Oral delivery of peptide pharmaceutical compositions

a technology of pharmaceutical compositions and peptides, applied in the direction of drug compositions, dispersed delivery, peptide/protein ingredients, etc., can solve the problem of inability to deliver via oral means

Inactive Publication Date: 2005-12-22
UNIGENE LABORATORIES
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Benefits of technology

[0010] It is accordingly an object of the present invention to provide a therapeutically effective oral pharmaceutical composition for reliably delivering pharmaceutical peptides, e.g., physiologically active peptide agents having analgesic and / or cardiovascular activity.

Problems solved by technology

However, even with such stable and protease-resistant analogs, oral delivery is not feasible due to low bioavailability.

Method used

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  • Oral delivery of peptide pharmaceutical compositions
  • Oral delivery of peptide pharmaceutical compositions
  • Oral delivery of peptide pharmaceutical compositions

Examples

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Embodiment Construction

[0058] In accordance with the invention, patients in need of treatment with peptides having analgesic and / or cardiovascular activity are provided with an oral pharmaceutical composition thereof (at appropriate dosage), preferably but not necessarily in tablet or capsule form of an ordinary size in the pharmaceutical industry. The dosages and frequency of administering the products are discussed in more detail below. Patients who may benefit are any who suffer from disorders that respond favorably to increased levels of a peptide-containing compound. For example, oral administration of dermorphin, deltorphin and / or enkephalin peptide analogs in accordance with the invention may be used to treat patients in need of pain relief, or those with conditions warranting improved cardiac performance, e.g., by improving myocardial contractile force.

[0059] Without intending to be bound by theory, the pharmaceutical compositions of the invention are believed to overcome a series of different an...

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Abstract

Bioavailability of peptide active agents to be administered orally is enhanced by a pharmaceutical composition providing targeted release of the peptide to the intestine by combining the composition with an absorption enhancer. Bioavailability is further significantly increased by administering the composition in an acid-resistant protective vehicle which transports components of the invention through the stomach. The composition may optionally further include a sufficient amount of a pH-lowering agent to lower local intestinal pH. All components are released together into the intestine with the peptide.

Description

CROSS REFERENCE TO A RELATED APPLICATION [0001] The present application is a 35 U.S.C. § 119 conversion of Provisional Application Ser. No. 60 / 580,872 filed Jun. 18, 2004BACKGROUND OF THE INVENTION [0002] 1. Field of the Invention [0003] The present invention relates to oral peptide pharmaceutical compositions having analgesic and / or cardiovascular activity, and to methods of enhancing bioavailability of such peptides when administered orally. [0004] 2. Description of the Related Art [0005] Opiates such as morphine and codeine, or opiate-like synthetic drugs are currently used for the management of moderate to severe pain. Many endogenous peptides of mammalian and amphibian origin (e.g., the endorphins) also bind to opioid receptors and elicit an analgesic response similar to classic narcotic opiates. This led to the hope that these peptides might be produced commercially and administered to patients to, e.g., relieve pain. It was found, however, that side effects such as depression...

Claims

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Application Information

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Patent Type & Authority Applications(United States)
IPC IPC(8): A61K38/08A61K9/00A61K9/48A61K38/06A61K38/07A61K47/18A61K47/26
CPCA61K9/0095A61K9/4858A61K9/4891A61K47/26A61K38/07A61K38/08A61K47/183A61K38/06A61P29/00A61P9/00A61K9/0053
Inventor MEHTA, NOZER M.STERN, WILLIAMGILLIGAN, JAMES P.
Owner UNIGENE LABORATORIES
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