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1. WO2007147596 - GALENICAL FORMULATIONS OF ALISKIREN AND HYDROCHLOROTHIAZIDE

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[ EN ]

What is claimed is:

1. A solid oral dosage form comprising

a) a therapeutically effective amount of Aliskiren, or a pharmaceutically acceptable
salt thereof,

b) a therapeutically effective amount of hydrochlorothiazide (HCTZ), and

c) a hydrophilic filler selected from a carbohydrate or combinations thereof.

2. A solid oral dosage form according to claim 1, wherein component (a) is present in an amount ranging from 25 to 47% by weight based on the total weight of the oral dosage form.

3. A solid oral dosage form according to claim 1 or 2, wherein component (a) is present in an amount ranging from 28 to 44% by weight based on the total weight of the oral dosage form.

4. A solid oral dosage form according to any of the preceding claims, wherein component (a) is present in an amount ranging from about 75 to about 600 mg of the free base per unit dosage form.

5. A solid oral dosage form according to any of the preceding claims, wherein component (a) is present in an amount ranging from about 75 to about 300 mg of the free base per unit dosage form.

6. A solid oral dosage form according to any of the preceding claims, wherein component (a) is present in an amount of about 83, about 166 or about 332 mg per unit dosage form.

7. A solid oral dosage form according to claim 1 , wherein component (b) is present in an amount ranging from 0.5 to 10% by weight based on the total weight of the oral dosage form.

8. A solid oral dosage form according to claim 1 or 2, wherein component (b) is present in an amount ranging from 1.4 to 5.5% by weight based on the total weight of the oral dosage form.

9. A solid oral dosage form according to any of the preceding claims, wherein component

(b) is present in an amount ranging from about 12.5 to about 25 mg per unit dosage form.

10. A solid oral dosage form according to claim 1 , wherein component (c) is present in an amount ranging from 3 to 30% by weight based on the total weight of the oral dosage form.

11. A solid oral dosage form according to claim 1 or 2, wherein component (c) is present in an amount ranging from 5 to 25% by weight based on the total weight of the oral dosage form.

12. A solid oral dosage form according to any of the preceding claims, wherein component

(c) is present in an amount ranging from about 30 mg to about 150 mg per unit dosage form.

13. A solid oral dosage form according to any of the preceding claims, wherein component (c) is present in an amount ranging from about 50 to about 100 mg per unit dosage form.

14. A solid oral dosage form according to any of the preceding claims, wherein component (c) is selected from the group of carbohydrates and combinations thereof , e. g. consisting of confectioner's sugar, compressible sugar, dextrates, dextrin, dextrose, lactose, mannitol, sorbitol, sucrose, starch such as corn starch, potato starch or wheat starch.

15. A solid oral dosage form according to any of the preceding claims, wherein component (c) is present as a mixture of wheat starch and lactose.

16. A solid oral dosage form according to any of the preceding claims, wherein the dosage form further comprises a further filler.

17. A solid oral dosage form according to any of the preceding claims, wherein the filler is microcrystalline cellulose.

18. A solid oral dosage form according to any of the preceding claims, wherein the dosage form further comprises a disintegrant.

19. A solid oral dosage form according to any of the preceding claims, wherein the disintegrant is crosslinked PVP.

20. A solid oral dosage form according to any of the preceding claims, wherein the disintegrant is present in an amount of 8 to 14, preferably 9 to 13, % by weight per unit dosage form.

21. A solid oral dosage form according to any of the preceding claims, wherein the dosage form further comprises a lubricant.

22. A solid oral dosage form according to any of the preceding claims, wherein the dosage form further comprises a glidant.

23. A solid oral dosage form according to any of the preceding claims, wherein the dosage form further comprises a binder.

24. A solid oral dosage form according according to any of the preceding claims for the treatment of hypertension, congestive heart failure, angina, myocardial infarction, artherosclerosis, diabetic nephropathy, diabetic cardiac myopathy, renal insufficiency, peripheral vascular disease, left ventricular hypertrophy, cognitive dysfunction, stroke, headache and chronic heart failure.

25. A solid oral dosage form according according to any of the preceding claims for the treatment of hypertension.

26. A method for the treatment of hypertension, congestive heart failure, angina, myocardial infarction, artherosclerosis, diabetic nephropathy, diabetic cardiac myopathy, renal insufficiency, peripheral vascular disease, left ventricular hypertrophy, cognitive dysfunction, stroke, headache and chronic heart failure which method comprises administering a therapeutically effective amount of a solid oral dosage form according to claims 1 to 24 to a patient in need thereof.

27. A method according to claim 26 for the treatment of hypertension.

28. Use of a solid oral dosage form according to claims 1 to 24 for the manufacture of a medicament for the treatment of hypertension, congestive heart failure, angina, myocardial infarction, artherosclerosis, diabetic nephropathy, diabetic cardiac myopathy, renal insufficiency, peripheral vascular disease, left ventricular hypertrophy, cognitive dysfunction, stroke, headache and chronic heart failure.

29. Use according to claim 28 for the treatment of hypertension.

30. A process for the manufacture of a solid oral dosage form according to any of claims 1 to 24 comprising the steps of:
i) granulating

a) a therapeutically effective amount of Aliskiren, or a pharmaceutically acceptable
salt thereof,

b) a therapeutically effective amount of hydrochlorothiazide (HCTZ)1 and

c) a hydrophilic filler selected from a carbohydrate or combinations thereof and additives with a granulation liquid;
ii) drying a resulting granulate;
iii) mixing the dried granulate with outer phase excipients;
iv) compressing a resulting mixture to form a solid oral dosage as a core tablet; and v) optionally coating a resulting core tablet to give a film-coated tablet.

31. A process according to claim 30, wherein the preparation of he granular phase in steps (i) and (ii) is performed as two separate phases, one containing the component (a), the other containing the component (b), whereby the two granular phases are combined prior to step (iϋ).

32. A process according to claim 31 , wherein component (c) is present in the granular phase containing component (b).