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Details for Patent: RE38629

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Details for Patent: RE38629

Title: Solid oral dosage form comprising a combination of metformin and glibenclamide
Abstract:The present invention relates to a solid oral dosage form comprising a combination of metformin and glibenclamide in which the size of glibenclamide is such that the glibenclamide bioavailability is comparable to the glibenclamide bioavailability obtained with a separate administration of metformin and glibenclamide.
Inventor(s): Bonhomme; Yves (Charbonnieres les Bains, FR), Nicholson; Geoffrey (Aylesbury, GB), Cave; Gillian (Flintshire, GB), Nicholson; Sarah J. (Cheshire, GB)
Assignee: Merck Sante (Lyons, FR)
Filing Date:Dec 27, 2002
Application Number:10/329,426
Claims:1. A solid oral dosage form comprising a combination of metformin and glibenclamide in which the size of the glibenclamide is such that at most 10% of the particles are less than 2 .mu.m and at most 10% of the particles are greater than 60 .mu.m, so that the glibenclamide bioavailability is comparable to the glibenclamide bioavailability obtained with a separate administration of metformin and glibenclamide.

2. A solid pharmaceutical composition comprising metformin and glibenclamide in particulate form, wherein the size of the glibenclamide particles is such that at most 10% of the particles are less than 2 .mu.m and at most 10% of the particles are greater than 60 .mu.m.

3. A solid oral dosage form as claimed in claim 1 in which the size of the glibenclamide is such that at most 10% of the particles are less than 3 .mu.m and at most 10% of the particles are greater than .[.60.]. .Iadd.40 .Iaddend..mu.m.

4. A solid oral dosage form comprising a combination of metformin and glibenclamide in which the size of glibenclamide is such that at most 25% of the particles are less than 11 .mu.m and at most 25% of the particles are greater than 46 .mu.m.

5. A solid oral dosage form .Iadd.of claim 4 .Iaddend.in which 50% of particles are less than 23 .mu.m.

6. A solid oral dosage form as claimed in claim 1 in which metformin is present as metformin salt and the weight ratio of metformin salt to glibenclamide is 50/1 to 250/1.

7. A solid oral dosage form as claimed in claim 1 which is a tablet.

8. A tablet as claimed in claim 7 which is obtained by a process comprising: a) forming granules by wet granulation of a mixture of metformin and glibenclamide; b) blending the granules with a tabletting aid c) tabletting the blend thus obtained into tablets.

9. A method for treating non-insulin dependent diabetes or hyperglycaemia, comprising administering to a subject in need thereof, the composition of claim 1.

10. A method for treating non-insulin dependent diabetes or hyperglycemia, comprising administering to a subject in need thereof, the composition of claim 2..Iadd.

11. A pharmaceutical composition comprising a single solid oral dosage form containing an effective dose of metformin and an effective dose of glibenclamide wherein, after oral administration thereof to a human, the bioavailability of glibenclamide is comparable to the bioavailability of glibenclamide achieved by oral administration of separate solid oral dosage forms to a human, one containing glibenclamide and the other metformin, in the same respective effective doses as in said single oral dosage form..Iaddend..Iadd.

12. A pharmaceutical composition comprising a single solid oral dosage form containing an effective dose of metformin and an effective dose of glibenclamide wherein, after oral administration thereof to a human, the C.sub.max and AUC of glibenclamide are comparable to the C.sub.max and AUC of glibenclamide achieved by oral administration of separate solid oral dosage forms to a human, one containing glibenclamide and the other metformin, in the same respective effective doses as in said single oral dosage form..Iaddend..Iadd.

13. A pharmaceutical composition comprising a single solid oral dosage form containing an effective dose of metformin and an effective dose of glibenclamide wherein, after oral administration thereof to a human, the C.sub.max and AUC of glibenclamide are .+-.25% of the C.sub.max and AUC, respectively, of the glibenclamide achieved by oral administration to a human of separate solid oral dosage forms, one containing glibenclamide and the other metformin, in the same respective effective doses as in said single oral dosage form..Iaddend..Iadd.

14. A pharmaceutical composition comprising a single solid oral dosage form containing an effective dose of metformin and an effective dose of glibenclamide wherein, after oral administration thereof to a human, the mean C.sub.max and mean AUC values of glibenclamide are, respectively, .+-.25% of 113 ng/ml and .+-.25% of 842 ng/ml/hr, for a 5 mg unit dose of glibenclamide, or proportionally higher or lower values for higher or lower unit doses of glibenclamide, respectively..Iaddend..Iadd.

15. A pharmaceutical composition comprising a single solid oral dosage form containing an effective dose of metformin and an effective dose glibenclamide wherein, after oral administration thereof to a human, the adjusted geometric mean C.sub.max and adjusted geometric mean AUC values of glibenclamide are, respectively, .+-.25% of 101 ng/ml and .+-.25% of 780 ng/ml/hr, for a 5 mg unit dose of glibenclamide, or proportionally higher or lower values for higher or lower unit doses of glibenclamide, respectively..Iaddend..Iadd.

16. A composition of one of claims 11-15 wherein the weight ratio of metformin to glibenclamide is 50/1 to 250/1..Iaddend..Iadd.

17. A composition of one of claims 11-15 wherein the weight ratio of metformin to glibenclamide is about 100/1..Iaddend..Iadd.

18. A composition of one of claims 11-15 wherein the weight ratio of metformin to glibenclamide is about 200..Iaddend..Iadd.

19. A composition of one of claims 11-15 wherein the unit dose of metformin is about 500 mg or about 250 mg..Iaddend..Iadd.

20. A composition of claim 19 wherein the unit dose of glibenclamide is 5, 2.5 or 1.25 mg..Iaddend..Iadd.

21. A composition of one of claims 11-15 in the form of a tablet or capsule..Iaddend..Iadd.

22. A composition of claim 13 wherein said C.sub.max and AUC values of glibenclamide in said single solid oral dosage form are .+-.20% of said C.sub.max and AUC values, respectively, of glibenclamide in said separate glibenclamide solid oral dosage form..Iaddend..Iadd.

23. A composition of claim 13 wherein said C.sub.max and AUC values of glibenclamide in said single solid oral dosage form are .+-.15% of said C.sub.max and AUC values, respectively, of glibenclamide in said separate glibenclamide solid oral dosage form..Iaddend..Iadd.

24. A composition of claim 13 wherein said C.sub.max and AUC values of glibenclamide in said single solid oral dosage form are .+-.10% of said C.sub.max and AUC values, respectively, of glibenclamide in said separate glibenclamide solid oral dosage form..Iaddend..Iadd.

25. A composition of claim 13 wherein said C.sub.max and AUC values of glibenclamide in said single solid oral dosage form are .+-.5% of said C.sub.max and AUC values, respectively, of glibenclamide in said separate glibenclamide solid oral dosage form..Iaddend..Iadd.

26. A composition of one of claims 14 or 15 wherein said C.sub.max and AUC values are .+-.20% of said numerical ranges..Iaddend..Iadd.

27. A composition of one of claims 14 or 15 wherein said C.sub.max and AUC values are .+-.15% of said numerical ranges..Iaddend..Iadd.

28. A composition of one of claims 14 or 15 wherein said C.sub.max and AUC values are .+-.10% of said numerical ranges..Iaddend..Iadd.

29. A composition of one of claims 14 or 15 wherein said C.sub.max and AUC values are .+-.5% of said numerical ranges..Iaddend..Iadd.

30. A method of treating non-insulin dependent diabetes or hyperglycemia comprising administering to a patient in need thereof a composition of one of claims 11-15..Iaddend..Iadd.

31. A method of achieving a bioavailability of glibenclamide in a human upon administering orally a single solid oral dosage form containing an effective dose of metformin and an effective dose of glibenclamide, said bioavailability being comparable to the bioavailability of glibenclamide achieved by oral administration of separate solid oral dosage forms to a human, one containing glibenclamide and the other metformin, in the same respective effective doses as in said single oral dosage form, comprising formulating glibenclamide with metformin in said single solid oral dosage form so as to assure said comparable bioavailability..Iaddend..Iadd.

32. A method of increasing bioavailability of glibenclamide in a human upon administering orally a single solid oral dosage form containing an effective dose of metformin and an effective dose of glibenclamide, such that said increased bioavailability is comparable to the bioavailability of glibenclamide achieved by oral administration of separate solid oral dosage forms to a human, one containing glibenclamide and the other metformin, in the same respective effective doses as in said single oral dosage form, comprising formulating glibenclamide with metformin in said single solid oral dosage form so as to assure said comparable bioavailability..Iaddend..Iadd.

33. A composition of one of claims 11-15 wherein metformin is present as a metformin salt..Iaddend..Iadd.

34. A method of one of claims 31-32 wherein metformin is present as a metformin salt..Iaddend..Iadd.

35. A method of claim 30 wherein metformin is present as a metformin salt..Iaddend.
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