# US 2021/0330648 A1 · Pharmaceutical composition and use thereof

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- Number: US 2021/0330648 A1
- Document ID: US20210330648A1
- Status: Published application
- Kind: A1
- Application number: 17/366,313
- Filed: 2021-07-02
- Published: 2021-10-28
- Earliest claimed: 2020-01-10
- Assignees: Alphala Co., Ltd & Chung-Chin Chen
- Applicants: Alphala Co., Ltd.
- Inventors: Chi-Jen HONG; Yen-Fu CHEN; Cheng-Ho CHUNG
- Web page: https://patentgrep.com/patent/US20210330648A1

## CPC

- A61K 31/4245: Oxadiazoles
- A61K 9/0053: {Mouth and digestive tract, i.e. intraoral and peroral administration}
- A61K 9/1641: {obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyethylene glycol, poloxamers}
- A61K 9/1652: {Polysaccharides, e.g. alginate, cellulose derivatives; Cyclodextrin (homeopathic globules A61K9/1623)}
- A61K 47/14: Esters of carboxylic acids, e.g. fatty acid monoglycerides, medium-chain triglycerides, parabens or PEG fatty acid esters
- A61K 47/38: Cellulose; Derivatives thereof
- A61P 1/00: Drugs for disorders of the alimentary tract or the digestive system
- 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

Disclosed is a pharmaceutical composition comprising: an active ingredient of the following formula (I) or a pharmaceutically acceptable salt or solvate thereof present in an amount of 8 wt % to 30 wt %: and two or more excipients at least including a dispersant and a solubilizer present in an amount of 70 wt % to 92 wt %. Also disclosed are methods for reducing the glycemic level and treating disorders associated with glucagon with the aforesaid pharmaceutical composition.

## Claims

### Claim 1

A pharmaceutical composition, comprising:
an active ingredient of the following formula (I) or a pharmaceutically acceptable salt or solvate thereof present in an amount of 8 wt % to 30 wt %:
two or more excipients at least including a dispersant and a solubilizer present in an amount of 70 wt % to 92 wt %.

### Claim 2 (depends on 1)

The pharmaceutical composition of claim 1, wherein a weight ratio of the dispersant to the solubilizer is ranged from 3.0 to 20.0.

### Claim 3 (depends on 1)

The pharmaceutical composition of claim 1, wherein the active ingredient of the formula (I) or the pharmaceutically acceptable salt or solvate thereof is present in an amount of 9 wt % to 28 wt %.

### Claim 4 (depends on 3)

The pharmaceutical composition of claim 3, wherein the active ingredient of the formula (I) or the pharmaceutically acceptable salt or solvate thereof is present in an amount of 10 wt % to 28 wt %.

### Claim 5 (depends on 4)

The pharmaceutical composition of claim 4, wherein the active ingredient of the formula (I) or the pharmaceutically acceptable salt or solvate thereof is present in an amount of 14.5 wt % to 20 wt %.

### Claim 6 (depends on 1)

The pharmaceutical composition of claim 1, wherein the dispersant is present in an amount of 40 wt % to 88 wt %.

### Claim 7 (depends on 6)

The pharmaceutical composition of claim 6, wherein the dispersant is present in an amount of 60 wt % to 85 wt %.

### Claim 8 (depends on 7)

The pharmaceutical composition of claim 7, wherein the dispersant is present in an amount of 70 wt % to 80 wt %.

### Claim 9 (depends on 1)

The pharmaceutical composition of claim 1, wherein the solubilizer is present in an amount of 2 wt % to 20 wt %.

### Claim 10 (depends on 9)

The pharmaceutical composition of claim 9, wherein the solubilizer is present in an amount of 5 wt % to 13 wt %.

### Claim 11 (depends on 10)

The pharmaceutical composition of claim 10, wherein the solubilizer is present in an amount of 5 wt % to 10 wt %.

### Claim 12 (depends on 1)

The pharmaceutical composition of claim 1, which is an oral pharmaceutical composition.

### Claim 13 (depends on 1)

The pharmaceutical composition of claim 1, wherein the dispersant comprises hypromellose acetate succinate.

### Claim 14 (depends on 1)

The pharmaceutical composition of claim 1, wherein the solubilizer comprises Macrogol 15 Hydroxystearate.

### Claim 15 (depends on 1)

The pharmaceutical composition of claim 1, wherein the active ingredient of the formula (I) or the pharmaceutically acceptable salt or solvate thereof is present in an amount of 10 wt % to 28 wt %; the dispersant is present in an amount of 60 wt % to 85 wt %; and the solubilizer is present in an amount of 5 wt % to 13 wt %.

### Claim 16 (depends on 15)

The pharmaceutical composition of claim 15, wherein the dispersant comprises hypromellose acetate succinate and the solubilizer comprises Macrogol 15 Hydroxystearate.

### Claim 17 (depends on 1)

The pharmaceutical composition of claim 1, wherein the active ingredient of the formula (I) or the pharmaceutically acceptable salt or solvate thereof is present in an amount of 14.5 wt % to 20 wt %; the dispersant is present in an amount of 70 wt % to 80 wt %; and the solubilizer is present in an amount of 5 wt % to 10 wt %.

### Claim 18 (depends on 17)

The pharmaceutical composition of claim 17, wherein the dispersant comprises hypromellose acetate succinate and the solubilizer comprises Macrogol 15 Hydroxystearate.

### Claim 19

A method for reducing the glycemic level in a subject, comprising administering to the subject in need thereof a pharmaceutical composition, wherein the pharmaceutical composition comprises:
an active ingredient of the following formula (I) or a pharmaceutically acceptable salt or solvate thereof present in an amount of 8 wt % to 30 wt %:
and
two or more excipients at least including a dispersant and a solubilizer preset in an amount of 70 wt % to 92 wt %.

### Claim 20

A method of treating disorders associated with glucagon, comprising administering to a subject in need thereof a pharmaceutical composition, wherein the pharmaceutical composition comprises:
an active ingredient of the following formula (I) or a pharmaceutically acceptable salt or solvate thereof present in an amount of 8 wt % to 30 wt %:
and
two or more excipients at least including a dispersant and a solubilizer present in an amount of 70 wt % to 92 wt %.