# US 12,178,814 B2 · Pharmaceutical composition

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- Number: US 12,178,814 B2
- Document ID: US12178814B2
- Status: Granted
- Kind: B2
- Application number: 17/441,361
- Filed: 2020-04-02
- Published: 2022-05-19
- Granted: 2024-12-31
- Earliest claimed: 2019-04-03
- Assignees: Astellas Pharma Inc.
- Applicants: Astellas Pharma Inc.
- Inventors: Akihiko Sasaki; Ko Tanaka; Masakazu Miyazaki; Seiji Takae
- Web page: https://patentgrep.com/patent/US12178814B2

## CPC

- A61K 31/497: containing further heterocyclic rings
- A61K 9/0095: {Drinks; Beverages; Syrups; Compositions for reconstitution thereof, e.g. powders or tablets to be dispersed in a glass of water; Veterinary drenches (A61K9/0007 takes precedence; eatable gels or foams A61K9/0056; oral mucosa adhesive forms A61K9/006)}
- A61K 9/1623: {Sugars or sugar alcohols, e.g. lactose; Derivatives thereof; Homeopathic globules}
- A61K 9/2018: {Sugars, or sugar alcohols, e.g. lactose, mannitol; Derivatives thereof, e.g. polysorbates}
- A61K 9/1694: {resulting in granules or microspheres of the matrix type containing more than 5% of excipient}
- A61K 9/2013: {Organic compounds, e.g. phospholipids, fats}
- 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)

## Abstract

Provided is a pharmaceutical composition containing 6-ethyl-3-{3-methoxy-4-[4-(4-methylpiperazin-1-yl)piperidin-1-yl]anilino}-5-[(oxan-4-yl)amino]pyrazine-2-carboxamide or a pharmaceutically acceptable salt thereof and a sweetener for reducing the bitterness of gilteritinib, suppressing the decrease in dissolution stability of gilteritinib due to, for example, stress such as heat and/or humidity over time, and having excellent dissolution stability. The pharmaceutical composition contains gilteritinib or a pharmaceutically acceptable salt thereof, a sweetener, and sugars and/or sugar alcohols.

## Claims

### Claim 1

A pharmaceutical composition comprising 6-ethyl-3-{3-methoxy-4-[4-(4-methylpiperazin-1-yl) piperidin-1-yl] anilino}-5-[(oxan-4-yl) amino] pyrazine-2-carboxamide or a pharmaceutically acceptable salt thereof, a sweetener, and two or more sugars and/or sugar alcohols.

### Claim 2 (depends on 1)

The pharmaceutical composition according to claim 1, wherein the sweetener is one, or two or more compounds selected from the group consisting of saccharin, acesulfame potassium, aspartame, and sucralose, and a mixture thereof.

### Claim 3 (depends on 1)

The pharmaceutical composition according to claim 1, wherein the sweetener is sucralose.

### Claim 4 (depends on 1)

The pharmaceutical composition according to claim 1, wherein the sugars are disaccharides and the sugar alcohols have 6 or 12 carbon atoms.

### Claim 5 (depends on 1)

The pharmaceutical composition according to claim 1, wherein the two or more sugars and/or sugar alcohols are selected from the group consisting of mannitol, isomalt hydrate, maltitol, sorbitol, lactose, sucrose, and trehalose, and a mixture thereof.

### Claim 6 (depends on 1)

The pharmaceutical composition according to claim 1, wherein one of the two or more sugars and/or sugar alcohols is mannitol.

### Claim 7 (depends on 1)

The pharmaceutical composition according to claim 1, wherein one of the two or more sugars and/or sugar alcohols is selected from the group consisting of isomalt hydrate, maltitol, sorbitol, sucrose, and trehalose.

### Claim 8 (depends on 1)

The pharmaceutical composition according to claim 1, wherein one of the two or more sugars and/or sugar alcohols is isomalt hydrate.

### Claim 9 (depends on 7)

The pharmaceutical composition according to claim 7, wherein a content of the one of the two or more sugars and/or sugar alcohols with respect to a weight of the pharmaceutical composition is 1% by weight to 20% by weight.

### Claim 10 (depends on 7)

The pharmaceutical composition according to claim 7, wherein the one of the two or more sugars and/or sugar alcohols is used as a binder.

### Claim 11 (depends on 1)

The pharmaceutical composition according to claim 1, wherein the pharmaceutically acceptable salt thereof is a hemifumarate.

### Claim 12 (depends on 1)

The pharmaceutical composition according to claim 1, wherein the pharmaceutical composition is solid.

### Claim 13 (depends on 1)

The pharmaceutical composition according to claim 1, further comprising a disintegrating agent.

### Claim 14 (depends on 12)

The pharmaceutical composition according to claim 12, wherein the pharmaceutical composition is a tablet.

### Claim 15 (depends on 1)

The pharmaceutical composition according to claim 1, wherein the pharmaceutical composition is dissolved or dispersed in a suitable solvent, and is a solution, suspension, paste, or gel.