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Last Updated: December 22, 2024

Claims for Patent: 4,980,173


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Summary for Patent: 4,980,173
Title: Pharmaceutical composition and method for the treatment of colitis ulcerosa and Crohn's disease by oral administration
Abstract:A pharmaceutical composition containing as active ingredient 5-aminosalicylic acid or a pharmaceutically acceptable salt or ester thereof allow the treatment of colitis ulcerosa or Crohn's disease by oral administration. A particular slow-release tablet formation and its preparation is disclosed.
Inventor(s): Halskov; Soren (Helsinge, DK)
Assignee: Farmaceutisk Laboratorium Ferring A/S (Vanlose, DK)
Application Number:07/371,085
Patent Claims: 1. A method for the preparation of sustained-release tablets useful for the treatment of colitis ulcerosa or Crohn's disease, comprising the steps of

(a) preparing a first granulate from 5-aminosalicylic acid or a pharmaceutically acceptable salt or ester thereof and about 10% by weight (solids content, based on the 5-aminosalicylic acid) of polyvinylpyrrolidone in an organic solvent thereby to provide granules of a particle size form about 0.7 to 1 mm, upon evaporation of the solvent,

(b) applying onto said granules a coating composition, comprising a solution in an organic solvent of a pharmaceutically acceptable coating material which will gradually release the active ingredient upon arrival at the small intestine, thereby to provide coated granules upon evaporation of the solvent,

(c) mixing the first granulate with about 5% by weight, calculated on the total solids content, of a lubricant and a conventional pharmaceutical tablet carrier in an amount in accordance with the desired size and active ingredient content of the tablet, and

(d) forming tablets from the resulting mixture.

2. A method according to claim 1 wherein the coating material is a cellulose derivative.

3. A method for the treatment of ulcerative colitis or Crohn's disease comprising orally administering an effective amount of a composition consisting essentially of free 5-aminosalicylic acid in admixture with a pharmaceutically acceptable carrier so as to delay the release of said effective amount of 5-aminolsalicylic acid to be administered essentially until the colon of the patient is reached.

4. A method according to claim 3, wherein the delayed release is dependent on the prevailing pH in the colon.

5. A method according to claim 3, wherein the carrier comprises a coating capable of delaying the release of said effective amount essentially until the colon is reached.

6. A method for the treatment of ulcerative colitis or Crohn's disease comprising orally administering an effective amount of a composition consisting essentially of free 5-aminosalicylic acid in admixture with a pharmaceutically acceptable carrier so as to gradually release said effective amount of 5-aminosalicylic acid throughout the small intestine and continuously throughout the colon of the patient.

7. A method according to claim 6 wherein the 5-aminosalicylic acid is in the form of particles coated with a pharmaceutically acceptable coating material which will gradually release the 5-aminosalicylic acid upon arrival at the small intestine.

8. A method according to claim 7 wherein the coating material is ethyl cellulose.

9. A method according to claim 6, wherein the gradual release is brought about by establishing suitable pH conditions in the composition.

10. A method for the treatment of Crohn's disease comprising orally administering an effective amount of a composition consisting essentially of free 5-aminosalicylic acid in admixture with a pharmaceutically acceptable carrier which will secure an early release of said effective amount of 5-aminosalicylic acid upon arrival in the small intestine.

11. A method according to claim 10, wherein the early release is dependent on the prevailing pH in the small intestine.

12. A method for the treatment of ulcerative colitis or Crohn's disease consisting essentially of orally administering an effective amount of a composition consisting essentially of free 5-aminosalicylic acid in admixture with a pharmaceutically acceptable carrier so as to delay the release of said effective amount of 5-aminosalicylic acid to be administered essentially until the colon of the patient is reached.

13. A method for the treatment of ulcerative colitis or Crohn's disease consisting essentially of orally administering an effective amount of a composition consisting essentially of free 5-aminosalicylic acid in admixture with a pharmaceutically acceptable carrier so as to gradually release said effective amount of 5-aminosalicylic acid throughout the small intestine and continuously throughout the colon of the patient.

14. A method for the treatment of Crohn's disease consisting essentially of orally administering an effective amount of a composition consisting essentially of free 5-aminosalicylic acid in admixture with a pharmaceutically acceptable carrier which will secure an early release of said effective amount of 5-aminosalicylic acid upon arrival in the small intestine.

15. A method for the preparation of sustained-release tablets useful for the treatment of colitis ulcerosa or Crohn's disease, comprising the steps of

(a) preparing a first granulate from 5-aminosalicylic acid or a pharmaceutically acceptable salt or ester thereof and about 10% by weight (solids content, based on the 5-aminosalicylic acid) of polyvinylpyrrolidone in an organic solvent thereby to provide granules of a particle size from about 0.7 to 1 mm, upon evaporation of the solvent,

(b) applying onto said granules a coating composition, comprising a solution in an organic solvent of a pharmaceutically acceptable coating material which will gradually release the active ingredient upon arrival at the small intestine, thereby to provide coated granules upon evaporation of the solvent,

(c) preparing a second granulate of about same particle size as the first granulate form a pharmaceutical carrier having essentially the same density as the 5-ASA derivative and about 10% by weight of polyvinylpyrrolidone in an organic solvent,

(d) mixing the first granulate with about 5% by weight, calculated on the total solids content, of a lubricant and the second granulate in an amount in accordance with the desired size and active ingredient content of the tablet, and

(e) forming tablets from the resulting mixture.

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