IP Library › Patent Application 15140865
Patent Application
App. No. 15/140,865

PHARMACEUTICAL COMPOSITIONS

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Quick Facts
Patent No.
US None
App. No.
15/140,865
Abstract

The present invention relates to pharmaceutical compositions comprising fixed dose combinations of a DPP-4 inhibitor drug and/or a SGLT-2 inhibitor drug, and metformin XR, processes for the preparation thereof, and their use to treat certain diseases.

Claims (36)

1 . A pharmaceutical composition comprising:

a) an inner extended release core comprising metformin or metformin hydrochloride and one or more excipients;

b) an optional intermediate seal coating; and

c) an outer immediate release coating comprising at least one active pharmaceutical ingredient, wherein said at least one pharmaceutical ingredient is a SGLT-2 inhibitor,

and one or more excipients.

2 . The pharmaceutical composition according to claim 1 , wherein the inner extended release core a) is a formulation comprising metformin hydrochloride, a swellable and/or extended release polymer, and one or more further excipients.

3 . (canceled)

4 . (canceled)

5 . The pharmaceutical composition according to claim 1 , wherein the outer immediate release coating c) is a film coat formulation comprising 1-chloro-4-(β-D-glucopyranos-1-yl)-2-[4-((S)-tetrahydrofuran-3-yloxy)-benzyl]-benzene, a film-coating agent, a plasticizer, and, optionally, a glidant.

6 . (canceled)

7 . The pharmaceutical composition according to claim 5 , wherein the film-coating agent is hydroxypropyl methylcellulose, e.g. Hypromellose 2910, Methocel E5, or Methocel E15.

8 . (canceled)

9 . The pharmaceutical composition according to claim 5 , wherein the plastizicer is polyethylene glycol, e.g. Macrogol 400, 6000 or 8000.

10 . (canceled)

11 . The pharmaceutical composition according to claim 5 , wherein the plastizicer is propylene glycol

12 . (canceled)

13 . The pharmaceutical composition according to claim 5 , wherein the optional glidant is talc.

14 . The pharmaceutical composition according to claim 1 , wherein the seal coating is present.

15 . The pharmaceutical composition according to claim 14 , wherein the seal coating comprises a film-coating agent, a plasticizer, and, optionally, a glidant, one or more pigments and/or colors.

16 . The pharmaceutical composition according to claim 1 , wherein the seal coating is absent.

17 . The pharmaceutical composition according to claim 1 , wherein the metformin hydrochloride is present in a unit dosage strength of 500, 750, 850, 1000 or 1500 mg.

18 . (canceled)

19 . The pharmaceutical composition according to claim 1 , wherein the SGLT-2 inhibitor is 1-chloro-4-(β-D-glucopyranos-1-yl)-2-[4-((S)-tetrahydrofuran-3-yloxy)-benzyl]-benzene and is present in a unit dosage strength of 5, 10, 12.5 or 25 mg.

20 . The pharmaceutical composition according to claim 1 , which is a tablet for oral administration.

21 . The tablet according to claim 20 further comprising an outer film over-coat.

22 . The tablet according to claim 21 , wherein the outer film over-coat comprises a film-coating agent, a plasticizer, and, optionally, a glidant, one or more pigments and/or colors.

23 . A method of using the pharmaceutical composition according to claim 1 for treating, preventing, slowing the progression, or delaying the onset of metabolic diseases either in type 2 diabetes patients who have not been previously treated with an antihyperglycemic agent,

or in type 2 diabetes patients with insufficient glycemic control despite therapy with one or two conventional antihyperglycemic agents selected from metformin, sulphonylureas, thiazolidinediones, glinides, alpha-glucosidase blockers, GLP-1 or GLP-1 analogues, and insulin or insulin analogues.

24 . The method of claim 23 , wherein the metabolic disease is type 2 diabetes mellitus and conditions related thereto.

25 . The method of claim 23 , wherein the SGLT-2 inhibitor is 1-chloro-4-(β-D-glucopyranos-1-yl)-2-[4-((S)-tetrahydrofuran-3-yloxy)-benzyl]-benzene.

26 . A pharmaceutical composition comprising:

a) an inner extended release core comprising metformin hydrochloride and one or more excipients;

b) an optional intermediate seal coating; and

c) an outer immediate release coating comprising at least one active pharmaceutical ingredient, wherein said at least one active pharmaceutical ingredient is 1-chloro-4-(β-D-glucopyranos-1-yl)-2-[4-((S)-tetrahydrofuran-3-yloxy)-benzyl]-benzene,

and one or more excipients.

27 . The pharmaceutical composition according to claim 26 which is a tablet for oral administration.