Claims for Patent: 10,596,120

Summary for Patent: 10,596,120

Title:	Pharmaceutical compositions
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.
Inventor(s):	Ito; Masanori (Mainz, DE), Egusa; Kenji (Osaka, JP), Messerschmid; Roman (Kobe, JP), Schneider; Peter (Ulm-Einsingen, DE)
Assignee:	Boehringer Ingelheim International GmbH (Ingelheim am Rhein, DE)
Application Number:	15/906,414
Patent Claims:	1. A pharmaceutical composition comprising: a) an inner extended release core, wherein the inner extended release core is a formulation comprising metformin hydrochloride, a swellable and/or extended release polymer, and one or more further excipients; b) an intermediate seal coating; and c) an outer immediate release coating, wherein the outer immediate release coating is a film coat formulation comprising the SGLT2-inhibitor 1-chloro-4-(.beta.-D-glucopyranos-1-yl)-2-[4-((S)-tetrahydrofuran-3-yloxy- )-benzyl]-benzene, a film-coating agent, a plasticizer, and, optionally, a glidant. 2. The pharmaceutical composition according to claim 1, wherein the film-coating agent is hydroxypropyl methylcellulose. 3. The pharmaceutical composition according to claim 1, wherein the plastizicer is polyethylene glycol. 4. The pharmaceutical composition according to claim 1, wherein the plastizicer is propylene glycol. 5. The pharmaceutical composition according to claim 1, wherein the optional glidant is talc. 6. The pharmaceutical composition according to claim 1, wherein the seal coating comprises a film-coating agent, a plasticizer, and, optionally, a glidant, one or more pigments and/or colors. 7. 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. 8. The pharmaceutical composition according to claim 1, wherein the SGLT-2 inhibitor is present in a unit dosage strength of 5, 10, 12.5 or 25 mg. 9. The pharmaceutical composition according to claim 1, which is a tablet for oral administration. 10. The tablet according to claim 9 further comprising an outer film over-coat. 11. The tablet according to claim 10, wherein the outer film over-coat comprises a film-coating agent, a plasticizer, and, optionally, a glidant, one or more pigments and/or colors. 12. 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; comprising administering the composition of claim 1 to said patient. 13. The method of claim 12, wherein the metabolic disease is type 2 diabetes mellitus and conditions related thereto. 14. The pharmaceutical composition according to claim 2, wherein the hydroxypropyl methylcellulose is Hypromellose 2910, Methocel E5, or Methocel E15. 15. The pharmaceutical composition according to claim 3, wherein the polyethylene glycol is Macrogol 400, 6000 or 8000. 16. The pharmaceutical composition according to claim 1, wherein the dosage strength is 5 mg of the SGLT2 inhibitor and 1000 mg metformin hydrochloride. 17. The pharmaceutical composition according to claim 1, wherein the dosage strength is 10 mg of the SGLT2 inhibitor and 1000 mg metformin hydrochloride. 18. The pharmaceutical composition according to claim 1, wherein the dosage strength is 12.5 mg of the SGLT2 inhibitor and 1000 mg metformin hydrochloride. 19. The pharmaceutical composition according to claim 1, wherein the dosage strength is 25 mg of the SGLT2 inhibitor and 1000 mg metformin hydrochloride. 20. The pharmaceutical composition according to claim 1, wherein the extended release material comprises poly(ethylene oxide) and/or hydroxypropyl methylcellulose (HPMC). 21. The pharmaceutical composition according to claim 6, wherein the film coating agent is a mixture of hydroxypropylcellulose and hydroxypropyl methylcellulose. 22. The pharmaceutical composition according to claim 1, wherein the outer immediate release coating comprises the SGLT2 inhibitor and 1-[(4-methyl-quinazolin-2- yl)methyl]-3-methyl-7-(2-butyn-1-yl)-8-(3-(R)-amino-piperidin-1-yl)-xanth- ine.