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Last Updated: November 27, 2020

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Claims for Patent: 9,925,174

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Summary for Patent: 9,925,174
Title:Administration form for the oral application of 3-[(2-{[4-(hexyloxycarbonyl-amino-imino-methyl)-phenylamino]-methyl}-1-me- thyl-1 H-benzimidazol acid ethyl ester and the salts thereof
Abstract: The invention relates to a new administration form for the oral application of the active substance ethyl 3-[(2-{[4-(hexyloxycarbonylamino-imino-methyl)-phenylamino]-methyl}-1-met- hyl-1H-benzimidazole-5-carbonyl)-pyridin-2-yl-amino]-propionate and the pharmacologically acceptable salts thereof.
Inventor(s): Brauns; Ulrich (Biberach, DE)
Assignee: Boehringer Ingelheim International GmbH (Ingelheim am Rhein, DE)
Application Number:11/381,890
Patent Claims: 1. A pharmaceutical composition for oral administration comprising: (a) a substantially spherical core material comprised of one or more pharmaceutically acceptable organic acids with a water solubility of >1 g / 250 mL at 20.degree. C.; and (b) an active substance layer containing one or more binders and optionally a separating agent, wherein said active substance is ethyl 3-[(2-{[4-(hexyloxycarbonylamino-imino-methyl) -phenylamino]-methyl}-1-methyl-1H-benzimidazole-5-carbonyl)-pyridin-2-yl-- amino]-propionate mesylate; (c) an insulating layer separating said core material and active substance layer, wherein said insulating layer is comprised of a water-soluble polymer, optionally with addition of suitable plasticizers, separating agents and pigments; and (d) an optional coating layer enclosing the active substance layer, wherein the pharmaceutical composition provides a patient with the active substance having a bioavailability that is therapeutically effective at normal and elevated gastric pH.

2. The pharmaceutical composition of claim 1, wherein the acceptable organic acid has a water solubility of > 1 g/160 mL at 25.degree. C.

3. Pharmaceutical composition according to claim 1, wherein the pharmaceutically acceptable organic acid is selected from the group consisting of tartaric acid, fumaric acid, succinic acid, citric acid, malic acid, glutamic acid, aspartic acid and any combination thereof.

4. Pharmaceutical composition according to claim 1, wherein the pharmaceutically acceptable organic acid is selected from the group consisting of tartaric acid, fumaric acid, citric acid, succinic acid and any combination thereof.

5. Pharmaceutical composition according to claim 1, wherein the pharmaceutically acceptable organic acid is tartaric acid.

6. Pharmaceutical composition according to claim 1, wherein the content of ethyl 3-[(2-{[4-(hexyloxycarbonylamino-imino-methyl) -phenylamino]-methyl}-1-methyl-1H-benzimidazole-5-carbonyl)-pyridin-2-yl-- amino]-propionate mesylate in the pharmaceutical composition is 5 to 60%.

7. Pharmaceutical composition according to claim 1, wherein the content of pharmaceutically acceptable organic acid is 20 to 90%.

8. Pharmaceutical composition according to claim 1, wherein said binder is selected from the group consisting of hydroxypropylcelluloses, hydroxypropylmethylcelluloses, methylcelluloses, hydroxyethylcelluloses, carboxymethylcelluloses, the polyvinylpyrrolidones, the copolymers of N-vinylpyrrolidone, vinyl acetate and any combination thereof.

9. Pharmaceutical composition according to claim 1, wherein said core material has an average particle size of 0.4 to 1.5 mm.

10. Pharmaceutical composition according to claim 1, wherein said water-soluble polymer is comprised of gum arabic or hydroxypropylmethylcellulose (HPMC).

11. Pharmaceutical composition according to claim 1, wherein said water-soluble polymer is comprised of a partially or totally synthetic polymer selected from the group consisting of hydroxypropylcelluloses, hydroxypropyl-methylcelluloses, methylcelluloses, hydroxyethylcelluloses, carboxymethylcelluloses, the polyvinylpyrrolidones, the copolymers of N-vinylpyrrolidone, vinyl acetate, and any combination thereof.

12. Pharmaceutical composition according to claim 1, wherein the composition containing the active substance is packed into hard capsules.

13. Pharmaceutical composition of claim 12, wherein the hard capsule is hydroxypropylmethylcellulose (HPMC).

14. Pharmaceutical composition of claim 1, wherein the pharmaceutically acceptable organic acid is tartaric acid.

15. The pharmaceutical composition according to claim 1, wherein the core material consists of tartaric acid and gum arabic, the insulating layer consists of gum Arabic or hydroxypropylmethylcellulose and talc and the active substance layer consists of talc, hydroxypropylcellulose and ethyl 3-[(2-{[4-(hexyloxycarbonylamino-imino-methyl) -phenylamino]-methyl}-1-methyl-1H-benzimidazole-5-carbonyl)-pyridin-2-yl-- amino]-propionate mesylate.

16. The pharmaceutical composition according to claim 15, wherein the tartaric acid in the core material is present in the composition at about 61.3%, the gum arabic in the core material is present in the composition at about 3.1%, the gum arabic in the insulating layer is present in the composition at about 2.8%, the talc in the insulating layer is present in the composition at about 5.6%, the talc in the active substance layer is present in the composition at about 3.2%, the hydroxypropylcellulose in the active substance layer is present in the composition at about 4.0% and the ethyl 3-[(2-{[4-(hexyloxycarbonylamino-imino-methyl) -phenylamino]-methyl}-1-methyl-1H-benzimidazole-5-carbonyl)-pyridin-2-yl-- amino]-propionate mesylate in the active substance layer is present in the composition at about 20%.

17. The pharmaceutical composition according to claim 15, wherein the tartaric acid in the core material is present in the composition at about 38.5%, the gum arabic in the core material is present in the composition at about 1.9%, the gum arabic in the insulating layer is present in the composition at about 1.7%, the talc in the insulating layer is present in the composition at about 3.5%, the talc in the active substance layer is present in the composition at about 6.4%, the hydroxypropylcellulose in the active substance layer is present in the composition at about 8.0% and the ethyl 3-[(2-{[4-(hexyloxycarbonylamino-imino-methyl) -phenylamino]-methyl}-1-methyl-1H-benzimidazole-5-carbonyl)-pyridin-2-yl-- amino]-propionate mesylate in the active substance layer is present in the composition at about 40%.

18. The pharmaceutical composition of claim 1, wherein the active substance layer contains from 50 mg to 200 mg of ethyl 3-[(2-{[4-(hexyloxycarbonylamino-imino-methyl) -phenylamino]-methyl}-1-methyl-1H-benzimidazole-5-carbonyl)-pyridin-2-yl-- amino]-propionate.

19. The pharmaceutical composition of claim 1, wherein the active substance layer contains from 75 mg to 150 mg of ethyl 3-[(2-{[4-(hexyloxycarbonylamino-imino-methyl) -phenylamino]-methyl}-1-methyl-1H-benzimidazole-5-carbonyl)-pyridin-2-yl-- amino]-propionate.

20. The pharmaceutical composition of claim 1, wherein the active substance layer contains 150 mg of ethyl 3-[(2-{[4-(hexyloxycarbonylamino-imino-methyl) -phenylamino]-methyl}-1-methyl-1H-benzimidazole-5-carbonyl)-pyridin-2-yl-- amino]-propionate.

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