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EP0127535A2 Expired / Lapsed EP ⏱️ 0.0 years remaining

Pharmaceutical compositions containing insulin

Assignee: Hadassah Medical Organization
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Filing: 1984-05-21
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Granted: —
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Expires: 2004-05-21
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Abstract

Abstract The invention provides a pharmaceutical composition for the oral administration of insulin comprising insulin, a bile acid or alkali metal salt thereof, the bile acid being selected from the group consisting of cholic acid, chenodeoxycholic acid, taurocholic acid, taurochenodeoxycholic acid, glycocholic acid, glycochenocholic acid, 3β-hydroxy-12- ketocholic acid, 12α-3β-dihydrocholic acid, and ursodesoxycholic acid, and a protease inhibitor, the composition being provided with an enterocoating to assure passage through the stomach and release in the intestine.

Inventors

  • 👤 Miriam Kidron
  • 👤 Ehud Ziv
  • 👤 Hanoch Bar-On
  • 👤 Amiram Eldor

Bibliographic Details

Application Number —
Jurisdiction EP
Data Source google_patents
Last Synchronized 2026-10-26 18:32
CPC Classifications
A; A61; A61K; A61K38/00; A61K38/16; A61K38/17; A61K38/22; A61K38/28; A61K38/55; A61K9/00; A61K9/20; A61K9/2004; A61K9/2013; A61K9/2068; A61K9/28; A61K9/2806; A61K9/2833; A61K9/284; A61K9/2846

Claims Analysis

Total Claims: 10
Claim 1
Independent Claim 75 words
A pharmaceutical composition for the oral administration of insulin comprising insulin, a bile acid or alkali metal salt thereof, said bile acid being selected from the group consisting of cholic acid, chenodeoxycholic acid,taurocholic acid, taurochenodeoxycholic acid, glycocholic acid, glycochenocholic acid, 3β-monohydroxychloric acid, lithocholic acid, 3a-hydroxy-12-ketocholic acid, 3β-hydroxy-12-ketocholic acid, 12a-3a-dihydrocholic acid, and ursodesoxycholic acid, and a protease inhibitor, said composition being provided with an enterocoating to assure passage through the stomach and release in the intestine.
Claim 2
Dependent Claim 75 words
A pharmaceutical composition for the oral administration of insulin comprising insulin, a bile acid or alkali metal salt thereof, said bile acid being selected from the group consisting of cholic acid, chenodeoxycholic acid,taurocholic acid, taurochenodeoxycholic acid, glycocholic acid, glycochenocholic acid, 3β-monohydroxychloric acid, lithocholic acid, 3a-hydroxy-12-ketocholic acid, 3β-hydroxy-12-ketocholic acid, 12a-3a-dihydrocholic acid, and ursodesoxycholic acid, and a protease inhibitor, said composition being provided with an enterocoating to assure passage through the stomach and release in the intestine.
Claim 3
Dependent Claim 34 words
A pharmaceutical composition according to claim 1, wherein said protease inhibitor is selected from the group consisting of aprotinin, A 2 -macroglobulin, antithrombin III and trypsin inhibitor from soy bean or chicken egg white.
Claim 4
Dependent Claim 19 words
A pharmaceutical composition according to claim 1, comprising sodium cholate as both the bile acid and the protease inhibitor.
Claim 5
Dependent Claim 26 words
A pharmaceutical composition according to claim 1,wherein the components of said composition are microencapsulated and enterocoated to provide for timed release of ingredients in the intestine.
Claim 6
Dependent Claim 3 words
CLAIMS (for AT)
Claim 7
Dependent Claim 90 words
A process for preparing a pharmaceutical composition for the oral administration of insulin, characterized in that it comprises mixing active ingredients consisting of insulin, a bile acid or alkali metal salt thereof, said bile acid being selected from the group consisting of cholic acid, chenodeoxycholic acid, taurocholic acid, taurochenodeoxycholic acid, glycocholic acid, glycochenocholic acid, 36-monohydroxychloric acid, lithocholic acid, 30(-hydroxy-12-ketocholic acid, 3β-hydroxy-12-ketocholic acid, 12α-3β-dihydrocholic acid, and ursodesoxycholic acid, and a protease inhibitor, and providing said active components with an enterocoating to assure passage through the stomach and release in the intestine.
Claim 8
Dependent Claim 90 words
A process for preparing a pharmaceutical composition for the oral administration of insulin, characterized in that it comprises mixing active ingredients consisting of insulin, a bile acid or alkali metal salt thereof, said bile acid being selected from the group consisting of cholic acid, chenodeoxycholic acid, taurocholic acid, taurochenodeoxycholic acid, glycocholic acid, glycochenocholic acid, 36-monohydroxychloric acid, lithocholic acid, 30(-hydroxy-12-ketocholic acid, 3β-hydroxy-12-ketocholic acid, 12α-3β-dihydrocholic acid, and ursodesoxycholic acid, and a protease inhibitor, and providing said active components with an enterocoating to assure passage through the stomach and release in the intestine.
Claim 9
Dependent Claim 53 words
Process according to claim 1, characterized in that said active components are mixed with a solid vehicle, the mixture thus obtained is mechanically pressed to form tablets, the later are coated with a solution of an enterocoating polymer in an organic solvent and the organic solvent is then removed from the coated tablets.
Claim 10
Dependent Claim 23 words
Process according to claim 2, characterized in that the solid vehicle is lactose and the organic solvent is a methylene chloride-isopropyl alcohol mixture.

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