 fatty acids is used in the examples that follow.

Embodiment 3

[0134] Example 3: Optimization of Protease Inhibitors

[0135]Various protease inhibitors (either non-toxic or having an acceptable toxicity profile; such as those listed above in this specification) were compared for their ability to protect insulin following oral administration in the methods and compositions of the invention. Insulin and / or exenatide tablets or capsules are formulated as described in the above examples, except that alternative protease inhibitors are used in place of SBTI and / or aprotinin. The amount of protease inhibitors was also varied to determine the optimal amount. The most effective protease inhibitors / amounts were used in subsequent examples.

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Abstract

This invention relates to methods and compositions for oral administration of proteins, in particular provides compositions comprising a protein, an absorption enhancer and a protease inhibitor, methods for treating diabetes mellitus, comprising administering same, and methods for oral administration of a protein with an enzymatic activity, comprising orally administering same.

Description

[0001] This application is a divisional application of the Chinese patent application with the application number 200980132155.8, the application date is August 11, 2009, and the invention title is "Method and Composition for Oral Administration of Protein". technical field [0002] The present invention provides oral compositions comprising proteins, absorption enhancers and protease inhibitors and methods of administering said compositions. Background technique [0003] Thanks to the development of biotechnology, the feasibility of bioactive peptides entering the pharmaceutical industry has been significantly improved. However, a limiting factor in the development of peptide drugs is their relative ineffectiveness when administered orally. Almost all peptide drugs are administered parenterally, but parenterally administered peptide drugs are often associated with low patient compliance. [0004] Insulin is a drug used to treat people with diabetes and is the only treatmen...

Claims

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Application Information

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IPC IPC(8): A61K38/56A61K9/00A61P3/10A61K38/29
Inventor 米丽娅姆·基德隆埃胡德·阿比特
Owner ENTERA BIO LTD