# US 11,304,907 B2 · Pharmaceutical compositions containing a DGAT1 inhibitor

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- Number: US 11,304,907 B2
- Document ID: US11304907B2
- Status: Granted
- Kind: B2
- Application number: 16/835,921
- Filed: 2020-03-31
- Published: 2020-07-23
- Granted: 2022-04-19
- Earliest claimed: 2010-10-14
- Assignees: Novartis AG
- Applicants: Novartis AG
- Inventors: Hong Wen; Natrajan Kumaraperumal; Richard Nause
- Web page: https://patentgrep.com/patent/US11304907B2

## CPC

- A61K 9/2054: {Cellulose; Cellulose derivatives, e.g. hydroxypropyl methylcellulose}
- A61K 9/2009: {Inorganic compounds}
- A61K 9/2013: {Organic compounds, e.g. phospholipids, fats}
- A61K 9/2018: {Sugars, or sugar alcohols, e.g. lactose, mannitol; Derivatives thereof, e.g. polysorbates}
- A61K 9/2027: {obtained by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyvinyl pyrrolidone, poly(meth)acrylates}
- A61K 9/2059: {Starch, including chemically or physically modified derivatives; Amylose; Amylopectin; Dextrin}
- A61K 9/2095: {Tabletting processes}
- A61K 9/2813: {Inorganic compounds}
- A61K 31/444: containing a six-membered ring with nitrogen as a ring heteroatom, e.g. amrinone
- 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 3/10: for hyperglycaemia, e.g. antidiabetics
- A61P 9/00: Drugs for disorders of the cardiovascular system
- A61P 17/00: Drugs for dermatological disorders
- A61P 29/00: Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
- A61P 35/00: Antineoplastic agents
- 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 a pharmaceutical composition comprising a) a therapeutically effective amount of a compound of formula (I), or a pharmaceutically acceptable salt thereof, b) one or more, e.g. 1, 2 or 3, surfactants with lubricant properties; c) one or more, e.g. 1, 2 or 3, dry binders with disintegrant properties; d) one or more, e.g. 1, 2 or 3, fillers, and e) one or more, e.g. 1, 2 or 3, disintegrants.

## Claims

### Claim 1

A pharmaceutical composition in the form of a tablet comprising
a) a therapeutically effective amount of the sodium salt of the compound trans-(4-{4-[5-(6-trifluoromethyl-pyridin-3-ylamino)-pyridin-2-yl]-phenyl}-cyclohexyl)-acetic acid of formula (I);
b) 2% of sodium lauryl sulfate by weight of the tablet prior to any optional film coating;
c) 10% of hydroxypropyl cellulose by weight of the tablet prior to any optional film coating;
d) 15 to 26% of microcrystalline cellulose by weight of the tablet prior to any optional film coating;
e) 0.5% of colloidal silica by weight of the tablet prior to any optional film coating;
f) 3% of sodium stearyl fumarate by weight of the tablet prior to any optional film coating;
g) 20 to 85% of anhydrous lactose by weight of the tablet prior to any optional film coating;
h) 2% of sodium starch glycolate by weight of the tablet prior to any optional film coating; and
i) an optional film coating.

### Claim 2 (depends on 1)

The pharmaceutical composition according to claim 1, further comprising 0.1 to 10% of magnesium stearate by weight of the tablet prior to any optional film coating.

### Claim 3 (depends on 1)

The pharmaceutical composition according to claim 1, further comprising a surfactant selected from stearic acid, palmitic acid, myristic acid, poloxamers, polyethylene glycols, the Tween series of surfactants, the Brij series of surfactants, Triton X-100, and combinations thereof.

### Claim 4 (depends on 1)

The pharmaceutical composition according to claim 1, further comprising a binder selected from polyethylene glycols, pregelatinized starch, starch, chitosan, guar gum, methyl cellulose, calcium carboxymethylcellulose, sodium carboxymethylcellulose, alginic acid, alginic acid sodium salt, hydroxypropylmethyl cellulose, hydroxypropyl cellulose and combinations thereof.

### Claim 5 (depends on 1)

The pharmaceutical composition according to claim 1, wherein the ratio of microcrystalline cellulose to anhydrous lactose is between 1:5 and 1:1.

### Claim 6 (depends on 1)

The pharmaceutical composition according to claim 1, further comprising croscarmellose sodium or cross-linked polyvinyl pyrrolidone as a disintegrant.

### Claim 7 (depends on 1)

The composition of claim 1, wherein the hydroxypropyl cellulose has a viscosity from 3 to 6 cps.

### Claim 8 (depends on 1)

The composition of claim 1, wherein the hydroxypropyl cellulose is low substituted hydroxypropyl cellulose (L-HPC LH-21).

### Claim 9 (depends on 1)

The composition of claim 1, further comprising 0.05 to 5% of one or more glidants selected from magnesium trisilicate, powdered cellulose, starch, talc and combinations thereof by weight of the tablet prior to any optional film coating.

### Claim 10 (depends on 1)

The composition of claim 1, wherein the film coating is comprised of hydroxypropyl methyl cellulose, polyethylene glycol and talc.

### Claim 11 (depends on 10)

The composition of claim 10, wherein the film coating further comprises iron oxide.

### Claim 12 (depends on 10)

The composition of claim 10, wherein the film coating further comprises titanium dioxide.

### Claim 13 (depends on 1)

A process for preparing a pharmaceutical composition according to claim 1 comprising the steps of:
(a) mixing the compound of the formula (I), or a pharmaceutically acceptable salt thereof, with at least one pharmaceutically acceptable excipient to form a blend;
(b) roller compacting, then milling said blend;
(c) lubricating the resulting mixture, and
(d) compressing the resulting mixture into a solid oral dosage form.