# US 9,517,204 B2 · Pharmaceutical composition for inhalation

> Agents: this data is available as JSON from the patentgrep API and MCP server — see https://patentgrep.com/llms.txt

- Number: US 9,517,204 B2
- Document ID: US9517204B2
- Status: Granted
- Kind: B2
- Application number: 14/344,467
- Filed: 2012-09-13
- Published: 2014-11-20
- Granted: 2016-12-13
- Earliest claimed: 2011-09-14
- Assignees: Shionogi & Co., Ltd.; Shizuoka Prefectural Universities Corporation
- Applicants: Satomi Onoue; Shizuo Yamada
- Inventors: Satomi Onoue; Shizuo Yamada
- Web page: https://patentgrep.com/patent/US9517204B2

## CPC

- A61K 9/14: Particulate form, e.g. powders, {Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles (microspheres A61K9/16; microcapsules A61K9/50; nanocapsules, nanoparticles of the matrix type A61K9/51)}
- A61K 9/0075: {for inhalation via a dry powder inhaler [DPI], e.g. comprising micronized drug mixed with lactose carrier particles}
- A61K 9/145: {with organic compounds}
- A61K 9/146: {with organic macromolecular compounds}
- A61K 31/4418: having a carbocyclic group directly attached to the heterocyclic ring, e.g. cyproheptadine
- 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
- A61P 11/00: Drugs for disorders of the respiratory system
- A61P 11/06: Antiasthmatics
- A61P 43/00: Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
- A61M 11/002: {by flow deviation causing inertial separation of transported particles}
- A61M 15/00: Inhalators {(drug delivery in endotracheal tubes A61M16/04)}
- A61M 2202/064: Powder
- 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
- A61M: DEVICES FOR INTRODUCING MEDIA INTO, OR ONTO, THE BODY (introducing media into or onto the bodies of animals A61D7/00; means for inserting tampons A61F13/26; devices for administering food or medicines orally A61J; containers for collecting, storing or administering blood or medical fluids A61J1/05); DEVICES FOR TRANSDUCING BODY MEDIA OR FOR TAKING MEDIA FROM THE BODY (surgery A61B; chemical aspects of surgical articles A61L); DEVICES FOR PRODUCING OR ENDING SLEEP OR STUPOR {(Electrotherapy, e.g. producing anaesthesia by the use of alternating or intermittent currents A61N1/36021)}

## Abstract

The present invention relates to a powder formulation which reduces side effect risk of a medicine having a side effect of drug-induced photodermatosis and increases therapeutic effect, and relates to the method for producing the same. Said powder formulation makes inhalation therapy possible by carrying out aerosolization easily, and since pharmacological effect in lung local part is increased, it is possible to decrease the dose. Skin transmigration of said medicine is controlled by a lung specific delivery technology, and photodermatosis which is a side effect can be controlled.

## Claims

### Claim 1

A powder formulation comprising:
(i) micronized particles with a mean particle diameter of 20 μm or less comprising
(i-1) pirfenidone and
(i-2) at least one excipient selected from the group consisting of a saccharide, a sugar alcohol, a fatty acid and salts thereof, a wax, calcium sulfate, calcium carbonate, talc and titanium oxide,
wherein the micronized particles exclude a polymer, and
(ii) a carrier with a mean particle diameter of 10 to 200 μm, wherein the micronized particles are adhered to the carrier.

### Claim 2 (depends on 1)

The powder formulation according to claim 1, wherein a particle diameter of the micronized particles is smaller than a mean particle diameter of the carrier.

### Claim 3 (depends on 1)

The powder formulation according to claim 1, wherein the saccharide is lactose.

### Claim 4 (depends on 1)

The powder formulation according to claim 1, wherein the sugar alcohol is erythritol.

### Claim 5 (depends on 1)

The powder formulation according to claim 1, wherein the excipient is erythritol and the carrier is lactose.

### Claim 6 (depends on 1)

The powder formulation according to claim 1, wherein a weight ratio between the pirfenidone and the excipient is in the range of 1:5000 to 10:1.

### Claim 7 (depends on 1)

The powder formulation according to claim 1, wherein a weight ratio between the micronized particles and the carrier is in the range of 1:100 to 10:1.

### Claim 8 (depends on 1)

The powder formulation according to claim 1, wherein a mean diameter of the micronized particles is in the range of 1 to 9 μm.

### Claim 9 (depends on 1)

The powder formulation according to claim 1, wherein the powder formulation is a transpulmonary inhalation formulation.

### Claim 10 (depends on 1)

The powder formulation according to claim 1, wherein a drug-inducement of photodermatosis of the pirfenidone has been reduced as compared with an oral administration formulation.

### Claim 11 (depends on 1)

A process for producing the formulation according to claim 1, comprising:
mixing micronized particles with a mean particle diameter of 20 μm or less comprising pirfenidone and an excipient with a carrier having a particle diameter of 10 to 200 μm.

### Claim 12 (depends on 11)

The process according to claim 11, wherein the micronized particles are prepared by mixing the pirfenidone and the excipient to obtain a mixture, and then micronizing the mixture with a jet mill.

### Claim 13 (depends on 12)

The process according to claim 12, wherein the micronized particles and the carrier are mixed in a container made from nylon or polyethylene.

### Claim 14 (depends on 11)

The process according to claim 11, wherein the micronized particles and the carrier form a complex.

### Claim 15 (depends on 11)

An inhalation formulation obtained by the process according to claim 11.