# US 2021/0267902 A1 · Pharmaceutical compositions

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- Number: US 2021/0267902 A1
- Document ID: US20210267902A1
- Status: Published application
- Kind: A1
- Application number: 17/123,366
- Filed: 2020-12-16
- Published: 2021-09-02
- Earliest claimed: 2011-03-07
- Assignees: Boehringer Ingelheim International GmbH
- Applicants: Boehringer Ingelheim International GmbH
- Inventors: Masanori ITO; Kenji EGUSA; Roman MESSERSCHMID; Peter SCHNEIDER
- Web page: https://patentgrep.com/patent/US20210267902A1

## CPC

- A61K 9/209: {containing drug in at least two layers or in the core and in at least one outer layer}
- A61K 9/0053: {Mouth and digestive tract, i.e. intraoral and peroral administration}
- A61K 9/2054: {Cellulose; Cellulose derivatives, e.g. hydroxypropyl methylcellulose}
- A61K 9/2813: {Inorganic compounds}
- A61K 9/2853: {obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyethylene glycol, polyethylene oxide, poloxamers, poly(lactide-co-glycolide)}
- A61K 9/2866: {Cellulose; Cellulose derivatives, e.g. hydroxypropyl methylcellulose}
- A61K 31/155: Amidines ([IMAGE cpc-sch-A61K-1029.gif]), e.g. guanidine (H2N—C(=NH)—NH2), isourea (N=C(OH)—NH2), isothiourea (—N=C(SH)—NH2)
- A61K 31/522: having oxo groups directly attached to the heterocyclic ring, e.g. hypoxanthine, guanine, acyclovir
- A61K 31/7048: having oxygen as a ring hetero atom, e.g. leucoglucosan, hesperidin, erythromycin, nystatin {, digitoxin or digoxin}
- A61K 45/06: Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
- A61P 1/16: for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
- A61P 3/00: Drugs for disorders of the metabolism (of the blood or the extracellular fluid A61P7/00)
- A61P 3/04: Anorexiants; Antiobesity agents
- A61P 3/06: Antihyperlipidemics
- A61P 3/08: for glucose homeostasis (pancreatic hormones A61P5/48)
- A61P 3/10: for hyperglycaemia, e.g. antidiabetics
- A61P 9/00: Drugs for disorders of the cardiovascular system
- A61P 9/04: Inotropic agents, i.e. stimulants of cardiac contraction; Drugs for heart failure
- A61P 9/06: Antiarrhythmics
- A61P 9/10: for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
- A61P 13/02: of urine or of the urinary tract, e.g. urine acidifiers
- A61P 13/12: of the kidneys
- A61P 17/02: for treating wounds, ulcers, burns, scars, keloids, or the like
- A61P 25/00: Drugs for disorders of the nervous system
- A61P 27/02: Ophthalmic agents
- A61P 27/12: for cataracts
- A61P 43/00: Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
- A61K: PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES (devices or methods specially adapted for bringing pharmaceutical products into particular physical or administering forms A61J3/00; chemical aspects of, or use of materials for deodorisation of air, for disinfection or sterilisation, or for bandages, dressings, absorbent pads or surgical articles A61L; soap compositions C11D)
- A61P: SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS

## 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

### Claim 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 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.

### Claim 2 (depends on 1)

The pharmaceutical composition according to claim 1, wherein the film-coating agent is hydroxypropyl methylcellulose.

### Claim 3 (depends on 1)

The pharmaceutical composition according to claim 1, wherein the plastizicer is polyethylene glycol.

### Claim 4 (depends on 1)

The pharmaceutical composition according to claim 1, wherein the plastizicer is propylene glycol.

### Claim 5 (depends on 1)

The pharmaceutical composition according to claim 1, wherein the optional glidant is talc.

### Claim 6 (depends on 1)

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.

### Claim 7 (depends on 1)

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.

### Claim 8 (depends on 1)

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.

### Claim 9 (depends on 1)

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

### Claim 10 (depends on 9)

The tablet according to claim 9 further comprising an outer film over-coat.

### Claim 11 (depends on 10)

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.

### Claim 12 (depends on 1)

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,
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.

### Claim 13 (depends on 12)

The method of claim 12, wherein the metabolic disease is type 2 diabetes mellitus and conditions related thereto.

### Claim 14 (depends on 12)

The method of claim 12, wherein the SGLT-2 inhibitor is 1-chloro-4-(β-D-glucopyranos-1-yl)-2-[4-((S)-tetrahydrofuran-3-yloxy)-benzyl]-benzene.

### Claim 15 (depends on 7)

The pharmaceutical composition according to claim 7, wherein the hydroxypropyl methylcellulose is Hypromellose 2910, Methocel E5, or Methocel E15.

### Claim 16 (depends on 3)

The pharmaceutical composition according to claim 3, wherein the polyethylene glycol is Macrogol 400, 6000 or 8000.