# US 11,304,937 B2 · Medicinal composition for inhalation

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- Number: US 11,304,937 B2
- Document ID: US11304937B2
- Status: Granted
- Kind: B2
- Application number: 16/316,261
- Filed: 2017-07-12
- Published: 2019-08-01
- Granted: 2022-04-19
- Earliest claimed: 2016-07-12
- Assignees: Shionogi & Co., Ltd.
- Applicants: Shionogi & Co., Ltd.
- Inventors: Takeshi Funaki; Yukiko Nishino; Yuki Masuda; Koichi Tsubone
- Web page: https://patentgrep.com/patent/US11304937B2

## CPC

- A61K 31/4418: having a carbocyclic group directly attached to the heterocyclic ring, e.g. cyproheptadine
- A61K 9/0075: {for inhalation via a dry powder inhaler [DPI], e.g. comprising micronized drug mixed with lactose carrier particles}
- A61K 9/143: {with inorganic compounds}
- A61K 9/145: {with organic compounds}
- A61K 9/146: {with organic macromolecular compounds}
- A61K 9/48: Preparations in capsules, e.g. of gelatin, of chocolate {(A61K9/0004 takes precedence; bite capsules A61K9/0056)}
- A61K 47/10: Alcohols; Phenols; Salts thereof, e.g. glycerol; Polyethylene glycols [PEG]; Poloxamers; PEG/POE alkyl ethers
- A61K 47/12: Carboxylic acids; Salts or anhydrides thereof
- A61K 47/14: Esters of carboxylic acids, e.g. fatty acid monoglycerides, medium-chain triglycerides, parabens or PEG fatty acid esters
- A61K 47/24: containing atoms other than carbon, hydrogen, oxygen, halogen, nitrogen or sulfur, e.g. cyclomethicone or phospholipids
- A61K 47/26: Carbohydrates, e.g. sugar alcohols, amino sugars, nucleic acids, mono-, di- or oligo-saccharides; Derivatives thereof, e.g. polysorbates, sorbitan fatty acid esters or glycyrrhizin
- A61K 47/32: Macromolecular compounds obtained by reactions only involving carbon-to-carbon unsaturated bonds, e.g. carbomers {, poly(meth)acrylates, or polyvinyl pyrrolidone}
- A61K 47/38: Cellulose; Derivatives thereof
- A61K 47/44: Oils, fats or waxes according to two or more groups of A61K47/02-A61K47/42; Natural or modified natural oils, fats or waxes, e.g. castor oil, polyethoxylated castor oil, montan wax, lignite, shellac, rosin, beeswax or lanolin (synthetic glycerides, e.g. medium-chain triglycerides, A61K47/14)
- A61P 11/00: Drugs for disorders of the respiratory 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

The present invention provides a particle comprising pirfenidone and a lipid, particularly magnesium stearate, and having a mean particle diameter of 5 μm or less, and a powder formulation comprising the particle and a carrier.

## Claims

### Claim 1

A powder formulation comprising a micronized particle and a carrier,
wherein the micronized particle comprises pirfenidone and magnesium stearate and has a mean particle diameter of 5 μm or less,
wherein a content of the magnesium stearate is 0.02 wt % to 0.90 wt % of the powder formulation, and
wherein a content of the pirfenidone is 12.5 wt % to 15.0 wt % of the powder formulation.

### Claim 2 (depends on 1)

The powder formulation according to claim 1, wherein a weight ratio between the pirfenidone and the magnesium stearate is in the range of 10:1 to 500:1.

### Claim 3 (depends on 1)

The powder formulation according to claim 1, wherein the carrier is selected from the group consisting of a saccharide, a sugar alcohol and a macromolecular polymer.

### Claim 4 (depends on 1)

The powder formulation according to claim 1, wherein the carrier is a saccharide, and the saccharide is selected from the group consisting of lactose, glucose, saccharose, trehalose and sucrose.

### Claim 5 (depends on 4)

The powder formulation according to claim 4, wherein the carrier is a saccharide, and the saccharide is lactose.

### Claim 6 (depends on 1)

The powder formulation according to claim 1, wherein the carrier is a sugar alcohol, and the sugar alcohol is selected from the group consisting of erythritol, mannitol and sorbitol.

### Claim 7 (depends on 1)

The powder formulation according to claim 1, wherein the carrier is a macromolecular polymer, and the macromolecular polymer is selected from the group consisting of calcium carmellose, polyvinyl pyrrolidone and methylcellulose.

### Claim 8 (depends on 1)

The powder formulation according to claim 1, wherein the carrier has a mean particle diameter of 10 μm to 250 μm.

### Claim 9 (depends on 1)

The powder formulation according to claim 1, wherein a weight ratio between the micronized particle and the carrier is 0.1:100 to 100:0.1.

### Claim 10 (depends on 1)

The powder formulation according to claim 1, wherein the content of the magnesium stearate is 0.02 wt % to 0.5 wt % of the powder formulation.

### Claim 11 (depends on 1)

The powder formulation according to claim 1, wherein the content of the magnesium stearate is 0.02 wt % to 0.5 wt % of the powder formulation, the carrier is lactose, and the content of the lactose is 69.5 wt % to 94.98 wt % of the powder formulation.

### Claim 12 (depends on 1)

A process for producing the powder formulation according to claim 1, comprising mixing pirfenidone and magnesium stearate, wherein a content of the magnesium stearate is 0.02 wt % to 0.90 wt % of the powder formulation and a content of the pirfenidone is 12.5 wt % to 15.0 wt % of the powder formulation, then micronizing the mixture by grinding the mixture using a jet mill grinder to produce a micronized particle, and then combining the micronized particle with a carrier to obtain the powder formulation.

### Claim 13 (depends on 1)

A process for producing the powder formulation according to claim 1, comprising grinding pirfenidone in the coexistence of magnesium stearate to obtain a micronized particle comprising pirfenidone and magnesium stearate and having a mean particle diameter of 5 μm or less, wherein a content of the magnesium stearate is 0.02 wt % to 0.90 wt % of the powder formulation and a content of the pirfenidone is 12.5 wt % to 15.0 wt % of the powder formulation, and mixing the micronized particle with a carrier to obtain the powder formulation.